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Terms in this set (235)

Class: Viral DNA Polymerase Inhibitor
Dosage Forms. Capsule: 200 mg; Suspension: 200 mg/5 mL; Tablet: 400 mg, 800 mg
Common FDA Label Indication, Dosing, and Titration.
Genital herpes simplex: Adults, initial episode, 400 mg po tid or 200 mg po 5 times a day × 7-10 d; Adults, recurrent episode, 400 mg po tid × 5 d or 800 mg bid × 5 d or 800 mg tid × 2 d; Children ≥12 y of age, 1000-1200 mg/d po in 3-5 divided doses × 7-10 d
Genital herpes simplex, suppressive therapy: Adults and Children ≥12 y of age, 400 mg po bid for up to 12 mo
Herpes zoster (shingles): Adults and Children ≥12 y of age, 800 mg po 5 times a day × 7-10 d
Varicella (chickenpox): Adults and Children ≥2 y of age and ≥40 kg, 800 mg po qid × 5 d; Children ≥2 y of age and < 40 kg, 20 mg/kg po qid × 5 d
Off-Label Uses.
Genital herpes simplex in HIV-positive patients, initial or recurrent: 400 mg po tid × 5-10 d
Genital herpes simplex in HIV-positive patients, chronic suppression: 400-800 mg po bid-tid
Cold sores (orolabial herpes simplex virus [HSV]), treatment: 200-400 mg 5 times a day × 5 d
MOA. Acyclovir is an acyclic nucleoside analogue of deoxyguanosine that is selectively phosphorylated by the virus-encoded thymidine kinase to its monophosphate form. Cellular enzymes then convert the monophosphate to the active antiviral acyclovir triphosphate, which competitively inhibits viral DNA synthesis by inactivation of viral DNA polymerase and incorporation into and termination of viral DNA replication. Acyclovir has potent activity against HSV I and II and herpes zoster virus (varicella-zoster virus [VZV]).
Drug Characteristics: Acyclovir
Dose Adjustment Hepatic Not required Absorption F = 10-20%, food has no effect on absorption
Dose Adjustment Renal CrCl 10-25 mL/min, increase interval to q8h; CrCl <10 mL/min, increase interval to q12h Distribution Vd = 0.8 L/kg; 9-33% protein bound, placenta, CSF, kidney, brain, lung, heart
Dialyzable Hemodialysis removes 60% of dose. No adjustment for peritoneal (<10% removed) Metabolism Not metabolized
Pregnancy Category B Elimination Renal 62-90% with a half-life of 2.5-3.3 h
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity to acyclovir or valacyclovir Black Box Warnings None
Class: Anthelmintic
Dosage Forms. Tablet: 200 mg
Common FDA Label Indication, Dosing, and Titration.
Parenchymal neurocysticercosis caused by Taenia solium, cystic hydatid disease of the liver, lung, and peritoneum caused by Echinococcus granulosus: Adults ≥60 kg, 400 mg po bid with meals × 8-30 d; Adults and Children <60 kg, 15 mg/kg/d (max 800 mg/d) in 2 divided doses × 8-30 d
Off-Label Uses.
Ancylostoma caninum, Ascaris lumbricoides (roundworm),Ancylostoma duodenale (hookworm), and Necator americanus (hookworm): 400 mg po as a single dose
Enterobius vermicularis (pinworm): 400 mg po as a single dose, repeat in 2 wk
Giardia duodenalis (giardiasis): 400 mg po once daily × 5 d
MOA.Selective degeneration of cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae. This leads to impaired glucose uptake in parasites and ATP production decreases leading to energy depletion and death.
Drug Characteristics: Albendazole
Dose Adjustment Hepatic Use with caution in hepatic dysfunction Absorption F <5%, food enhances absorption up to 5 times
Dose Adjustment Renal Not required Distribution Cyst, CSF
Dialyzable Not dialyzable Metabolism Hepatic to 1 active metabolite; minor substrate of CYP3A4/5, 1A2
Pregnancy Category C Elimination Renal <1% with half-life of 8-15 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to albendazole Black Box Warnings None
Medication Safety Issues: Albendazole
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Aplenzin, Relenza No
Class: Selective β2-Adrenergic Agonist
Dosage Forms. Metered-Dose Inhaler (MDI), Aerosol Solution for Inhalation, Aerosol Powder for Inhalation, Dry Powder Inhaler (DPI): 90 (base) mcg/actuation; Tablet: 2 mg, 4 mg; Extended-Release Tablet: 4 mg, 8 mg; Syrup: 2 mg/5 mL; Nebulization Solution for Inhalation: 0.63 mg/3 mL, 2.5 mg/3 mL, 2.5 mg/0.5 mL
Common FDA Label Indication, Dosing, and Titration.
Asthma (acute exacerbation): Adults, MDI, 4-8 inhalations every 20 min up to 4 h, then every 1-4 h prn; Children, 4-8 inhalations every 20 min for 3 doses, then every 1-4 h prn (use mask for children <4 y of age)
Asthma (bronchospasm): Adults and Children, MDI/DPI, 2 inhalations every 4-6 h prn; Adults and Children ≥12 y of age, oral, 2-4 mg immediate-release tablet po tid or qid or 4-8 mg extended-release tablet po q12h (max 32 mg/d); Children 6-11 y of age, 2 mg immediate-release tablet po tid or qid or 4 mg extended-release tablet po q12h; Children 2-6 y of age, 0.1 mg/kg oral syrup po tid
Exercise-induced asthma, prevention: Adults, MDI/DPI, 2 inhalations 15-30 min prior to exercise; Children ≥4 y of age, 2 inhalations 15-30 min prior to exercise
Off-Label Uses.
None
MOA. Albuterol is a selective β2-adrenergic agonist that acts on β2-adrenergic receptors of intracellular adenylyl cyclase to increase cyclic AMP levels resulting in bronchial smooth muscle relaxation.
Drug Characteristics: Albuterol
Dose Adjustment Hepatic Not required Absorption F = 50-85% (oral tablet), 100% (extended-release tablet), food decreases rate (but not extent) of absorption of extended-release tablet
Dose Adjustment Renal Not required Distribution Vd = 156 L; 10% protein bound
Dialyzable Unknown Metabolism 20% via sulfotransferases
Pregnancy Category C Elimination Renal 80% with a half-life of 3.8 h (inhalation), 3.7-5 h (oral)
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Class: Bisphosphonate
Dosage Forms. Tablet: 5 mg, 10 mg, 35 mg, 40 mg, 70 mg; Solution: 70 mg/75 mL; Effervescent Tablet: 70 mg
Common FDA Label Indication, Dosing, and Titration.
Postmenopausal osteoporosis, prophylaxis: 5 mg po daily or 35 mg po once weekly
Postmenopausal osteoporosis, treatment: 10 mg po daily or 70 mg po once weekly
Osteoporosis, treatment, male: 10 mg once daily or 70 mg po once weekly
Glucocorticoid-induced osteoporosis in those with daily dosage ≥7.5 mg of prednisone (or equivalent): 5 mg po once daily; a dose of 10 mg po once daily should be used in postmenopausal females who are not receiving estrogen
Paget disease: 40 mg po daily for 6 mo
Off-Label Uses.
Postoperative knee arthroplasty: 10 mg po once daily beginning after knee arthroplasty for up to 1 y
Osteogenesis imperfecta: 10 mg po once daily or 70 mg po once weekly
MOA. Alendronate binds to bone hydroxyapatite, and at the cellular level, inhibits osteoclast activity, thereby inhibiting bone resorption and modulating bone metabolism.
Drug Characteristics: Alendronate
Dose Adjustment Hepatic Not required Absorption F <1%, food impairs absorption, take 30-60 min prior to meal
Dose Adjustment Renal CrCl <35 mL/min, avoid use Distribution Vd = 2576 L; 78% protein bound
Dialyzable Not dialyzable Metabolism Not metabolized
Pregnancy Category C Elimination Renal 50% with a half-life in bone of >10 y
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Esophageal abnormalities, hypersensitivity, hypocalcemia, inability to sit or stand upright for at least 30 min; increased risk for adverse esophageal effects Black Box Warnings None
Class: Benzodiazepine, Short or Intermediate. C-IV
Dosage Forms. Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg; Tablet, Disintegrating: 0.25 mg, 0.5 mg, 1 mg, 2 mg; Tablet, Extended Release: 0.5 mg, 1 mg, 2 mg, 3 mg; Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Anxiety: immediate-release, orally disintegrating tablet or solution, 0.25-0.5 mg po tid; max daily dose, 4 mg in divided doses
Panic disorder, with or without agoraphobia: immediate-release or orally disintegrating tablets, 0.5 mg po tid, extended-release 3-6 mg po daily; dose may be increased every 3-4 d by <1 mg/d
Off-Label Uses.
Alcohol withdrawal syndrome: 0.5-1 mg po bid × 7-10 d
MOA. Enhances the postsynaptic effect of the inhibitory neurotransmitter, γ-aminobutyric acid (GABA).
Drug Characteristics: Alprazolam
Dose Adjustment Hepatic Reduce initial dose to 0.25 mg in advanced liver disease Absorption F = 80%, no effect of food on absorption of immediate release, food increases absorption of ER formulation by 25%
Dose Adjustment Renal Not required Distribution Vd = 0.9-1.2 L/kg; 80% protein bound
Dialyzable Not dialyzable Metabolism Hepatic 20-30%; major substrate of CYP3A4/5
Pregnancy Category D Elimination Renal 80% with a half-life of 10-12 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to benzodiazepines, narrow-angle glaucoma, concurrent ketoconazole, or itraconazole Black Box Warnings Concurrent use with opioids
Medication Safety Issues: Alprazolam
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XRALPRAZolamALPRAZolam XRNoZantac, LORazepam, XopenexAvoid
Class: Antiarrhythmic
Dosage Forms. Tablet: 100 mg, 200 mg, 400 mg
Common FDA Label Indication, Dosing, and Titration.
Ventricular arrhythmia, treatment and prophylaxis: 800-1600 mg po daily in divided doses × 1-3 wk, titrate down to 600-800 mg po daily × 1 mo, then to maintenance dose of 400-600 mg po daily given as single dose or divided bid
Off-Label Uses.
Atrial fibrillation, prophylaxis after open heart surgery: 600-1200 mg po daily in divided doses, started post-op and continued until hospital discharge
Supraventricular arrhythmia: 600-1200 mg po daily for 1-2 wk, tapered to 400-600 mg po daily × 1-3 wk then to maintenance dose of 200 mg po daily
MOA. Type III antiarrhythmic that prolongs the effective refractory period of atrial and ventricular tissue by blocking potassium conductance.
Drug Characteristics: Amiodarone
Dose Adjustment Hepatic Should be considered Absorption F = 50%, food enhances rate and extent of absorption
Dose Adjustment Renal Not required Distribution Vd = 66 L/kg; 96% protein bound
Dialyzable Not dialyzable Metabolism Hepatic via CYP2C8 and 3A4/5 to active metabolite; inhibitor of CYP2A6, 2C9, 2D6, 3A4/5 and P-glycoprotein
Pregnancy Category D Elimination Renal with a half-life of 40-55 d
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, severe bradycardia, severe sinus node dysfunction, 2nd or 3rd degree AV block, and cardiogenic shock Black Box Warnings Arrhythmias, hepatotoxicity, proarrhythmic effects, pulmonary toxicity
Medication Safety Issues: Amiodarone
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoNoYesAmantadine, amiloride, Cardura, CordranAvoid as first line for atrial fibrillation unless patient has HF
Class: Tricyclic Antidepressant
Dosage Forms. Tablet: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg
Common FDA Label Indication, Dosing, and Titration.
Depression: Adults, 75 mg po divided into 1-3 daily doses, titrate to max 300 mg/d; Children ≥12 y of age, 10 mg po tid or 20 mg po daily hs
Off-Label Uses.
Migraine prophylaxis: 10-25 mg po daily hs; titrate to max 150 mg/d
Chronic pain: 25-100 mg po daily hs; titrate to max 150 mg/d
Polyneuropathy, postherpetic neuralgia, treatment and prophylaxis: 10-25 mg po daily hs; may titrate to max 200 mg/d
Posttraumatic stress disorder (PTSD): 50 mg po daily; titrate to max 300 mg/d
MOA. Amitriptyline is a tricyclic antidepressant that blocks presynaptic reuptake of serotonin and norepinephrine with subsequent down-regulation of adrenergic receptors.
Drug Characteristics: Amitriptyline
Dose Adjustment Hepatic Start with low initial doses and increase as needed and tolerated Absorption F = 100%, no effect of food on absorption
Dose Adjustment Renal Not required Distribution Vd is highly variable
Dialyzable Not dialyzable Metabolism Extensive hepatic; minor substrate of CYP1A2, 2B6, 2C9, 2C19, and 3A4/5; major substrate of CYP2D6
Pregnancy Category C Elimination Minimal renal with a half-life of 9-27 h
Lactation Weigh risks and benefits Pharmacogenetics Caution in CYP2D6 poor metabolizers, or concurrently with CYP2D6 inhibitors
ContraindicationsHypersensitivity; concurrent MAOI or MAOI use in last 14 d; use during acute recovery period after MIBlack Box WarningsSuicidality; not approved for children <12 y of age
Class: β-Lactam Antibiotic
Dosage Forms. Capsule: 250 mg, 500 mg; Chewable Tablet: 125 mg, 250 mg; Suspension: 125 mg/5 mL, 200 mg/5 mL; 250 mg/5 mL, 400 mg/5 mL; Tablet: 500 mg, 875 mg; Tablet, Extended Release: 775 mg
Common FDA Label Indication, Dosing, and Titration.
Acute otitis media: Adults, 500-875 mg po q12h × 10 d; Children, 80-90 mg/kg/d po in 2-3 divided doses
Lower respiratory tract infection: Adults, 1 g po tid × 10 d; Children, 45 mg/kg/d divided q12h
Pharyngitis, tonsillitis: Adults and Children >12 y, 775 mg po daily × 10 d
Streptococcal pharyngitis: Adults, 1 g po daily × 10 d; Children, 50 mg/kg po once daily for 10 d, max 1 g daily
Ear, nose, and throat infection, infection of skin and/or subcutaneous tissue, infection of genitourinary system: Adults, 500-875 mg po q12h × 10 d; Children, 25-45 mg/kg/d po divided q12h
Helicobacter pylori gastrointestinal tract infection: 1 g po bid with PPI
Off-Label Uses.
Bacterial endocarditis, prophylaxis: Adults, 2 g po 1 h before procedure; Children, 50 mg/kg po 1 h prior to procedure, max 2 g daily
Lyme disease: 500 mg po tid × 21-30 d; Children: 50 mg/kg/d po in 3 divided doses × 21-30 d
MOA. Semisynthetic penicillin derivative that inhibits the biosynthesis of bacterial cell wall mucopeptide. Typically active against Streptococcus, Enterococcus, Staphylococcus, and Enterobacteriaceae.
Drug Characteristics: Amoxicillin
Dose Adjustment Hepatic Not required Absorption F = 85%, no effect of food on absorption
Dose Adjustment Renal Moderate, increase interval to 8-12 h; severe, increase interval to q24h Distribution 17-20% protein bound. Lung, pleural fluid, bile, liver, and inner ear
Dialyzable Yes (hemodialysis only) Metabolism Partially hepatic
Pregnancy Category B Elimination Renal 50-70% with a half-life of 1-2 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings
Class: β-Lactam Antibiotic
Dosage Forms. Tablet: 250 mg amoxicillin/125 mg clavulanate, 500 mg amoxicillin/125 mg clavulanate, 875 mg amoxicillin/125 mg clavulanate; Tablet, Extended Release: 1000 mg amoxicillin/62.5 mg clavulanate; Tablet, Chewable: 200 mg amoxicillin/28.5 mg clavulanate, 400 mg amoxicillin/57 mg clavulanate; Suspension: 125 mg amoxicillin/31.25 mg clavulanate/5 mL, 200 mg amoxicillin/28.5 mg clavulanate/5 mL, 250 mg amoxicillin/62.5 mg clavulanate/5 mL, 400 mg amoxicillin/57 mg clavulanate/5 mL, 600 mg amoxicillin/42.9 mg clavulanate/5 mL
Common FDA Label Indication, Dosing, and Titration.
Acute otitis media: Adults, 500-875 mg po q12h × 10 d; Children, 80-90 mg/kg/d po in 2-3 divided doses
Community-acquired pneumonia: Adults, 2000 mg po bid × 7-10 d
Lower respiratory tract infection: Adults, 1000 mg po tid × 10 d; Children, 45 mg/kg/d po divided q12h
Sinusitis, infection of skin or subcutaneous tissue, infectious disease of genitourinary system: Adults, 500-875 mg po q12h × 10 d; Children, 25-45 mg/kg/d po divided q12h
Off-Label Uses.
Streptococcal pharyngitis: Adults, 875 mg po q12h or 500 mg po q8h; Children, 45 mg/kg/d divided q12h
MOA. Amoxicillin is a semisynthetic penicillin derivative. Typically active against Streptococcus, Enterococcus, Staphylococcus, and Enterobacteriaceae. Amoxicillin is not effective against β-lactamase-producing bacteria. Clavulanate, a β-lactamase inhibitor, has weak antibacterial activity but is a potent inhibitor of plasmid-mediated β-lactamases and protects amoxicillin from degradation by β-lactamases.
Drug Characteristics: Amoxicillin/Clavulanate
Dose Adjustment Hepatic Consider dose adjustment in severe impairment Absorption F = 85%, no effect of food on absorption
Dose Adjustment Renal CrCl 10-30 mL/min, increase interval to q12h; CrCl <10 mL/min, increase interval to q24h; avoid 875 mg tablet and extended-release tablet for those on hemodialysis or CrCl <30 mL/min Distribution 17-20% protein bound; lung, pleural fluid, bile, liver, and inner ear
Dialyzable Yes (peritoneal and hemodialysis) Metabolism Amoxicillin not metabolized, extensive metabolism of clavulanic acid
Pregnancy Category B Elimination Renal 50-70% (amoxicillin) with a half-life of 1-2 h
Lactation Compatible Pharmacogenetics None known
ContraindicationsHypersensitivity to penicillins; extended-release products are contraindicated in patients on dialysis or severe renal dysfunctionBlack Box Warnings
Class: Factor Xa Inhibitor
Dosage Forms. Tablet: 2.5 mg, 5 mg
Common FDA Label Indication, Dosing, and Titration.
Atrial fibrillation, nonvalvular (prophylaxis, to reduce the risk of stroke): 5 mg po bid
Hip or knee replacement surgery (prophylaxis, to reduce the risk of deep vein thrombosis and pulmonary embolism): 2.5 mg po bid × 12 d (knee replacement) or 35 d (hip replacement); start 12-24 h postoperatively
Deep vein thrombosis or pulmonary embolism (treatment and to reduce the future risk): 10 mg po bid × 7 d, then 5 mg po bid
Off-Label Uses.
Heparin-induced thrombocytopenia with thrombosis, hemodynamically stable patients or after initial therapy with parenteral non-heparin anticoagulant: with thrombosis, 10 mg po bid × 7 d, then 5 mg po bid; without thrombosis, 5 mg po bid
MOA. Apixaban is a selective inhibitor of FXa. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.
Drug Characteristics: Apixaban
Dose Adjustment Hepatic Severe, not recommended Absorption F = 50%, no food effect
Dose Adjustment Renal In atrial fibrillation patients, if 2 or more of following characteristics, reduce dose to 2.5 mg bid: age ≥80 y, body weight ≤60 kg, or SCr ≥1.5 mg/dL Distribution Vd = 21 L; 87% protein bound
Dialyzable Use same dose in patients undergoing hemodialysis Metabolism Hepatic, primarily via CYP3A4/5
Pregnancy B Elimination Renal 27% with a half-life of 12 h
Lactation Weigh risks and benefits Pharmacogenetics None known
ContraindicationsHypersensitivity, active bleedingBlack Box WarningsPremature discontinuation increases risk of thrombotic events; increased risk of spinal hematoma with spinal puncture or neuraxial anesthesiav
Class: Antipsychotic
Dosage Forms. Tablet: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg; Tablet, Disintegrating: 10 mg, 15 mg; Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Bipolar disorder, manic or mixed episodes, acute treatment: Adults, 10-15 mg po daily, may titrate to 15-30 mg po daily; Children >10 y, 2 mg po daily, may titrate to 10 mg po daily
Schizophrenia: Adults, 10-15 mg po daily, may titrate to max 30 mg/d; Children >13 y, 2 mg po daily, may titrate to 10 mg po daily
Depression, adjunctive with antidepressant: 2-4 mg po daily, may titrate to 15 mg po daily
Tourette syndrome: Children ≥6 y of age and <50 kg, 2 mg po daily, may titrate to 5-10 mg po daily; Children ≥6 y of age and ≥50 kg, 2 mg po daily, may titrate to 10-20 mg po daily
Irritability with autistic disorder: Children ≥6 y of age, 2 mg po daily × 7 d, then 5 mg po daily, may titrate to 15 mg/d
Off-Label Uses.
None
MOA. Aripiprazole is an atypical antipsychotic agent (quinolinone derivative). It exhibits partial agonist activity at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors and antagonist activity at 5-HT2A receptors.
Drug Characteristics: Aripiprazole
Dose Adjustment Hepatic Not required Absorption F = 87%, no effect of food on absorption
Dose Adjustment Renal Not required Distribution Vd = 4.9 L/kg; >99% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, 80%; major substrate of CYP2D6 and 3A4/5
Pregnancy Category C Elimination Renal 10-20% with a half-life of 75-94 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2D6 poor metabolizers should receive 50% lower dose
Contraindications Hypersensitivity Black Box Warnings Dementia, suicidality
Medication Safety Issues: Aripiprazole
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoARIPiprazoleDisintegrating tabletNoAmbien, lansoprazole, omeprazole, pantoprazole, rabeprazoleStroke risk; avoid except in schizophrenia or bipolar disorder
Class: Antiretroviral Agent, Protease Inhibitor
Dosage Forms. Capsule: 150 mg, 200 mg, 300 mg; Oral Powder: 50 mg
Common FDA Label Indication, Dosing, and Titration.
Treatment of HIV-1 infection, antiretroviral-naïve: Adults and Children ≥13 y of age and ≥40 kg, 300 mg po daily with ritonavir 100 mg or cobicistat 150 mg; Adults unable to tolerate ritonavir, atazanavir 400 mg daily (ritonavir unboosted regimen not recommended in Children)
Treatment of HIV-1 infection, patients with prior virologic failure: Adults and Children ≥13 y of age and ≥40 kg, 300 mg po daily with ritonavir 100 mg or cobicistat (monotherapy with atazanavir not recommended); Children <13 y of age, weight based and used in combination with ritonavir
Treatment of HIV-1 infection in pregnant patients, antiretroviral-naïve or experienced: 300 mg po daily with ritonavir 100 mg po daily
Off-Label Uses.
None
MOA. Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles.
Drug Characteristics: Atazanavir
Dose Adjustment Hepatic Use with caution if moderate hepatic impairment Absorption F approaches 100%, food increases absorption by 50%
Dose Adjustment Renal Not required Distribution CSF and semen
Dialyzable Yes Metabolism Hepatic; substrate of CYP3A4/5, strong inhibitor of CYP3A4/5 and UGT1A1
Pregnancy Category B Elimination Hepatic 80% with half-life of 7 h
Lactation Weigh risks and benefits Pharmacogenetics Resistance is associated with HIV mutations
Contraindications Hypersensitivity or concurrent therapy with alfuzosin, cisapride, ergot derivatives indinavir, irinotecan, lovastatin, midazolam (oral), pimozide, rifampin, sildenafil, simvastatin, or triazolam Black Box Warnings None
Medication Safety Issues: Atazanavir
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No Do not open capsule Yes No No
Class: β-Adrenergic Blocker, Cardioselective
Dosage Forms. Tablet: 25 mg, 50 mg, 100 mg
Common FDA Label Indication, Dosing, and Titration.
Angina pectoris, chronic: 50 mg po daily; titrate to 100-200 mg po daily
Hypertension: Adults, 50 mg po daily, titrate to 100 mg po daily; Children, 0.5-1 mg/kg/d po in 1-2 divided doses, titrate to 2 mg/kg/d po in 1-2 divided doses (max 100 mg/d)
Off-Label Uses.
Cardiac dysrhythmia: Adults, 50-100 mg po daily; Children, 0.3-1.4 mg/kg po daily, titrate to 2 mg/kg po daily
Migraine prophylaxis: 50-100 mg po daily
MOA. Atenolol is a cardioselective β-adrenergic that decreases AV nodal conduction in supraventricular tachycardias and blockade of catecholamine-induced dysrhythmias.
Drug Characteristics: Atenolol
Dose Adjustment Hepatic Not required Absorption F = 50%, food decreases AUC by 20%
Dose Adjustment Renal CrCl 15-35 mL/min, max dose 50 mg po daily; CrCl <15 mL/min, max dose 25 mg po daily Distribution Vd = 50-75 L; <5% protein bound
Dialyzable Yes, give 25-50 mg after each dialysis procedure Metabolism Not metabolized
Pregnancy Category D Elimination Renal 40-50%, fecal 50% (unchanged) with a half-life of 6-7 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to atenolol, severe sinus bradycardia, 2nd- or 3rd-degree AV block, overt heart failure or cardiogenic shock Black Box Warnings Avoid abrupt withdrawal
Medication Safety Issues: Atenolol
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Albuterol No
Class: Norepinephrine Reuptake Inhibitor, CNS Stimulant
Dosage Forms. Capsule: 10 mg, 18 mg, 25 mg, 40 mg, 60 mg, 80 mg, 100 mg
Common FDA Label Indication, Dosing, and Titration.
ADHD: Children >6 y of age and weighing ≤70 kg, 0.5 mg/kg/d po, may titrate to lower of 1.4 mg/kg/d or 100 mg/d; Children >6 y of age and weighing >70 kg, 40 mg/d po, may titrate to 100 mg/d; Adults, 40 mg po daily, may titrate to 100 mg/d
Off-Label Uses.
None
MOA.Atomoxetine is a selective norepinephrine reuptake inhibitor that produces therapeutic effects in patients with ADHD. The exact mechanism of how selective inhibition of presynaptic norepinephrine exerts effects in ADHD has not been determined.
Drug Characteristics: Atomoxetine
Dose Adjustment Hepatic Child-Pugh Class B: initial and target doses should be reduced to 50% of normal dose; Child-Pugh Class C: initial and target doses should be reduced to 25% of normal dose Absorption F = 63% (normal metabolizers); 94% (poor metabolizers); food does not affect absorption
Dose Adjustment Renal Not required Distribution Vd = 0.85 L/kg; 98% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic to 1 active metabolite; major substrate of CYP2D6
Pregnancy Category C Elimination Renal 80%, fecal 17% with a half-life of 5.2-21.6 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2D6 poor metabolizers, decrease dose as with drug interaction with CYP2D6 inhibitor
Contraindications Hypersensitivity to atomoxetine; concomitant use of MAOIs or use within 2 wk; narrow-angle glaucoma, pheochromocytoma Black Box Warnings Suicidality in children and adolescents
Class: HMG-CoA Reductase Inhibitor
Dosage Forms. Tablet: 10 mg, 20 mg, 40 mg, 80 mg
Common FDA Label Indication, Dosing, and Titration.
Hyperlipidemia: 10-20 mg po daily, may increase to 80 mg po daily
Primary and secondary prevention of atherosclerotic cardiovascular disease: 10-20 mg po daily, may increase to 80 mg po daily for those patients requiring high-intensity therapy (eg, LDL >190 mg/dL or high ASCVD risk)
Secondary prevention of cardiovascular events in patients with or at high risk for CAD: 80 mg daily, may reduce dose to 40 mg po daily if high dose not tolerated
Familial hypercholesterolemia (homozygous): Children (boys and postmenarchal girls 10-17 y of age), 10 mg po daily, may titrate to 40 mg po daily; Adults, 10-80 mg po daily
Off-Label Uses.
None
MOA.HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol also can decrease because of decreased production of VLDL-cholesterol or increased VLDL; removal by LDL receptors.
Drug Characteristics: Atorvastatin
Dose Adjustment Hepatic Avoid use in patients with active liver disease or unexplained persistent elevated LFTs Absorption F = 14%, food slows rate of absorption
Dose Adjustment Renal Not required Distribution Vd = 381 L; 98% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; major substrate of CYP3A4/5 and P-glycoprotein; inhibits P-glycoprotein
Pregnancy Category X Elimination Biliary and renal with a half-life of 7-14 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to atorvastatin, pregnancy or lactation Black Box Warnings None
Medication Safety Issues: Atorvastatin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No AtorvaSTATin No No AtoMOXetine, lovastatin, nystatin, pravastatin, rosuvastatin, simvastatin No
Class: Macrolide Antibiotic
Dosage Forms. Oral Tablet: 250 mg, 500 mg, 600 mg; Microspheres for Suspension: 2 g/bottle; Powder for Oral Suspension: 100 mg/5 mL, 200 mg/5 mL, 1 g packet
Common FDA Label Indication, Dosing, and Titration.
Acute infective exacerbation of COPD, skin or tissue infection: 500 mg po daily × 3 d or 500 mg po × 1 dose, then 250 mg po daily × 2-5 d
Bacterial sinusitis: Adults, 500 mg po daily × 3 d; Children, 10 mg/kg po daily × 3 d, or 2 g po × 1 dose
Chancroid, nongonococcal cervicitis, nongonococcal urethritis: 1 g po × 1 dose
Community-acquired pneumonia: 500 mg po daily × 3 d or 500 mg po × 1 dose, then 250 mg po daily × 2-5 d; Infants ≥6 mo of age, tablets and immediate-release suspension, 10 mg/kg po on day 1, then 5 mg/kg po daily × 2-5 d or extended-release suspension, <34 kg, 60 mg/kg po × 1 dose; >34 kg, 2 g po × 1 dose
Gonorrhea, urethritis, or cervicitis: 2 g po × 1 dose
Streptococcal pharyngitis: 500 mg po × 1 dose, then 250 mg po daily × 2-5 d; Children, 12 mg/kg po daily × 5 d
Off-Label Uses.
Traveler's diarrhea: Adults, 1000 mg po × 1 dose, or 500 mg po daily × 3 d; Children, 10 mg/kg po daily × 3 d
Bacterial endocarditis, prophylaxis: Adults, 500 mg po 30-60 min prior to procedure; Children, 15 mg/kg po 30-60 min prior to procedure
MOA. Azithromycin is a macrolide antibiotic that is slightly less active than erythromycin against gram-positive bacteria but substantially more active against Moraxella (Branhamella)catarrhalis, Haemophilus sp., Legionella sp., Neisseria sp., Bordetella sp., Mycoplasma sp., and Chlamydia trachomatis. Azithromycin binds to the 50S ribosomal subunit, thus interfering with microbial protein synthesis.
Drug Characteristics: Azithromycin
Dose Adjustment Hepatic Not required Absorption F = 38%, no effect of food on absorption
Dose Adjustment Renal Not required Distribution Blister fluid, bronchial secretions, cervix, ear fluid, ovaries, sputum, soft tissue
Dialyzable Not dialyzable Metabolism Hepatic
Pregnancy Category B Elimination Renal 6% with a half-life of 68 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to azithromycin, erythromycin, or any macrolide or ketolide antibiotic Black Box Warnings None
Medication Safety Issues: Azithromycin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Azathioprine, erythromycin, Fosamax No
Class: Centrally Acting Skeletal Muscle Relaxant
Dosage Forms. Oral Tablet: 5 mg, 10 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Spasticity: 5 mg po tid; may increase dose in 5-15 mg/d increments; max dose in Adults and Children ≥12 y of age, 80 mg/d po; max dose in Children 8-12 y of age, 60 mg/d; max dose in Children <8 y of age, 40 mg/d po
Off-Label Uses.
Intractable hiccoughs: 5 mg po bid, increasing to 15-45 mg/d in 3 divided doses; or 10-20 mg 2-3 times daily
MOA. Baclofen inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. Baclofen is an analogue of γ-aminobutyric acid (GABA), but there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects.
Drug Characteristics: Baclofen
Dose Adjustment Hepatic Not required Absorption F = 100%, no effect of food on absorption
Dose Adjustment Renal In patients with renal dysfunction, monitor carefully for toxicity and reduce dose as necessary Distribution Vd = 59.1 L; 30% protein bound
Dialyzable Yes Metabolism Limited hepatic metabolism
Pregnancy Category C Elimination Renal 60-80% with a half-life of 3-7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings Avoid abrupt discontinuation of oral or intrathecal product
Medication Safety Issues: Baclofen
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No Yes, intrathecal Bactroban
Class: Cardioselective β-Adrenergic Blocker
Dosage Forms. Oral Tablet: 5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertension: 2.5-5 mg po daily, may titrate to max of 20 mg po daily
Off-Label Uses.
Angina: 5-20 mg po daily
Atrial fibrillation: 2.5-10 mg po daily
Heart failure: 1.25-10 mg po daily
MOA. Bisoprolol is a cardioselective β-adrenergic blocker that decreases AV nodal conduction in supraventricular tachycardia and blockade of catecholamine-induced dysrhythmias. The antihypertensive mechanism is unknown, but contributing factors are renin blockade and decreases in myocardial contractility and cardiac output.
Drug Characteristics: Bisoprolol
Dose Adjustment Hepatic Initiate with 2.5 mg po daily, may titrate to max of 10 mg po daily Absorption F = 80%; food has no effect on absorption
Dose Adjustment Renal Initiate with 2.5 mg po daily, may titrate to max of 10 mg po daily Distribution Protein binding 30%; distribution limited to extracellular fluid space and kidneys
Dialyzable Not dialyzable Metabolism Extensive hepatic; major substrate of CYP3A4/5
Pregnancy Category C Elimination Renal 50% with a half-life of 9-12 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to bisoprolol, severe sinus bradycardia, 2nd- or 3rd-degree AV block, overt heart failure, cardiogenic shock Black Box Warnings None
Medication Safety Issues: Bisoprolol
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoNoNoDiaBeta, ZetiaNo
Class: Inhaled Corticosteroid
Dosage Forms. Inhalation Suspension: 0.25 mg/2 mL, 0.5 mg/2 mL, 1 mg/2 mL; Metered-Dose Inhaler (MDI): 90 mcg/actuation, 180 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Asthma: Children 1-8 y of age with no previous inhaled corticosteroid therapy, 0.5 mg inhaled via nebulization in 1 or 2 divided doses; Children 1-8 y of age previously treated with corticosteroids, 0.5 mg inhaled via nebulization daily or bid, may titrate to 1 mg/d; Children >8 y of age and Adults, 180-360 mcg bid via MDI, max 720 mcg bid via MDI
Off-Label Uses.
COPD, stable: 100-400 mcg daily via MDI in combination with long-acting bronchodilator
MOA. Budesonide is an anti-inflammatory with potent glucocorticoid and weak mineralocorticoid activity. It exhibits a broad range of active inhibition against multiple cell types and mediators involving allergic and nonallergic/irritant-mediated inflammation.
Drug Characteristics: Budesonide
Dose Adjustment Hepatic Not required Absorption F = 6%
Dose Adjustment Renal Not required Distribution Vd = 3 L/kg; protein binding 85-90%
Dialyzable Not dialyzable Metabolism Extensive hepatic; major substrate of CYP3A4/5
Pregnancy Category B Elimination Renal 60%, fecal 15-29% with a half-life of 2-3 h
Lactation Weigh risks and benefits Pharmacogenetics None known
ContraindicationsHypersensitivity to budesonide; hypersensitivity to milk proteins (Flexhaler); primary treatment of status asthmaticus or other acute episodes of asthmaBlack Box Warnings
Class: Inhaled Corticosteroid/Bronchodilator Combination
Dosage Forms. Metered-Dose Inhaler (MDI): (Budesonide/Formoterol) 80 mcg/4.5 mcg/inhalation, 160 mcg/4.5 mcg/inhalation
Common FDA Label Indication, Dosing, and Titration.
Asthma: Children ≥12 y of age and Adults, 80 mcg/4.5 mcg, 2 inhalations bid, may titrate to 160 mcg/4.5 mcg, 2 inhalations bid
COPD: 160 mcg/4.5 mcg 2 inhalations bid
Off-Label Uses.
Asthma: Children 5-11 y of age, 80 mcg/4.5 mcg, 2 inhalations bid
MOA. Budesonide is an anti-inflammatory with potent glucocorticoid and weak mineralocorticoid activity. It exhibits a broad range of active inhibition against multiple cell types and mediators involving allergic and nonallergic/irritant-mediated inflammation. Formoterol is a long-acting selective β2-adrenergic agonist that produces bronchodilation.
Drug Characteristics: Budesonide/Formoterol
Dose Adjustment Hepatic Not required Absorption F = 39% for budesonide; unknown for formoterol inhalation
Dose Adjustment Renal Not required Distribution Protein binding 85-90% (budesonide); 31-64% for formoterol
Dialyzable Not dialyzable Metabolism Extensive hepatic; major substrate of CYP3A4/5 (budesonide)
Pregnancy Category C Elimination Renal 60% with a half-life of 2-3 h (budesonide); renal 1-28% with a half-life of 10 h (formoterol)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to budesonide or formoterol; primary treatment of status asthmaticus or acute episodes of asthma or COPD Black Box Warnings Asthma deaths; pediatrics, increased risk of hospitalization
Medication Safety Issues: Budesonide/Formoterol
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoNoNoNoNo
Class: Opioid Partial Agonist and Antagonist Combination. C-III
Dosage Forms. Sublingual Film: (Buprenorphine/Naloxone) 2 mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, 12 mg/3 mg; Sublingual Tablet: (Buprenorphine/Naloxone) 0.7 mg/0.18 mg, 1.4 mg/0.36 mg, 2 mg/0.5 mg, 2.9 mg/0.71 mg, 5.7 mg/1.4 mg, 8.6 mg/2.1 mg, 11.4 mg/2.9 mg; Buccal Film: (Buprenorphine/Naloxone) 2.1 mg/0.3 mg, 4.2 mg/0.7 mg, 6.3 mg/1 mg
Common FDA Label Indication, Dosing, and Titration.
Opioid dependence: Adults and Children >16 y of age, 12-16 mg (buprenorphine component) once daily sublingually, titrate to response; typical dose range from 4 to 24 mg/d
Off-Label Uses.
None
MOA. Buprenorphine is a µ-opioid receptor partial agonist and a -opioid receptor antagonist. Naloxone is a µ-opioid receptor antagonist that causes opioid withdrawal when injected parenterally and is included in the formulation to reduce the risk of abuse.
Drug Characteristics: Buprenorphine/Naloxone
Dose Adjustment Hepatic Use with caution Absorption F = 15% (buprenorphine); F = 3% (naloxone)
Dose Adjustment Renal Not required Distribution Vd = 97-187 L (buprenorphine)
Dialyzable Unknown Metabolism Buprenorphine, hepatic, major substrate of CYP3A4/5; naloxone, hepatic via glucuronidation
Pregnancy Category C Elimination Renal 30% with half-life of 33 h (buprenorphine), 6 h (naloxone)
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Buprenorphine/Naloxone
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoNoYesNoNo
Class: Monocyclic Antidepressant
Dosage Forms. Oral Tablet (Immediate Release): 75 mg, 100 mg; Oral Tablet (Extended Release 12 h): 100 mg, 150 mg, 200 mg; Oral Tablet (Extended Release 24 h): 150 mg, 174 mg, 300 mg, 348 mg, 450 mg, 522 mg
Common FDA Label Indication, Dosing, and Titration.
Depression: Immediate release, 100 mg po bid × 3 d, increase to 100 mg po tid (max 450 mg/d); Extended release 12 h, 150 mg po daily in the morning × 3 d, then increase to 150 mg po bid (max 200 mg bid); Extended-release hydrochloride 24 h, 150 mg po daily × 3 d, then increase to 300 mg po daily (max 450 mg/d); Extended-release hydrobromide 24 h, 174 mg po daily × 3 d, then increase to 348 mg po daily (max 522 mg/d)
Seasonal affective disorder (SAD): Extended-release hydrochloride 24 h, 150 mg po daily, may titrate to 300 mg po daily; Extended-release hydrobromide 24 h, 174 mg po daily, may titrate to 348 mg po daily
Smoking cessation assistance: Extended release 12 h, 150 mg po daily in the morning × 3 d, then 150 mg po bid (max 300 mg/d) for 7-12 wk; begin treatment 1 wk prior to smoking quit date
Off-Label Uses.
None
MOA. Bupropion is a monocyclic antidepressant, unique as a mild dopamine and norepinephrine uptake inhibitor with no direct effect on serotonin receptors or MAO.
Drug Characteristics: Bupropion
Dose Adjustment Hepatic Mild to moderate: reduce frequency and/or dose. Severe liver disease: max dose 150 mg qod Absorption Food has minimal effect on absorption
Dose Adjustment Renal Reduce frequency and/or dose Distribution Vd = 19-21 L/kg; 84% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, 10-15%; major substrate of CYP2B6; inhibitor of CYP2D6
Pregnancy Category C Elimination Renal 87%, fecal 10% with a half-life of 14-37 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Seizure disorder; history of anorexia/bulimia; use of MAOI within 14 d; patients undergoing abrupt discontinuation of ethanol, benzodiazepines, barbiturates, or antiepileptics Black Box WarningsSuicidality; neuropsychiatric reactions
Class: Anticonvulsant
Dosage Forms. Oral Tablet: 200 mg; Oral Tablet, Chewable: 100 mg; Oral Tablet, Extended Release: 100 mg, 200 mg, 400 mg; Oral Suspension: 100 mg/5 mL; Oral Capsule, Extended Release: 100 mg, 200 mg, 300 mg
Common FDA Label Indication, Dosing, and Titration.
Epilepsy, partial, generalized, and mixed types: Adults, 200 mg po bid, may titrate to 1200 mg po daily; Children <6 y of age, 10-20 mg/kg/d po in 2-4 divided doses, may titrate to 250-350 mg/d po (or 35 mg/kg/d); Children 6-12 y of age, 100 mg po bid, may titrate to 800 mg po daily
Trigeminal neuralgia: 100 mg po q12h, may titrate to 1200 mg po daily for pain control
Off-Label Uses.
Neuropathic pain: 50-100 mg po bid in combination with opioids, may titrate to 1200 mg/d po
Bipolar disease, acute manic and mixed episodes: 200 mg po bid, may titrate to 1600 mg/d po
MOA. Carbamazepine acts presynaptically to block firing of action potentials, which decreases the release of excitatory neurotransmitters, and postsynaptically by blocking high-frequency repetitive discharge initiated at cell bodies.
Drug Characteristics: Carbamazepine
Dose Adjustment Hepatic Avoid Absorption F = 89%; no effect of food on absorption
Dose Adjustment Renal Not required Distribution Vd = 0.59-2 L/kg; 75-90% protein bound
Dialyzable Yes Metabolism Hepatic; major substrate of CYP3A4/5; strong inducer of CYP1A2, 2B6, 2C19, 2C8, 2C9, 3A4/5 and P-glycoprotein
Pregnancy Category D Elimination Renal 72% with an initial half-life of 25-65 h, then 12-17 h after 3-5 wk of treatment due to autoinduction
Lactation Compatible Pharmacogenetics Use alternative anticonvulsant in HLA-A31:01 positive or HLA-B15:02 positive patients, increased risk of Stevens-Johnson syndrome
Contraindications Hypersensitivity to carbamazepine, history of bone marrow depression, MAOIs, nefazodone Black Box Warnings Agranulocytosis; aplastic anemia; dermatological reactions (especially in Asians); screen for HLA-B*15:02
Medication Safety Issues: Carbamazepine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XR CarBAMazepine, TEGretol Do not crush or chew ER tablets or capsules No OXcarbazepine, Toradol, TRENtal Avoid in certain circumstances
Class: Antiparkinsonian
Dosage Forms. Oral Tablet, Immediate Release: (Carbidopa/Levodopa) 10 mg/100 mg, 25 mg/100 mg, 25 mg/250 mg; Oral Tablet, Extended Release: (Carbidopa/Levodopa) 25 mg/100 mg, 50 mg/200 mg; Oral Capsule, Extended Release: (Carbidopa/Levodopa) 23.75 mg/95 mg, 36.25 mg/145 mg, 48.75 mg/195 mg, 61.25 mg/245 mg; Orally Disintegrating Tablet: (Carbidopa/Levodopa) 10 mg/100 mg, 25 mg/100 mg, 25 mg/250 mg; Oral Suspension: (Carbidopa/Levodopa) 4.63 mg/20 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Parkinson disease: Immediate release, 25 mg/100 mg po tid, increasing dose to therapeutic response; extended release, 50 mg/200 mg po bid, separate doses by at least 6 h; extended-release capsules, 23.75 mg/95 mg po tid × 3 d, then may increase to 36.25 mg/145 mg po tid; patients generally treated with 400-1600 mg of levodopa per d; max 200 mg of carbidopa and 2000 mg of levodopa
Off-Label Uses.
Restless legs syndrome: 25 mg/100 mg po qhs, may repeat dose if awakening within 2 h
MOA. When levodopa is administered orally, it is rapidly decarboxylated to dopamine in extracerebral tissues so that only a small portion of a given dose is transported unchanged to the CNS. For this reason, when given alone, large doses of levodopa are required for adequate therapeutic effect. However, these doses often result in nausea and other adverse reactions. Carbidopa inhibits decarboxylation of circulating levodopa, preventing nausea and allowing more levodopa to reach the CNS. Carbidopa does not cross the blood-brain barrier and does not affect the metabolism of levodopa within the CNS.
Drug Characteristics: Carbidopa/Levodopa
Dose Adjustment Hepatic Not required Absorption Carbidopa F = 60%; levodopa F = 70-75%
Dose Adjustment Renal Not required Distribution CSF concentrations of levodopa are 10-20% of plasma levels
Dialyzable Not dialyzable Metabolism Levodopa undergoes extensive decarboxylation to dopamine in the gut wall, liver, and kidney; when given with carbidopa, peripheral decarboxylation of levodopa is blocked, increasing availability of levodopa for brain transport
Pregnancy Category C Elimination Carbidopa, renal 30% with a half-life of 1-2 h; levodopa, renal 70-80% with a half-life of 45-90 min
Lactation Avoid; may inhibit lactation Pharmacogenetics None known
ContraindicationsHypersensitivity to carbidopa or levodopa, narrow-angle glaucoma, non-selective MAOIBlack Box Warnings
Class: α/β-Adrenergic Blocker
Dosage Forms. Oral Tablet: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg; Oral Capsule, Extended Release: 10 mg, 20 mg, 40 mg, 80 mg
Common FDA Label Indication, Dosing, and Titration.
Heart failure: Tablet, 3.125 mg po bid, may titrate to 25 mg po bid for patients weighing <85 kg, 50 mg po bid for patients weighing >85 kg;
Hypertension: Tablet, 6.25 mg po bid; max 25 mg po bid; Extended-release capsule, 20 mg po daily in the morning, max 80 mg po daily
Impaired left ventricular function post-myocardial infarction: Tablet, 3.125-6.25 mg po bid, may titrate to 25 mg po bid; extended-release capsule, 10-20 mg po daily in the morning, max 80 mg po daily
Off-Label Uses.
Angina pectoris: 25-50 mg po bid
Cardiac dysrhythmia: 6.25 mg po bid, may titrate to 50 mg po bid
Post-acute coronary syndrome: 3.215 mg po bid, may titrate to 25 mg po bid
MOA. Carvedilol is a selective α1- and nonselective β-adrenergic blocker that decreases AV nodal conduction in supraventricular tachycardias and blockade of catecholamine-induced dysrhythmia.
Drug Characteristics: Carvedilol
Dose Adjustment Hepatic Avoid use in patients with hepatic impairment; contraindicated in severe liver dysfunction Absorption F = 25-35%; food significantly increases AUC and Cmax for extended-release product
Dose Adjustment Renal Not required Distribution Vd = 115 L; >95% protein bound
Dialyzable Not dialyzable Metabolism Hepatic 98%; major substrate of CYP2D6, P-glycoprotein; inhibitor of P-glycoprotein
Pregnancy Category C Elimination Renal 16%, fecal 60% with a half-life of 6-10 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2D6 poor metabolizers with higher plasma levels, consider lower initial dose
Contraindications Hypersensitivity, bronchial asthma, severe sinus bradycardia, 2nd- or 3rd-degree AV block, sick sinus syndrome, overt heart failure, cardiogenic shock, severe hepatic impairment Black Box Warnings
Class: Third-Generation Cephalosporin

Dosage Forms. Powder for Oral Suspension: 125 mg/5 mL, 250 mg/5 mL; Oral Capsule: 300 mg
Common FDA Label Indication, Dosing, and Titration.
Acute otitis media, pharyngitis, tonsillitis: Children 6 mo through 12 y, 7 mg/kg po bid × 5-10 d or 14 mg/kg po daily × 10 d; max 600 mg/d; Adults, 300 mg po bid × 5-10 d
Bronchitis, acute, secondary bacterial infection: Adults and Children >12 y of age, 300 mg po bid × 5-10 d
Community-acquired pneumonia, uncomplicated skin, and/or subcutaneous tissue infection: 300 mg po bid × 10 d
Off-Label Uses.
Acute uncomplicated cystitis or acute simple cystitis: 300 mg po BID × 5-7 d
Urinary tract infection, including pyelonephritis: 300 mg po BID × 10-14 d
MOA. Cefdinir is a 3rd-generation cephalosporin with activity against a number of gram-positive and gram-negative bacteria including β-lactamase-producing strains.
Drug Characteristics: Cefdinir
Dose Adjustment Hepatic Not required Absorption F = 25%, food decreases absorption by 30%
Dose Adjustment Renal CrCl <30 mL/min, decrease interval to daily Distribution Lung, maxillary sinus, middle ear fluid, skin, sputum
Dialyzable Administer after hemodialysis and decrease interval to qod Metabolism Not metabolized
Pregnancy Category B Elimination Renal 18% with a half-life of 2 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to cephalosporin Black Box Warnings None
Medication Safety Issues: Cefdinir
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No No No
Class: Second-Generation Cephalosporin
Dosage Forms. Oral Tablet: 125 mg, 250 mg, 500 mg
Common FDA Label Indication, Dosing, and Titration.
Acute infective exacerbation of COPD, uncomplicated skin and/or subcutaneous tissue infection, acute bacterial maxillary sinusitis, uncomplicated urinary tract infection: Adults, 250-500 mg po bid × 10 d
Acute otitis media: Children who are able to swallow tablets, 250 mg po bid × 10 d
Bronchitis, acute, secondary bacterial infection: Adults and Children >12 y of age, 250-500 mg po bid × 5-10 d
Gonorrhea, uncomplicated: 1 g po × 1 dose
Lyme disease: 500 mg po bid × 14-21 d
Pharyngitis, tonsillitis: Adults, 250 mg po bid × 10 d
Off-Label Uses.
None
MOA. Cefuroxime is a 2nd-generation cephalosporin whose activity is better than cefazolin but less than cefotaxime, against Haemophilus influenzae, including β-lactamase-producing strains. The activity of cefuroxime against Staphylococcus aureus is slightly less than that of cefazolin. Its activity against anaerobes is poor, similar to the 1st-generation cephalosporins.
Drug Characteristics: Cefuroxime
Dose Adjustment Hepatic Not required Absorption F = 37%, food increases absorption to 52%, suspension must be taken with food; tablets can be taken without regard to food
Dose Adjustment Renal CrCl = 10-30 mL/min, administer full dose every 24 h; CrCl ≤10 mL/min, administer full dose every 48 h Distribution Aqueous humor, bronchial secretions, ear fluid, placenta, sinus
Dialyzable Dialyzable by both hemodialysis and peritoneal dialysis Metabolism Cefuroxime is rapidly hydrolyzed by plasma and GI esterases
Pregnancy Category B Elimination Renal 50% with a half-life of 2 h
Lactation Usually compatible Pharmacogenetics None known
ContraindicationsHypersensitivity to cephalosporinsBlack Box WarningsNone
Class: Cyclooxygenase-2 Inhibitor
Dosage Forms. Oral Capsule: 50 mg, 100 mg, 200 mg, 400 mg
Common FDA Label Indication, Dosing, and Titration.
Osteoarthritis: 100 mg po bid or 200 mg po daily
Rheumatoid arthritis: Adults, 100-200 mg po bid; Children >2 y of age, 10-25 kg, 50 mg po bid, >25 kg, 100 mg po bid
Ankylosing spondylitis: 100 mg po bid or 200 mg po daily; may increase to 400 mg po daily if not improved within 6 wk
Acute pain, primary dysmenorrhea: 200 mg po bid prn
Off-Label Uses.
Acute gout: 200 mg po bid × 5-7 d
MOA. Inhibition of the COX-2 enzyme isoform is thought to be responsible for the anti-inflammatory effects of NSAIDs.
Drug Characteristics: Celecoxib
Dose Adjustment Hepatic Moderate: reduce dose by 50%; severe: avoid use Absorption Well absorbed, food enhances absorption
Dose Adjustment Renal CrCl <30 mL/min: avoid use Distribution Vd = 400 L; 97% protein bound
Dialyzable Unknown Metabolism Hepatic 97%; major substrate of CYP2C9; moderate inhibitor of CYP2C8 and 2D6
Pregnancy Category C prior to 30 wk gestation; D from 30 wk gestation Elimination Renal 27% with a half-life of 11 h
Lactation Weigh risks and benefits Pharmacogenetics Consider dose reduction of 50% in CYP2C9 poor metabolizers
Contraindications Asthma, urticaria, or allergic-type reaction following aspirin or other NSAID administration; CABG surgery, treatment of perioperative pain, hypersensitivity to sulfonamides Black Box Warnings GI toxicity, cardiotoxicity, CABG
Medication Safety Issues: Celecoxib
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No CeleBREX No No CeleXA, Cerebyx, Cervarix, Clarinex Avoid in certain circumsta
Class: First-Generation Cephalosporin
Dosage Forms. Powder for Oral Suspension: 125 mg/5 mL, 250 mg/5 mL; Oral Tablet: 250 mg, 500 mg; Oral Capsule: 250 mg, 500 mg, 750 mg
Common FDA Label Indication, Dosing, and Titration.
Infection of skin and/or subcutaneous tissue: Adults, 500 mg po q12h; Children, 25-50 mg/kg/d po divided q6h to q12h
Osteomyelitis: Adults, 250 mg-1 g po q6h; Children, 25-100 mg/kg/d po divided q6h, max 4 g/d
Otitis media, respiratory tract infection, urinary tract infection: Adults, 250 mg-1 g po q6h; Children, 25-100 mg/kg/d po divided q6h, max 4 g/d
Streptococcal pharyngitis: Adults, 500 mg po q12h × 10 d; Children, 25-50 mg/kg/d po divided q6h × 10 d, max 4 g/d
Off-Label Uses.
Bacterial endocarditis; prophylaxis for high-risk patients; dental, respiratory, or infected skin/skin structure or musculoskeletal tissue procedures: Adults, 2 g po 30-60 min prior to procedure; Children, 50 mg/kg 30-60 min prior to procedure
MOA. Cephalexin is a 1st-generation cephalosporin that inhibits bacterial wall synthesis of actively dividing cells by binding to ≥1 penicillin-binding proteins (PBPs). Most gram-positive bacteria, including non-penicillinase and penicillinase-producing staphylococci, and streptococci. Activity against gram-negative bacteria is less than that observed with the 2nd-and 3rd-generation cephalosporins and is primarily restricted to Escherichia coli, Klebsiella, and Proteus mirabilis.
Drug Characteristics: Cephalexin
Dose Adjustment Hepatic Not required Absorption F = 90%, food has little effect on absorption
Dose Adjustment Renal CrCl <50 mL/min, max dose 500 mg q12h Distribution Widely into body tissues and fluids
Dialyzable Dialyzable by both hemodialysis and peritoneal dialysis Metabolism Not metabolized
Pregnancy Category B Elimination Renal 80-100% with a half-life of 1 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to cephalosporins Black Box Warnings None
Class: Antihistamine
Dosage Forms. Oral Tablet: 5 mg, 10 mg; Oral Tablet, Chewable: 5 mg, 10 mg; Oral Tablet, Disintegrating: 10 mg; Oral Capsule: 10 mg; Oral Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Perennial or seasonal allergic rhinitis: Children 6-23 mo of age, 2.5 mg po daily; Children 2-5 y of age, 2.5-5 mg po daily; Children ≥6 y of age and Adults, 5-10 mg po daily
Urticaria, chronic: Children 6-23 mo of age, 2.5 mg po daily; Children 2-5 y of age, 2.5-5 mg po daily; Children ≥6 y of age and Adults, 5-10 mg po daily
Off-Label Uses.
Atopic dermatitis: Children 6-23 mo of age, 2.5 mg po daily; Children 2-5 y of age, 2.5-5 mg po daily; Children ≥6 y of age and Adults, 5-10 mg po daily
MOA. Cetirizine is a low-sedating, long-acting H1-receptor antagonist that is a metabolite of hydroxyzine. Cetirizine competitively inhibits the interaction of histamine with H1 receptors, thereby preventing the allergic response.
Drug Characteristics: Cetirizine
Dose Adjustment Hepatic Chronic liver failure, 5 mg po daily Absorption F = 70%, limited effect of food on absorption
Dose Adjustment Renal CrCl <50 mL/min, max dose 5 mg po daily Distribution Vd = 0.5-0.8 L/kg with 90% protein binding
Dialyzable Yes Metabolism Limited hepatic; substrate of P-glycoprotein
Pregnancy Category B Elimination Renal 70% with a half-life of 8.3 h
Lactation Weigh risks and benefits Pharmacogenetics None known
ContraindicationsHypersensitivity to cetirizine or hydroxyzineBlack Box Warnings None
Class: Antibacterial Cleansing Agent
Dosage Forms. Liquid Oral Rinse: 0.12%; Topical Solution: 2%, 4%
Common FDA Label Indication, Dosing, and Titration.
Gingivitis: 15 mL oral rinse (undiluted, 0.12%), swish 30 s and spit bid (morning and evening) after tooth brushing
Skin or wound cleansing: Rinse area to be cleansed, apply minimum amount of solution necessary to cover skin or wound area, and wash gently; then rinse
Off-Label Uses.
Burn, prevention of nosocomial infectious disease: Rinse area to be cleansed, apply minimum amount of 4% solution necessary to cover skin or wound area, and wash gently; then rinse
Oropharyngeal decontamination, to reduce risk of ventilator-associated pneumonia in critically ill patients: 15 mL oral rinse (undiluted, 0.12%), swab oral area q8h
MOA. Chlorhexidine, a polybiguanide, is an antiseptic and antimicrobial drug with bactericidal activity. The bactericidal effect of chlorhexidine is a result of the binding of this cationic molecule to negatively charged bacterial cell walls and extramicrobial complexes. Chlorhexidine has activity against gram-positive and gram-negative organisms, facultative anaerobes, aerobes, and yeast; it is both bacteriostatic and bactericidal, depending on its concentration.
Drug Characteristics: Chlorhexidine
Dose Adjustment Hepatic Not required Absorption Not absorbed
Dose Adjustment Renal Not required Distribution Not absorbed
Dialyzable Unknown Metabolism Not absorbed
Pregnancy Category C Elimination Not absorbed
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to chlorhexidine Black Box Warnings None
Medication Safety Issues: Chlorhexidine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Precedex No
Class: Fluoroquinolone Antibiotic
Dosage Forms. Microcapsules for Oral Suspension: 250 mg/5 mL, 500 mg/5 mL; Oral Tablet: 100 mg, 250 mg, 500 mg, 750 mg; Oral Tablet, Extended Release: 500 mg, 1000 mg
Common FDA Label Indication, Dosing, and Titration.
Anthrax, postexposure prophylaxis: Adults, 500 mg po q12h × at least 60 d, Children, 15 mg/kg po bid × at least 60 d, max 500 mg/dose
Bacterial prostatitis, chronic: 500 mg po q12h × 28 d
Bronchitis, lower respiratory tract infection, infection of bone, skin, or soft tissue, sinusitis: 500-750 mg po q12h × 7-14 d
Urinary tract infectious disease: Immediate release, 250-500 mg po q12h × 3 d, or extended release, 500 mg q24h × 3 d
Off-Label Uses.
Traveler's diarrhea: 750 mg po as a single dose (mild); 500 mg po bid × 3 d (severe)
MOA. Ciprofloxacin is a fluoroquinolone that inhibits bacterial DNA gyrase. It is highly active against aerobic, gram-negative bacilli.
Drug Characteristics: Ciprofloxacin Oral
Dose Adjustment Hepatic Not required Absorption F = 50-85%, minor food effect
Dose Adjustment Renal CrCl 30-50 mL/min, 250-500 mg q12h; CrCl 5-29 mL/min, 250-500 mg q18h Distribution Widespread (bile, CSF, gynecologic tissues, liver, lung, prostate, peritoneum, synovial fluid, sputum, etc)
Dialyzable Dialyzable by both hemodialysis and peritoneal dialysis. Give 250-500 mg q24h after dialysis Metabolism Not metabolized; substrate of P-glycoprotein; strong inhibitor of CYP1A2
Pregnancy Category C Elimination Renal 30-57% with a half-life of 3-6 h
Lactation Weigh risks and benefits Pharmacogenetics Serious and sometimes fatal hemolytic reactions may occur in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency
Contraindications Hypersensitivity to ciprofloxacin or other quinolones, concomitant tizanidine Black Box Warnings Myasthenia gravis, tendon inflammation and rupture, peripheral neuropathy, CNS effects, cardiac, dermatologic and hypersensitivity reactions, aortic dissection and rupture, hypoglycemia, mental health adverse effects
Medication Safety Issues: Ciprofloxacin Oral
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XR No XR formulation No Ceftin,
Class: Fluoroquinolone Antibiotic
Dosage Forms. Otic Solution: 0.2%; Suspension, Intratympanic: 6%
Common FDA Label Indication, Dosing, and Titration.
Otitis externa, acute: Adults and Children >1 y of age, 0.25 mL (entire single-use container) into affected ear(s) bid (approximately q12h) × 7 d
Otitis media with effusion: 0.1 mL (6 mg) once intratympanically to each affected ear following suctioning of middle ear effusion during tympanostomy tube placement
Off-Label Uses.
None
MOA. Ciprofloxacin is a fluoroquinolone that inhibits bacterial DNA gyrase, an enzyme responsible for the unwinding of DNA for transcription and subsequent supercoiling of DNA for packaging into chromosomal subunits. It is highly active against aerobic, gram-negative bacilli, especially Enterobacteriaceae, with MICs often <8.1 mg/L. It is also active against some strains of Pseudomonas aeruginosa and Staphylococcus sp., with an MIC of 0.5-1 mg/L. However, recent reports indicate increasing resistance to this agent in Staphylococcus aureus. It has poor activity against streptococci and anaerobes.
Drug Characteristics: Ciprofloxacin Otic
Dose Adjustment Hepatic Not required Absorption Not systemically absorbed
Dose Adjustment Renal Not required Distribution Not systemically absorbed
Dialyzable Not absorbed Metabolism Not systemically absorbed
Pregnancy Category C Elimination Not systemically absorbed
Lactation Unknown if ciprofloxacin otic solution is excreted into breast milk. Weigh risks and benefits Pharmacogenetics None known that affect otic solution administration
Contraindications Hypersensitivity to ciprofloxacin or other quinolones Black Box Warnings None
Medication Safety Issues: Ciprofloxacin Otic
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No CefTRIAXone, cephalexin No
Class: Macrolide Antibiotic
Dosage Forms. Oral Tablet: 250 mg, 500 mg; Oral Suspension: 125 mg/5 mL; 250 mg/5 mL; Oral Tablet, Extended Release: 500 mg
Common FDA Label Indication, Dosing, and Titration.
Acute infective exacerbation of bronchitis: 250-500 mg po bid × 7-14 d or extended-release tablets, 1000 mg po daily for 7 d
Community-acquired pneumonia, skin infection, sinusitis, pharyngitis: Adults, 250 mg po bid × 7-14 d or extended-release tablets, 1000 mg po daily for 7 d; Children ≥6 mo of age, 15 mg/kg/d divided q12h × 10 d
Disseminated infection due to M. avium-intracellulare group, prophylaxis-HIV infection, primary prevention and treatment: 500 mg po bid
H. pyloriGI tract infection: 500 mg, bid × 10-14 d in combination with various other antibiotics and PPIs
Off-Label Uses.
Bacterial endocarditis prophylaxis for high-risk patients; dental, respiratory, or infected skin/skin structure or musculoskeletal tissue procedures: Adults, 500 mg po 30-60 min prior to procedure; Children, 15 mg/kg po 30-60 min prior to procedure
MOA. Clarithromycin binds to the 50S ribosomal subunit of the 70S ribosome of susceptible organisms, thereby inhibiting bacterial RNA-dependent protein synthesis.
Drug Characteristics: Clarithromycin
Dose Adjustment Hepatic Not required Absorption F = 50%, extended release should be taken with food, immediate release can be taken without regard to food
Dose Adjustment Renal CrCl <30 mL/min, reduce dose by 50% or increase interval to q24h Distribution Gastric tissue, lung, ear fluid, prostate, sputum, soft tissue
Dialyzable Unknown Metabolism Hepatic; substrate of CYP3A4/5 to active metabolites, inhibitor of CYP3A4/5, P-glycoprotein
Pregnancy Category C Elimination Renal 20-40% with a half-life of 5-7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to any macrolide or ketolide antibiotic; concomitant colchicine, cisapride, pimozide, astemizole, terfenadine, ergotamine, dihydroergotamine, or HMG-CoA reductase inhibitors metabolized by CYP3A4/5 Black Box Warnings None
Medication Safety Issues: Clarithromycin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XL No XL formulation No Claritin No
Class: Adrenal Corticosteroid
Dosage Forms. Oral Tablet: 0.5 mg, 0.75 mg, 1 mg, 1.5 mg, 2 mg, 4 mg, 6 mg; Oral Solution: 0.5 mg/5 mL, 1 mg/mL; Oral Elixir: 0.5 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Dosing for indications listed below: Adults, 0.75-9 mg/d po; Children, 0.02-0.3 mg/kg/d in 3-4 divided doses; for all patients, adjust dose according to patient response
Allergic states (eg, asthma, etc)
Dermatologic diseases (eg, exfoliative erythroderma, etc)
Endocrine disorders (eg, adrenocortical insufficiency, etc)
GI diseases (eg, regional enteritis, ulcerative colitis, etc)
Hematologic disorders (eg, acquired hemolytic anemia, etc)
Neoplastic diseases (eg, palliative management of leukemias and lymphomas, etc)
Nervous system (eg, multiple sclerosis, cerebral edema, etc)
Renal diseases (eg, idiopathic nephrotic syndrome, systemic lupus erythematosus, etc)
Respiratory diseases (eg, idiopathic eosinophilic pneumonia, etc)
Rheumatic disorders (eg, rheumatoid arthritis, etc)
Off-Label Uses.
Chemotherapy-induced nausea and vomiting: 20 mg IV before chemotherapy, 8 mg IV or po bid × 3 d after chemotherapy
MOA. Glucocorticosteroids are naturally occurring and synthetic adrenocortical steroids that cause varied metabolic effects. They modify the body's immune responses to diverse stimuli and are used primarily for their anti-inflammatory effects in disorders of many organ systems.
Drug Characteristics: Dexamethasone
Dose Adjustment Hepatic Adjust dose to response Absorption F = 85%
Dose Adjustment Renal Adjust dose to response Distribution Vd = 2 L/kg
Dialyzable Not dialyzable Metabolism Hepatic; substrate of CYP3A4/5; inhibitor of P-glycoprotein; inducer of CYP3A4/5 and P-glycoprotein
Pregnancy Category C Elimination Primarily renal with a half-life of 2-2.5 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to glucocorticosteroids; concurrent use of live vaccines; fungal infections Black Box Warnings None
Class: CNS Stimulant. C-II
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg; Oral Capsule, Extended Release: 5 mg, 10 mg, 15 mg, 20 mg, 25 mg, 30 mg, 35 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
Attention-deficit hyperactivity disorder, methylphenidate-naive patients: Adults, immediate release 2.5 mg po bid (max 20 mg po daily) or extended release 10 mg po daily (max 40 mg/d); Children ≥6 y of age, immediate release 2.5 mg po bid (max 20 mg po daily) or extended release 5 mg po daily (max 30 mg/d)
Attention-deficit hyperactivity disorder, currently using methylphenidate: Adults and Children ≥6 y of age, one-half the total daily dose of extended-release racemic methylphenidate; patients currently using dexmethylphenidate immediate release may be switched to the same daily dose of dexmethylphenidate extended release
Off-Label Uses.
None
MOA. Amphetamines are noncatecholamine sympathomimetic amines with CNS stimulant activity. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.
Drug Characteristics: Dexmethylphenidate
Dose Adjustment Hepatic Not required Absorption F = 22-25%, minimal food effect
Dose Adjustment Renal Not required Distribution Vd = 2.6 L/kg
Dialyzable Unknown Metabolism Extensive via de-esterification
Pregnancy Category C Elimination Minimal renal with a half-life of 3 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to amphetamines, MAOI use, drug dependence, glaucoma, tics, or history of Tourette syndrome Black Box Warnings Tolerance and dependence
Medication Safety Issues: Dexmethylphenidate
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XL No Extended-release capsule, but may open No Methadone, Folotyn No
Class: Digitalis Glycoside
Dosage Forms. Oral Tablet: 62.5 mcg, 125 mcg, 250 mcg; Oral Solution: 0.05 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Atrial fibrillation: Loading dose of 0.25 mg po q2h to a total dose of 1.5 mg, then 0.125-0.375 mg po daily
Heart failure: Premature Infant, loading dose of 20 mcg/kg, then 5 mcg/kg/d; Full-term Infant to Children 2 mo of age, loading dose of 30 mcg/kg, then 8-10 mcg/kg/d; Children 2-23 mo of age, loading dose of 40-50 mcg/kg, then 10-12 mcg/kg/d; Children 2-10 y of age, loading dose of 30-40 mcg/kg (solution), then 8-10 mcg/kg/d; Children >10 y of age, loading dose of 0.75-1.5 mg/kg, then 0.125-0.5 mg/kg po; Adults, loading dose of 0.5-0.75 mg po once, followed by 0.125-0.375 mg po q6-8h to achieve response, followed by 0.125-0.5 mg po daily
Supraventricular tachyarrhythmia: Loading dose of 0.75-1.5 mg po (divided into 3 doses, 50% of total dose initially, followed by 25% of total dose at 6-8 h intervals later), then 0.125-0.5 mg po daily
Off-Label Uses.
Fetal tachycardia, supraventricular tachycardia: 0.125-0.375 mg po daily (administered to mother)
MOA. Digitalis glycosides exert positive inotropic effects through improved availability of calcium to myocardial contractile elements, thereby increasing cardiac output in heart failure. Antiarrhythmic actions are caused primarily by an increase in AV nodal refractory period via increased vagal tone, sympathetic withdrawal, and direct mechanisms.
Drug Characteristics: Digoxin
Dose Adjustment Hepatic Not required Absorption F = 60-80% (tablet); food reduces absorption rate
Dose Adjustment Renal Mild-to-moderate renal impairment, 125 mcg po daily; severe renal impairment, 62.5 mcg po daily; titrate q2wk Distribution Vd = 4-7 L/kg; 25% protein bound
Dialyzable Not dialyzable Metabolism Modest hepatic; substrate of P-glycoprotein
Pregnancy Category C Elimination Renal 57-50% (unchanged) with a half-life of 1.3-2.2 d
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity to digoxin, ventricular fibrillation Black Box Warnings
None
Class: Calcium Channel Blocker
Dosage Forms. Oral Tablet: 30 mg, 60 mg, 90 mg, 120 mg; Oral Capsule, Extended Release, 12 h: 60 mg, 90 mg, 120 mg; Oral Capsule, Extended Release, 24 h: 120 mg, 180 mg, 240 mg, 300 mg, 360 mg, 420 mg; Oral Tablet, Extended Release, 24 h: 120 mg, 180 mg, 240 mg, 300 mg, 360 mg, 420 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertension: Extended release, 12 h, 60-120 mg po bid, may titrate to 360 mg/d po; extended release, 24 h, 120-240 mg po daily, may titrate to 540 mg po daily
Stable, chronic angina: Immediate release, 30 mg po qid, may titrate to 360 mg/d po; extended release, 24 h, 120 mg po daily, may titrate to 540 mg/d po
Atrial arrhythmia and paroxysmal supraventricular tachycardia: 180-360 mg po daily (frequency of dosing based on formulation)
Off-Label Uses.
Hypertension: Children, 1.5-2 mg/kg/d po in 3-4 divided doses, may titrate to 3.5 mg/kg/d po
MOA. Diltiazem is a calcium-channel-blocking drug that decreases heart rate, prolongs AV nodal conduction, and decreases arteriolar and coronary vascular tone. It also has negative inotropic properties.
Drug Characteristics: Diltiazem
Dose Adjustment Hepatic Dosage reduction may be needed Absorption F = 35-40% immediate release, F = 93-95% extended release; food decreases absorption
Dose Adjustment Renal Not required Distribution Vd = 305-391 L; 77-93% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; substrate of CYP3A4/5, P-glycoprotein; moderate inhibitor of CYP3A4/5
Pregnancy Category C Elimination Renal 35% with a half-life of 3-6.6 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to diltiazem; hypotension; 2nd- or 3rd-degree AV block, sick sinus syndrome Black Box Warnings None
Class: Antidiarrheal. C-V
Dosage Forms. Oral Tablet: (Diphenoxylate/Atropine) 2.5 mg/0.025 mg; Oral Solution: (Diphenoxylate/Atropine) 2.5 mg/0.025 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Diarrhea: Children ≥2 y of age, 0.3 mg-0.4 mg/kg/d (diphenoxylate) po in 4 divided doses to max 20 mg/d (diphenoxylate); Adults, 2 tablets po qid until diarrhea resolves, then reduce dose to maintain efficacy, to max 20 mg/d (diphenoxylate)
Off-Label Uses.
None
MOA. Diphenoxylate is a synthetic meperidine congener without analgesic activity that slows GI motility. Because high doses of diphenoxylate (40-60 mg) cause systemic opioid activity, atropine is added in subtherapeutic amounts to decrease abuse potential.
Drug Characteristics: Diphenoxylate/Atropine
Dose Adjustment Hepatic Not required Absorption F = 90%
Dose Adjustment Renal Not required Distribution Vd = 324 L
Dialyzable Not dialyzable Metabolism Rapidly and extensively hepatically metabolized to an active metabolite
Pregnancy Category C Elimination Renal 14% with half-life of 2.5 h (parent), 12-14 h (active metabolite)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to diphenoxylate or atropine products; diarrhea associated with enterotoxin-producing bacteria or pseudomembranous enterocolitis; obstructive jaundice Black Box Warnings None
Medication Safety Issues: Diphenoxylate/Atropine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No LaMICtal, LamISIL, loperamide No
Class: Vaccine, Inactivated, Bacterial
Dosage Forms. Suspension for Intramuscular Injection: Children, primary immunization formulation available in combination with tetanus and acellular pertussis (DTaP, indicated for patients ≤6 y of age), or with tetanus (DT) in combination with other pediatric vaccines; Adults, booster formulation available in combination with tetanus (Td), and tetanus and acellular pertussis (Tdap, indicated for patients ≥10 y of age, or 7-10 y of age if primary vaccination series not completed, has lower dose of diphtheria toxoid and acellular pertussis vaccine than DTaP)
Common FDA Label Indication, Dosing, and Titration.
Prevention of diphtheria: Children, as primary series of DTaP, all infants at 2, 4, 6 mo of age (may be given as early as 6 wk of age and repeated q4-8wk × 3 doses), 4th dose at 15-18 mo of age (≥6 mo since 3rd dose, as early as 12 mo of age), and a 5th dose at 4-6 y of age; booster of Tdap at 11-12 y of age; Adults and Children ≥7 y of age, Td every 10 y if primary series completed (Tdap should replace Td as single dose of 10 y booster in patient who has not completed primary series or if vaccination status unknown); if Child has a valid contraindication to pertussis vaccine, DT should be used to complete primary vaccine series
Off-Label Uses.
None
Drug Characteristics: Diphtheria Toxoid
Pregnancy Category C ADME Not known
Lactation Caution advised; weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to diphtheria toxoid or a component of the vaccine (some formulations may contain: polysorbate 80) Black Box Warnings None
Medication Safety Issues: Diphtheria Toxoid
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Adacel, Daptacel, Tdap, DTaP No
Class: Anticonvulsant
Dosage Forms. Oral Tablet, Extended Release, 24 h: 250 mg, 500 mg; Oral Tablet, Delayed Release: 125 mg, 250 mg, 500 mg; Oral Capsule, Delayed-Release Sprinkles: 125 mg; Oral Solution: 250 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Absence seizure, simple and complex: 15 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
Complex partial epileptic seizure: 10-15 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
Manic bipolar disorder: 25 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
Migraine prophylaxis: Extended release 24 h, 500 mg po daily for 1 wk, then 1 g po daily; delayed release 250 mg po bid, increasing to 500 mg po bid
Off-Label Uses.
None
MOA. Divalproex is composed of sodium valproate and valproic acid. Valproic acid is a carboxylic acid compound whose anticonvulsant activity might be mediated by an inhibitory neurotransmitter, GABA. Valproic acid might increase GABA levels by inhibiting GABA metabolism or enhancing postsynaptic GABA activity. Valproic acid also limits repetitive neuronal firing through voltage- and usage-dependent sodium channels.
Drug Characteristics: Divalproex
Dose Adjustment Hepatic Avoid use in severe hepatic dysfunction Absorption F = 89%, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 11 L; 88-90% protein bound
Dialyzable Yes, but no dosage supplementation required Metabolism Extensive hepatic metabolism; minor substrate of multiple CYP pathways
Pregnancy Category X for migraine prophylaxis; D for all other indications Elimination Renal 30-50% with a half-life of 9-16 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to divalproex, hepatic disease, urea cycle disorders Black Box Warnings Hepatotoxicity, teratogenicity, pancreatitis
Medication Safety Issues: Divalproex
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
ER No Extended release No Depakene, Senokot, vecuronium Avoid in certain circumstances
Class: Tricyclic Antidepressant
Dosage Forms. Oral Capsule: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg; Oral Tablet: 3 mg, 6 mg; Oral Solution: 10 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Depression, anxiety, alcoholism: Very mild, 25-50 mg po daily, may titrate to 300 mg po daily; Mild-moderate, 75 mg po daily, may titrate to 300 mg po daily
Insomnia: Adults <65 y of age, 6 mg po daily hs; Adults ≥65 y of age, 3 mg po daily hs, may titrate to 6 mg po daily hs
Off-Label Uses.
None
MOA. Doxepin is a tricyclic antidepressant, which influences the adrenergic activity at the synapses where it prevents norepinephrine deactivation through reuptake into the nerve terminals. By binding to histamine receptor sites, it competitively inhibits the biological activation of histamine receptors. Antagonism of the H1 receptor is the most likely mechanism by which doxepin exerts its sleep maintenance effect.
Drug Characteristics: Doxepin
Dose Adjustment Hepatic Not required Absorption Food increases AUC and Cmax, delays Tmax
Dose Adjustment Renal Not required Distribution Vd = 20.2 L/kg; 80% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; major substrate of CYP2D6
Pregnancy Category C Elimination Renal with a half-life of 15 h
Lactation Avoid Pharmacogenetics Caution with CYP2D6 poor metabolizers
Contraindications Hypersensitivity to doxepin; MAOI use, glaucoma, severe urinary retention Black Box Warnings Suicidality
Medication Safety Issues: Doxepin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No SINEquan No No SEROquel, doxazosin, digoxin Highly anticholinergic, orthostatic hypotension; avoid dose >6 mg/d
Class: Tetracycline Antibiotic
Dosage Forms. Powder for Oral Suspension: 25 mg/5 mL; Oral Tablet: 20 mg, 50 mg, 75 mg, 100 mg, 150 mg; Oral Capsule, Delayed Release: 40 mg; Oral Tablet, Delayed Release: 50 mg, 75 mg, 100 mg, 150 mg, 200 mg; Oral Capsule: 50 mg, 75 mg, 100 mg, 150 mg; Oral Syrup: 50 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Acinetobacter infection: Children <8 y of age and <45 kg, 2.2-4.4 mg/kg po in 1-2 divided doses; Children >8 y of age and >45 kg and Adults, 100 mg po q12h on d 1, then 100 mg po daily
Acne vulgaris: Children <8 y of age and <45 kg, 2.2-4.4 mg/kg po in 1-2 divided doses; Children >8 y of age and >45 kg and Adults, 100 mg po q12h on d 1, then 100 mg po daily or bid
Gonorrhea, uncomplicated: 100 mg po bid × 7 d or 300-mg po single dose followed in 1 h by another 300-mg dose
Staphylococcal infection of skin: Children <8 y of age and <45 kg, 2.2-4.4 mg/kg po in 1-2 divided doses; Children >8 y of age and >45 kg and Adults, 100 mg po q12h on d 1, then 100 mg po daily
Off-Label Uses.
Lyme disease, prophylaxis: 200 mg po as a single dose
MOA. Doxycycline is a broad-spectrum bacteriostatic compound that inhibits protein synthesis at the 30S ribosomal subunit. Activity includes gram-positive, gram-negative, aerobic, and anaerobic bacteria, as well as spirochetes, mycoplasmas, rickettsiae, chlamydiae, and some protozoa. Many bacteria have developed plasmid-mediated resistance.
Drug Characteristics: Doxycycline
Dose Adjustment Hepatic Not required Absorption F = 100%, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 0.75 L/kg, 80% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, 50%
Pregnancy Category C Elimination Renal 35-45% with a half-life of 15-24 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to doxycycline or concurrent retinoic acid derivatives Black Box Warnings None
Class: Serotonin/Norepinephrine Reuptake Inhibitor
Dosage Forms. Oral Capsule, Delayed Release: 20 mg, 30 mg, 40 mg, 60 mg
Common FDA Label Indication, Dosing, and Titration.
Anxiety: 60 mg po daily, may titrate to 120 mg po daily
Depression: 20-30 mg po bid or 60 mg po once daily, may titrate to 120 mg po daily
Diabetic peripheral neuropathy pain, fibromyalgia, musculoskeletal pain: 60 mg po daily, may titrate to 120 mg po daily
Off-Label Uses.
Urinary incontinence: 40 mg po bid
MOA. Duloxetine is a selective serotonin and norepinephrine reuptake inhibitor that exerts its antidepressant and pain inhibitory actions by potentiating the serotonergic and noradrenergic activity in the CNS. It has no significant affinity for adrenergic, dopaminergic, cholinergic, opioid, glutamate, or histaminergic receptors in vitro and does not inhibit monoamine oxidase.
Drug Characteristics: Duloxetine
Dose Adjustment Hepatic Avoid Absorption F = 30-80%; food slows absorption
Dose Adjustment Renal Initiate at low dose and titrate slowly; avoid if CrCl <30 mL/min Distribution Vd = 1640 L; 90% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; substrate of CYP1A2 and CYP2D6; inhibits CYP2D6
Pregnancy Category C Elimination Renal 70% with a half-life of 8-17 h
Lactation Weigh risks and benefits Pharmacogenetics Use with caution when co-administered with CYP1A2 and 2D6 inhibitors, CYP1A2 inducers, or with agents metabolized by CYP2D6
Contraindications Hypersensitivity to duloxetine; MAOI, TCA, linezolid use, uncontrolled glaucoma Black Box Warnings Suicidality; not approved for children
Medication Safety Issues: Duloxetine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No DULoxetine Delayed-release capsule No FLUoxetine, vortioxetine Avoid in certain circumstances
Class: Antiretroviral Agent, Reverse Transcriptase Inhibitor
Dosage Forms. Oral Capsule: 50 mg, 200 mg; Oral Tablet: 600 mg
Common FDA Label Indication, Dosing, and Titration.
Treatment of HIV-1 infections: Adults and Children ≥40 kg, 600 mg po daily hs; Children <40 kg, weight based; if coadministering with rifampin, increase efavirenz to 800 mg po daily; if coadministering with voriconazole, decrease efavirenz to 300 mg po daily and increase voriconazole to 400 mg po q12h
Off-Label Uses.
None
MOA. Binds to HIV reverse transcriptase, blocking the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication.
Drug Characteristics: Efavirenz
Dose Adjustment Hepatic Avoid if moderate or severe hepatic impairment Absorption F = 42%, food increases absorption by 20-30%
Dose Adjustment Renal Not required Distribution CSF concentration exceeds serum concentration
Dialyzable No Metabolism Hepatic; substrate of via CYP3A/5, 2B6; inhibits CY2C9 and 2C19; induces CYP3A4/5
Pregnancy Category D Elimination Renal 14-34% (metabolites), fecal 16-60% (unchanged) with half-life of 52-76 h
Lactation Avoid Pharmacogenetics Resistance is associated with HIV mutations, CYP2B6 poor metabolizers have increased risk of QTc prolongation
Contraindications Hypersensitivity or concurrent use of bepridil, cisapride, midazolam, pimozide, triazolam, St. John's wort, or ergot alkaloids Black Box Warnings None
Medication Safety Issues: Efavirenz
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No Do not open, crush, or chew capsule Yes No No
Class: Antimigraine Serotonin Receptor Agonist
Dosage Forms. Oral Tablet: 20 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
Migraine: 20-40 mg po at onset of migraine, may repeat after 2 h prn; max single dose 40 mg, max daily dose 80 mg/d
Off-Label Uses.
None
MOA. Eletriptan binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors. It has no significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine, either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system, resulting in the inhibition of pro-inflammatory neuropeptide release.
Drug Characteristics: Eletriptan
Dose Adjustment Hepatic Avoid in severe hepatic dysfunction Absorption F = 50%, high-fat food increases bioavailability 20-30%
Dose Adjustment Renal Not required Distribution Vd = 138 L
Dialyzable Unknown Metabolism Hepatic; substrate of CYP3A4/5
Pregnancy Category C Elimination Nonrenal 90% with a half-life of 4 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to eletriptan, cerebrovascular syndromes, hemiplegic or basilar migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled hypertension Black Box Warnings None
Medication Safety Issues: Eletriptan
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Sumatriptan No
Class: Antiretroviral Agent, Reverse Transcriptase Inhibitor
Dosage Forms. Oral Tablet: (Emtricitabine/Tenofovir) 100 mg/150 mg, 133 mg/200 mg, 167 mg/250 mg, 200 mg/300 mg
Common FDA Label Indication, Dosing, and Titration.
Treatment of HIV-1 infection in combination with other antiretroviral agents: Adults and Children ≥35 kg, Emtricitabine/Tenofovir 200 mg/300 mg po daily; Children <35 kg, weight-based dosing
Preexposure prophylaxis (PrEP) for prevention of HIV-1 infection in adults who are at high risk for acquiring HIV: Emtricitabine/Tenofovir 200 mg/300 mg po daily (high risk is defined as inconsistent condom use, incarcerated, drug, and alcohol dependence)
Off-Label Uses.
Treatment of hepatitis B in patients with antiviral-resistant HBV or coinfection with HIV: Emtricitabine/Tenofovir 200 mg/300 mg po daily
MOA. Emtricitabine is a cytidine analogue while tenofovir is an analogue of adenosine 5'-monophosphate. Each drug interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Drug Characteristics: Emtricitabine/Tenofovir Disoproxil
Dose Adjustment Hepatic Not required Absorption Emtricitabine F = 92%; tenofovir F = 25%, no food effect
Dose Adjustment Renal CrCl = 30-49 mL/min, increase dose interval to 48 h; CrCl <30 mL/min, avoid Distribution Emtricitabine, saliva, semen; tenofovir, lymphocytes
Dialyzable No Metabolism Minimal; tenofovir induces P-glycoprotein
Pregnancy Category B Elimination Emtricitabine, renal 86% (unchanged) with half-life of 10 h; tenofovir, renal 70-80% with half-life of 17 h
Lactation Weigh risks and benefits Pharmacogenetics Resistance is associated with HIV mutations
Contraindications Do not use for preexposure prophylaxis in patients with unknown or HIV-1 positive status. Only for use in combination with other antiretrovirals Black Box Warnings Hepatitis B, lactic acidosis, drug resistance with preexposure prophylaxis
Class: ACE-I, Antihypertensive
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg, 20 mg; Oral Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Heart failure: Infants ≥4 d of age and Adolescents, 0.1-0.5 mg/kg po daily, max 0.94 mg/kg po daily; Adults, 2.5 mg po daily, titrate to 20-40 mg po daily in divided doses
Hypertension: Infants ≥1 mo of age and Adolescents, 0.08 mg/kg up to 5 mg po daily, max 0.58 mg/kg or 40 mg po daily; Adults, 5 mg po daily, max 40 mg po daily in divided doses
Kidney disease, nondiabetic: Children 7-18 y of age, 0.1-0.5 mg/kg po daily, max 20 mg po daily; Adults, 5 mg po daily, max 20 mg po daily
Off-Label Uses.
Diabetic nephropathy: 5-20 mg po daily
MI: 2.5 mg po daily, may titrate to 20 mg po daily
MOA. Enalapril is a prodrug that is rapidly converted to its active metabolite, enalaprilat, a competitive ACE-I. It reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, inhibits the sympathetic nervous system, and inhibits the tissue renin-angiotensin system. The net effect is reduction in total peripheral resistance and blood pressure in hypertensive patients, and reduction of elevated afterload in patients with heart failure.
Drug Characteristics: Enalapril
Dose Adjustment Hepatic Not required Absorption F = 60%, no effect of food on absorption
Dose Adjustment Renal CrCl <30 mL/min, initial dose 2.5 mg po daily, max 40 mg po daily Distribution 50-60% protein bound
Dialyzable Yes Metabolism Extensive hepatic to 1 active metabolite
Pregnancy Category D Elimination Renal 61% with a half-life of 1.3 h (parent drug), 11 h (metabolite)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to enalapril, history of angioedema, pregnancy, concurrent sacubitril Black Box Warnings Pregnancy
Class: Anticoagulant, Low-Molecular-Weight Heparin
Dosage Forms. Prefilled Syringes: 30 mg/0.3 mL, 40 mg/0.4 mL, 60 mg/0.6 mL, 80 mg/0.8 mL, 100 mg/1 mL, 120 mg/0.8 mL, 150 mg/1 mL; Multiple-Dose Vial: 300 mg/3 mL
Common FDA Label Indication, Dosing, and Titration.
Deep vein thrombosis prophylaxis, abdominal surgery: 40 mg sq once 2 h prior to surgery, then daily × 7-10 d
Deep vein thrombosis prophylaxis, hip or knee replacement surgery: 30 mg sq q12h starting 12-24 h postoperatively × 7-14 d
Deep vein thrombosis prophylaxis, acute medical illness: 40 mg sq daily × 6-11 d
Deep vein thrombosis treatment: 1 mg/kg sq q12h or 1.5 mg/kg q24h; initiate warfarin therapy as soon as possible and continue enoxaparin for at least 5 d and until target INR is reached
Acute ST segment elevation myocardial infarction: Adults <75 y of age, 30 mg IV together with 1 mg/kg sq once, then 1 mg/kg sq q12h (max 100 mg for the first 2 doses only); Adults ≥75 y of age, 0.75 mg/kg sq q12h (no initial bolus)
Unstable angina and non-Q-wave myocardial infarction: 1 mg/kg sq q12h × 2-8 d with aspirin 100-325 mg po daily
Off-Label Uses.
None
MOA. Enoxaparin is a low-molecular-weight heparin which has antifactor Xa and IIa properties.
Drug Characteristics: Enoxaparin
Dose Adjustment Hepatic Not required Absorption F = 100% following sq dose
Dose Adjustment Renal CrCl <30 mL/min: avoid use or reduce dose by 50% Distribution Vd = 4.3 L
Dialyzable Not dialyzable Metabolism Hepatic
Pregnancy Category B Elimination Renal 40% with a half-life of 7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to enoxaparin, heparin, or pork products; active major bleeding; concurrent neuraxial analgesia Black Box Warnings Neuraxial anesthesia may cause hematomas
Class: Anaphylaxis Agent
Dosage Forms. Solution for Auto-injection: 0.1 mg/0.1 mL, 0.15 mg/0.15 mL, 0.15 mg/0.3 mL, 0.3 mg/0.3 mL
Common FDA Label Indication, Dosing, and Titration.
Emergency treatment of acute anaphylaxis due to allergic reactions: Using auto-injector, Children 7.5-14 kg, 0.1 mg IM or sq; Children 15-30 kg, 0.15 mg IM or sq; Children >30 kg and Adults, 0.3 mg IM or sq; may be repeated if severe anaphylaxis persists
Off-Label Uses.
None
MOA. Epinephrine treats severe allergic reactions to insect stings or bites, foods, drugs, and other allergens. It acts on both α- and β-adrenergic receptors. Through its action on α-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on β-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation that helps alleviate bronchospasm, wheezing, and dyspnea that may occur during anaphylaxis. Epinephrine also alleviates pruritus, urticaria, and angioedema.
Drug Characteristics: Epinephrine
Dose Adjustment Hepatic Not required Absorption 20% of dose rapidly absorbed after sq dose; remaining 80% absorbed over 6-8 h
Dose Adjustment Renal Not required Distribution N/A
Dialyzable Not dialyzable Metabolism Rapid and complete hepatic
Pregnancy Category C Elimination Renal as inactivated metabolites
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications None in emergency situations Black Box Warnings None
Class: Erythropoietic Stimulating Agent
Dosage Forms. Injection Solution: 2000 units/mL, 3000 units/mL, 4000 units/mL, 10 000 units/mL, 20 000 units/mL, 40 000 units/mL
Common FDA Label Indication, Dosing, and Titration.
Anemia of cancer chemotherapy: Children, 600 units/kg (max 40 000 units) IV once weekly; Adults, 40 000 units sq weekly; dose adjusted based on changes in Hgb levels
Anemia of chronic renal failure: Children, 50 units/kg IV or sq 3 times per week; Adults not on dialysis, 10 000 units sq weekly, 20 000 units sq every other week, 30 000 units every 3rd wk, or 40 000 units sq every 4 wk; Adults on dialysis, 50-100 units/kg IV or sq 3 times per week; dose adjusted based on changes in Hgb levels
Perioperative collection of blood for allogeneic infusion: 300 units/kg/d sq for 10 d before surgery, on the day of surgery, and for 4 d postoperatively
Off-Label Uses.
Anemia due to myelodysplastic syndrome: 40 000-60 000 units sq 1-3 times/wk
MOA. Epoetin alfa is recombinant human erythropoietin. It binds to the erythropoietin receptor on erythroid progenitor cells, stimulating production/differentiation of mature red cells.
Drug Characteristics: Epoetin
Dose Adjustment Hepatic Not required Absorption Subcutaneously, F = 22-33%
Dose Adjustment Renal Not required Distribution Vd = 52 mL/kg
Dialyzable Not dialyzable Metabolism Hepatic via galactose receptors
Pregnancy Category C Elimination Renal (minimal) with a half-life of 4-13 h (in CKD patients), 16-67 h (in anemic cancer patients)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to epoetin, albumin, uncontrolled hypertension Black Box Warnings Increased CV, stroke, DVT, mortality risk; cancer recurrence
Medication Safety Issues: Epoetin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Neupogen, darbepoetin No
Class: SSRI Antidepressant
Dosage Forms. Oral Tablet: 5 mg, 10 mg, 20 mg; Oral Solution: 5 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Depression: Children ≥12 y of age and Adults, 10 mg po daily, may titrate to 20 mg po daily
Generalized anxiety disorder: 10 mg po daily, may titrate to 20 mg po daily
Off-Label Uses.
OCD: 20-60 mg po daily
Panic disorder: 20-30 mg po daily, may titrate to 60 mg po daily
Hot flashes: 10 mg once po daily, may increase to 20 mg once daily after 4 wk
MOA. Escitalopram is the s-enantiomer of racemic citalopram and is an antidepressant that is a selective and potent inhibitor of presynaptic reuptake of serotonin (an SSRI). It does not affect reuptake of norepinephrine or dopamine and has a relative lack of affinity for muscarinic, histamine, α1- and α2-adrenergic, and serotonin receptors.
Drug Characteristics: Escitalopram
Dose Adjustment Hepatic Dose at 10 mg po daily Absorption F = 80%, food has no effect on absorption
Dose Adjustment Renal Use with caution in severe renal impairment Distribution Vd = 12 L/kg; 56% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; substrate of CYP3A4/5, CYP2C19
Pregnancy Category C Elimination Renal 10% with a half-life of 27-32 h
Lactation Avoid Pharmacogenetics Increased risk of adverse reactions with CYP2C19 poor metabolizers
Contraindications Hypersensitivity to citalopram or escitalopram; concurrent MAOI use Black Box Warnings Suicidality
Medication Safety Issues: Escitalopram
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Loxitane Avoid in certain circumstances
Class: Proton Pump Inhibitor
Dosage Forms. Oral Capsule, Delayed Release: 20 mg, 40 mg, 49.3 mg; Oral Tablet, Delayed Release: 20 mg; Oral Granules: 2.5 mg, 5 mg, 10 mg, 20 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
Helicobacter pylori GI infection: 40 mg po daily × 10-14 d in combination with amoxicillin 1000 mg and clarithromycin 500 mg po bid
Erosive esophagitis, GERD treatment: Children 1-11 y of age and <20 kg, 10 mg po daily × 8 wk; Children ≥20 kg, 10-20 mg po daily × 8 wk; Adults, 20-40 mg po daily × 4-8 wk
Erosive esophagitis, heartburn: Children 1-11 y of age, 10 mg po daily × 8 wk; Children ≥12 y of age and Adults, 20-40 mg po daily × up to 8 wk
Prevention of NSAID-induced gastropathy: 20-40 mg po daily × up to 6 mo
Zollinger-Ellison syndrome: 40 mg po bid up to 240 mg/d
Off-Label Uses.
None
MOA. Esomeprazole is a proton pump inhibitor (PPI) that, when protonated in the secretory canaliculi of the parietal cells, covalently binds to H+/K+-ATPase (proton pump), which is the final pathway for acid secretion. Esomeprazole produces a profound and prolonged antisecretory effect, and inhibits basal, nocturnal, pentagastrin-stimulated, and food-stimulated gastric acid secretion.
Drug Characteristics: Esomeprazole
Dose Adjustment Hepatic Severe, max dose of 20 mg daily Absorption F = 90%, food reduces F by 50%
Dose Adjustment Renal Not required Distribution Vd = 16 L; 97% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic; substrate of CYP2C19; inducer of CYP2C19
Pregnancy Category B Elimination Renal 80% with a half-life of 60-90 min
Lactation Weigh risks and benefits Pharmacogenetics For CYP2C19 poor metabolizers should consider 20 mg dose; moderate CYP2C19 inhibitor
Contraindications Hypersensitivity to omeprazole or esomeprazole Black Box Warnings None
Class: Estrogen
Dosage Forms. Oral Tablet: 0.5 mg, 1 mg, 2 mg
Common FDA Label Indication, Dosing, and Titration.
Abnormal vasomotor function (moderate to severe), menopause: 1-2 mg po daily for 21 d followed by 7 d off
Atrophic vulva or vagina (moderate to severe), menopause: Oral tablet, 1-2 mg po daily in a cyclical pattern (3 wk on, 1 wk off)
Breast cancer, metastatic, for palliation only: 10 mg po tid × 3 mo
Carcinoma of prostate, advanced, androgen-dependent, for palliation only: 1-2 mg po tid
Decreased estrogen level, secondary to hypogonadism, castration, or primary ovarian failure: 1-2 mg po daily
Postmenopausal osteoporosis, prophylaxis: 0.5 mg po daily for 23 d followed by 5 d off
Off-Label Uses.
None
MOA. Estradiol (17β-estradiol; E2) is the most potent of the naturally occurring estrogens and the major estrogen secreted during the reproductive years. Estradiol and other estrogens produce characteristic effects on specific tissues (such as breast), cause proliferation of vaginal and uterine mucosa, increase calcium deposition in bone, and accelerate epiphyseal closure after initial growth stimulation.
Drug Characteristics: Estradiol Oral
Dose Adjustment Hepatic Not required Absorption F = 40%, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Widely distributed; 98% protein bound
Dialyzable Yes Metabolism Extensive hepatic; substrate of many CYP pathways, major substrate of CYP3A4/5, 1A2, P-glycoprotein
Pregnancy Category X Elimination Renal with a half-life of 21 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to estradiol; history of thromboembolic disorders, breast cancer, any estrogen-dependent neoplasm, known or suspected pregnancy Black Box Warnings Endometrial and breast cancer risk, dementia risk; should not be used to reduce CV risk; secondary exposure risk (transdermal solution)
Class: Estrogen
Dosage Forms. Transdermal Patch, Once Weekly or Twice Weekly: 0.014 mg/d, 0.025 mg/d, 0.0375 mg/d, 0.05 mg/d, 0.06 mg/d, 0.075 mg/d, 0.1 mg/d
Common FDA Label Indication, Dosing, and Titration.
Abnormal vasomotor function or atrophic vagina or vulva (moderate-severe), menopause: 0.025-0.0375 mg/d patch applied to the skin twice weekly (dose and frequency of patch change dependent on specific product selected); adjust dose as necessary based on response and attempt taper and discontinuation at 3-6 mo intervals
Postmenopausal osteoporosis, prophylaxis: 0.014-0.025 mg/d patch applied to the skin once or twice weekly (dose and frequency of patch change dependent on specific product selected); adjust dose as necessary based on response
Off-Label Uses.
None
MOA. Estradiol (17β-estradiol; E2) is the most potent of the naturally occurring estrogens and the major estrogen secreted during the reproductive years. Estradiol and other estrogens produce characteristic effects on specific tissues (such as breast), cause proliferation of vaginal and uterine mucosa, increase calcium deposition in bone, and accelerate epiphyseal closure after initial growth stimulation.
Drug Characteristics: Estradiol Transdermal Patch
Dose Adjustment Hepatic Not required Absorption F improved by bypassing first-pass metabolism via topical administration
Dose Adjustment Renal Not required Distribution Widely distributed; 98% protein bound
Dialyzable Yes Metabolism Extensive hepatic; substrate of many CYP pathways, major substrate of CYP3A4/5, 1A2, P-glycoprotein
Pregnancy Category X Elimination Renal with a half-life of 21 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to estradiol; history of thromboembolic disorders, breast cancer, any estrogen-dependent neoplasm, pregnancy Black Box Warnings Endometrial and breast cancer risk, dementia risk; should not be used to reduce CV risk; secondary exposure risk (transdermal solution)
Class: Antirheumatic, Disease Modifying
Dosage Forms. Solution Auto-injector: 50 mg/1 mL; Solution Prefilled Syringe: 25 mg/0.5 mL, 50 mg/1 mL; Powder for Reconstitution: 25 mg
Common FDA Label Indication, Dosing, and Titration.
Ankylosing spondylitis: Adults, 50 mg sq once per wk or 25 mg sq twice per wk
Polyarticular juvenile idiopathic arthritis: Children ≥2 y of age and <63 kg, 0.8 mg/kg (max 50 mg) sq once per wk; ≥63 kg, 50 mg once per wk
Plaque psoriasis: Adults, 50 mg twice per wk × 3 mo, then 50 mg sq once per wk
Psoriatic arthritis: Adults, 50 mg sq once per wk or 25 mg sq twice per wk
Rheumatoid arthritis: Adults, 50 mg sq once per wk or 25 mg sq twice per wk
Off-Label Uses.
Acute graft-versus-host disease: Adults, 0.4 mg/kg sq (max 25 mg/dose) twice per wk × 8 wk
MOA. Etanercept is a recombinant DNA-derived protein composed of tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. Etanercept binds to soluble human tumor necrosis factor alpha (TNF-alpha) with the p55 and p75 cell surface TNF receptors.
Drug Characteristics: Etanercept
Dose Adjustment Hepatic Not required Absorption F = 60%
Dose Adjustment Renal Not required Distribution Vd = 1.78-3.39 L/m2
Dialyzable Unknown Metabolism Not metabolized
Pregnancy Category B Elimination Half-life of 102 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, sepsis Black Box Warnings Serious infections, malignancies
Medication Safety Issues: Etanercept
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Levbid No
Class: NSAID
Dosage Forms. Tablet, Immediate Release: 400 mg, 500 mg; Tablet, Extended Release: 400 mg, 500 mg, 600 mg; Capsule, Immediate Release: 200 mg, 300 mg
Common FDA Label Indication, Dosing, and Titration.
General pain: Immediate release, 200-400 mg po q6h; max 1000 mg/d
Osteoarthritis and rheumatoid arthritis: Immediate release, 300 mg po bid-tid or 400-500 mg po bid; extended release, 400-1000 mg po daily; max 1000 mg/d
Juvenile rheumatoid arthritis: Extended release, Children 6-16 y of age and 20-30 kg, 400 mg po daily; 31-45 kg, 600 mg po daily; 46-60 kg, 800 mg po daily; >60 kg, 1000 mg po daily
Off-Label Uses.
None
MOA. Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) and reversibly alters platelet function and prolongs bleeding time.
Drug Characteristics: Etodolac
Dose Adjustment Hepatic Not required Absorption F = 80%, food has minimal effect on absorption
Dose Adjustment Renal Avoid in severe renal failure Distribution Vd = 393 mL/kg (immediate release); Vd = 570 mL/kg (extended release); 99% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic not via CYP450
Pregnancy Category C Elimination Renal 72% with a half-life of 6-7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to etodolac; concurrent use of ketorolac or pentoxifylline; allergic-type reaction following aspirin or other NSAID; CABG surgery, treatment of perioperative pain Black Box Warnings Cardiovascular and GI risk
Medication Safety Issues: Etodolac
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
CR No Extended-release product No Lopid Avoid chronic use
Class: Antihyperlipidemic, Cholesterol Absorption Inhibitor
Dosage Forms. Oral Tablet: 10 mg
Common FDA Label Indication, Dosing, and Titration.
Familial hypercholesterolemia-homozygous, with atorvastatin or simvastatin: Adults and Children >10 y of age, 10 mg po daily
Mixed hyperlipidemia: 10 mg po daily in combination with fenofibrate
Primary hypercholesterolemia: 10 mg po daily, alone or in combination with an HMG-CoA reductase inhibitor (statin)
Off-Label Uses.
None
MOA. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins and of fenofibrate.
Drug Characteristics: Ezetimibe
Dose Adjustment Hepatic Avoid if moderate or severe hepatic dysfunction Absorption F variable, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 105 L; 90% protein bound
Dialyzable Unknown Metabolism In intestine and liver, not via CYP450
Pregnancy Category C Elimination Renal 11% with a half-life of 9-30 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to ezetimibe, gallbladder disease, severe hepatic dysfunction, concurrent use with a statin in a pregnant or nursing mother Black Box Warnings None
Medication Safety Issues: Ezetimibe
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoNoNoZestrilNo
Class: Histamine H2 Antagonist
Dosage Forms. Oral Tablet: 10 mg, 20 mg, 40 mg; Powder for Oral Suspension: 40 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Duodenal ulcer, acute: Children >1 y of age, 0.5 mg/kg/d po hs, max 40 mg/d; Adults, 20 mg po bid or 40 mg po daily hs
Duodenal ulcer, maintenance: Adults, 20 mg po daily hs
Gastroesophageal reflux disease: Children >1 y of age, 1 mg/kg/d po hs, max 80 mg/d, duration based on response; Adults, 20-40 mg po bid × up to 12 wk
Gastric ulcer, acute: Children >1 y of age, 0.5 mg/kg/d po hs, max 40 mg/d; Adults, 40 mg po daily hs
Indigestion (OTC): 10-20 mg po bid
Off-Label Uses.
None
MOA. Famotidine is a competitive inhibitor of histamine H2 receptors. The primary clinically important pharmacologic activity of famotidine is inhibition of gastric secretion. Both the acid concentration and the volume of gastric secretion are suppressed by famotidine, while changes in pepsin secretion are proportional to volume output.
Drug Characteristics: Famotidine
Dose Adjustment Hepatic Not required Absorption F = 40-45%, no effect of food on absorption
Dose Adjustment Renal Adults, CrCl <50 mL/min, reduce dose 50% or increase dosing interval to 36-48 h; Children, CrCl 30-60 mL/min/1.73 m2, administer 50% of dose; Children, CrCl <30 mL/min/1.73 m2, administer 25% of dose Distribution Vd = 1.3 L/kg; 10-20% protein bound
Dialyzable Not dialyzable Metabolism Minimal
Pregnancy Category B Elimination Renal 60% with a half-life of 2.5-3.5 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to famotidine or other H2 antagonists Black Box Warnings None
Class: Antihyperlipidemic
Dosage Forms. Oral Tablet: 35 mg, 40 mg, 48 mg, 54 mg, 105 mg, 120 mg, 145 mg, 160 mg; Oral Capsule: 30 mg, 43 mg, 50 mg, 67 mg, 90 mg, 130 mg, 134 mg, 150 mg, 200 mg; Oral Capsule, Delayed Release: 45 mg, 135 mg
Common FDA Label Indication, Dosing, and Titration.
Hypercholesterolemia, primary hypercholesterolemia, or mixed dyslipidemia (Frederickson type 2a, 2b): 160 mg po daily
Hypertriglyceridemia, Frederickson types 4 and 5 hyperlipidemia: 54-160 mg po daily
Off-Label Uses.
None
MOA. Fibric acid derivatives activate peroxisome proliferator-activated receptor α (PPARα), which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly.
Drug Characteristics: Fenofibrate
Dose Adjustment Hepatic Avoid use in severe hepatic impairment Absorption F = 60%, absorption increased when taken with food
Dose Adjustment Renal Avoid use in severe renal impairment Distribution Vd = 60 L; >99% protein bound
Dialyzable Not dialyzable Metabolism Prodrug that undergoes rapid hydrolysis at the ester bond to fenofibric acid; fenofibric acid is glucuronidated in the liver
Pregnancy Category C Elimination Renal 60-93% with a half-life of 24 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity, gallbladder disease, severe renal or hepatic dysfunction, nursing mothers Black Box Warnings
Class: Opioid Analgesic. C-II
Dosage Forms. Transdermal Patch: 12.5 mcg/h, 25 mcg/h, 50 mcg/h, 75 mcg/h, 87.5 mcg/h, 100 mcg/h; Transdermal Iontophoretic System: 40 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Pain, chronic (moderate to severe): Adults and Children >2 y of age, opioid tolerant, with pain that cannot be managed by other means, transdermal fentanyl dosage based on the patient's current 24-h oral morphine requirement; replace patch q72h; may replace patch q48h in patients not achieving adequate analgesia
Off-Label Uses.
None
MOA. Fentanyl is a phenylpiperidine opioid agonist with predominant effects on the mu opioid receptor and is about 50-100 times more potent as an analgesic than morphine.
Drug Characteristics: Fentanyl Transdermal
Dose Adjustment Hepatic Not required Absorption F = 92% with transdermal
Dose Adjustment Renal CrCl <10 mL/min, reduce dose by 50% Distribution Vd = 6 L/kg; 80-85% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic metabolism, CYP3A4/5 substrate
Pregnancy Category C Elimination Renal 75% with a half-life of 20-24 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Acute or postoperative pain, bronchial asthma, hypersensitivity to fentanyl, mild or intermittent pain management, opioid nontolerant patients, paralytic ileus Black Box Warnings CYP3A4/5 inhibitors; respiratory depression; transdermal not for use postoperatively; fatalities in children; formulations not interchangeable; fever; care with disposal; REMS program; concurrent use with benzodiazepines or other CNS depressants
Medication Safety Issues: Fentanyl Transdermal
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
Suffix describes mcg/h of fentanyl delivered. Transdermal fentanyl patches should always be prescribed in mcg/h, not size FentaNYL Do not cut patch
Class: Antihistamine
Dosage Forms. Oral Tablet: 60 mg, 180 mg; Oral Disintegrating Tablet: 30 mg; Oral Suspension: 30 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Seasonal allergic rhinitis (OTC): Children 2-11 y of age, 30 mg po bid; Children ≥12 y of age and Adults, 60 mg po bid or 180 mg po daily
Idiopathic urticaria: Children 6 mo-2 y of age, 15 mg po bid; Children 2-11 y of age, 30 mg po bid; Children ≥12 y of age and Adults, 60 mg po bid or 180 mg po daily
Off-Label Uses.
Perennial allergic rhinitis: Children 2-11 y of age, 30 mg po bid; Children ≥12 y of age and Adults, 60 mg po bid or 180 mg po daily
MOA. Fexofenadine, the major active metabolite of terfenadine, is an antihistamine with selective peripheral H1-receptor antagonist activity. Both enantiomers of fexofenadine displayed approximately equipotent antihistaminic effects.
Drug Characteristics: Fexofenadine
Dose Adjustment Hepatic Not required Absorption Rapidly absorbed, bioavailability not established
Dose Adjustment Renal Use with caution Distribution Vd = 5.4-5.8 L/kg
Dialyzable Not dialyzable Metabolism Little hepatic or extrahepatic metabolism
Pregnancy Category C Elimination Fecal 80% with a half-life of 14-18 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to fexofenadine Black Box Warnings None
Medication Safety Issues: Fexofenadine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
Allergy, 24-HR No Do not split or chew disintegrating tablet No Viagra No
Class: Imidazole Antifungal
Dosage Forms. Oral Suspension: 10 mg/mL, 40 mg/mL; Oral Tablet: 50 mg, 100 mg, 150 mg, 200 mg
Common FDA Label Indication, Dosing, and Titration.
Candidal vulvovaginitis, uncomplicated: 150 mg po × 1
Candidal vulvovaginitis, complicated: 150 mg po q72h × 3 doses
Candidiasis, systemic: Adults, 400 mg po daily; Children ≥6 mo of age, 6-12 mg/kg/d po
Cryptococcal meningitis: Adults, 400-800 mg po daily × 8 wk, then 200 mg po daily × 6-12 mo; Children ≥6 mo of age, 12 mg/kg po on day 1, then 6 mg/kg/d (max 12 mg/kg/d) for 10-12 wk
Oropharyngeal candidiasis: Adults, 100-200 mg po daily × 7-14 d; Children ≥6 mo of age, 6 mg/kg po on day 1, then 3 mg/kg once daily for at least 2 wk
Off-Label Uses.
Onychomycosis due to dermatophyte: 200 mg po qwk × 3 mo (fingernails) or × 6 mo (toenails)
Tinea: 200 mg po qwk × 3 doses
MOA. Fluconazole inhibits biosynthesis of ergosterol or other sterols, damaging the fungal cell wall membrane and altering its permeability.
Drug Characteristics: Fluconazole
Dose Adjustment Hepatic Not required Absorption F = 90% with no food effect
Dose Adjustment Renal Not required for single-dose therapy; for repeated dose therapy, CrCl 21-50 mL/min, increase dosing interval to 48 h or decrease dose by 50%; CrCl <10 mL/min, extend dosing interval to 48 h and decrease dose by 50% Distribution Blister, CSF, nails, skin, saliva, sputum, vaginal tissue, urine
Dialyzable 100% of dose is removed by hemodialysis Metabolism Minimal metabolism, but moderate inhibitor of CYP2C19, 3A4/5 and strong inhibitor of CYP2C9
Pregnancy Category C Elimination Renal 80% (unchanged) with a half-life of 30 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to fluconazole, concurrent ergot alkaloids, CYP3A4/5 substrates that prolong QTc Black Box Warnings None
Class: Topical Corticosteroid
Dosage Forms. Topical Cream: 0.05%, 0.1%; Topical Ointment: 0.05%; Topical Solution: 0.05%; Topical Gel: 0.05%
Common FDA Label Indication, Dosing, and Titration.
Skin disorders, corticosteroid responsive: Children ≥12 y of age and Adults, apply thin layer topically to affected area daily to qid (max 2 wk)
Plaque psoriasis: Children ≥12 y of age and Adults, apply thin layer topically to affected area daily to qid (max 2-4 wk)
Atopic dermatitis: Children ≥12 y of age and Adults, apply thin layer topically to affected area daily to qid (max 2 wk)
Off-Label Uses.
Oral lichen planus: Apply thin layer topically bid with antimycotics
MOA. Fluocinonide is an anti-inflammatory, antipruritic, and vasoconstrictive corticosteroid. Corticosteroids are thought to act by the induction of phospholipase A2-inhibitory proteins, lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Drug Characteristics: Fluocinonide
Dose Adjustment Hepatic Not required Absorption Minimal absorption unless covering large surface area or covering areas lacking skin integrity
Dose Adjustment Renal Not required Distribution Not absorbed
Dialyzable Unknown Metabolism Not absorbed
Pregnancy Category C Elimination Not absorbed
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to fluocinonide or other corticosteroids Black Box Warnings None
Class: SSRI Antidepressant
Dosage Forms. Oral Capsule: 10 mg, 20 mg, 40 mg; Oral Capsule, Delayed Release, Weekly: 90 mg; Oral Tablet: 10 mg, 20 mg, 60 mg; Oral Solution: 20 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Depression: Adults, 20 mg po daily, may titrate to 80 mg po daily; Children ≥8 y of age, 10-20 mg po daily, max 20 mg po daily
OCD: Adults, 20 mg po daily, may titrate to 80 mg po daily; Children ≥7 y of age, 10 mg po daily, may titrate to 60 mg po daily
Panic disorder: 10 mg po daily, may increase to 60 mg po daily
Premenstrual dysphoric disorder: 20 mg po daily or for 14 d prior to expected start of menses through the first full d of menses, may titrate to 80 mg po daily
Bulimia nervosa: 20 mg po daily
Off-Label Uses.
Posttraumatic stress disorder: 20-80 mg po daily
Fibromyalgia: 20-80 mg po daily
MOA. Fluoxetine is a bicyclic antidepressant that is a selective and potent inhibitor of presynaptic reuptake of serotonin (an SSRI).
Drug Characteristics: Fluoxetine
Dose Adjustment Hepatic Use lower dose Absorption F = 100%; no effect of food on absorption
Dose Adjustment Renal Not required Distribution Vd = 12-43 L/kg; 95% protein bound
Dialyzable Not dialyzable Metabolism >90% hepatic, CYP2C9 and CYP2D6 substrate; strong CYP2D6 inhibitor, moderate 2C19 inhibitor
Pregnancy Category C Elimination Renal 60% with half-life of 4-6 d
Lactation Avoid Pharmacogenetics Use caution in CYP2D6 poor metabolizers
Contraindications Hypersensitivity; concomitant pimozide, thioridazine, or MAOIs Black Box Warnings Suicidality; approved in children >7 y of age
Class: Intranasal Adrenal Glucocorticosteroid
Dosage Forms. Nasal Spray: 27.5 mcg/actuation, 50 mcg/actuation; Nasal Exhaler Suspension: 93 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Allergic rhinitis: Children ≥4 y of age and Adults, 2 sprays/nostril daily or 1 spray/nostril bid; max 2 sprays/nostril/d (200 mcg/d)
Nonallergic rhinitis: Children ≥4 y of age and Adults, 2 sprays/nostril daily or 1 spray/nostril bid; max 2 sprays/nostril/d (200 mcg/d)
Nasal polyps: Adults ≥18 y of age, Xhance product, 1 spray/nostril bid; may increase to max 2 sprays/nostril bid (744 mcg/d)
Off-Label Uses.
Adjunct to antibiotics in empiric treatment of acute bacterial rhinosinusitis: 1 spray/nostril bid
MOA. Fluticasone has anti-inflammatory, antipruritic, and vasoconstrictive properties. Corticosteroids are thought to act by the induction of phospholipase A2-inhibitory proteins, lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Drug Characteristics: Fluticasone Nasal
Dose Adjustment Hepatic Not required Absorption <2% of dose absorbed systemically after nasal administration
Dose Adjustment Renal Not required Distribution Vd = 4 L/kg after nasal administration
Dialyzable Not dialyzable Metabolism Complete first-pass metabolism
Pregnancy Category C Elimination Fecal with half-life (calculated from IV dose) of 5-7 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Class: Inhaled Adrenal Corticosteroid
Dosage Forms. Metered-Dose Inhaler (MDI): 44 mcg/actuation, 110 mcg/actuation, 220 mcg/actuation; Aerosol Powder for Inhalation: 50 mcg/actuation, 100 mcg/actuation, 200 mcg/actuation, 250 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Asthma: Children 4-11 y of age, regardless of previous treatment, starting dose 88 mcg bid with max dose of 88 mcg bid; Children ≥12 y of age and Adults previously treated with inhaled bronchodilators alone, 88 mcg bid; titrate dose to response with max 440 mcg bid; if previously treated with inhaled corticosteroids, starting dose 88-220 mcg bid; titrate dose to response with max 440 mcg bid; if previously treated with oral corticosteroids, starting dose 440 mcg bid; titrate dose to response with max 880 mcg bid
Off-Label Uses.
None
MOA. Fluticasone is a synthetic trifluorinated corticosteroid with anti-inflammatory effects. It is a human glucocorticoid receptor agonist that inhibits multiple cell types and mediator production or secretion involved in asthma. Glucocorticosteroids are naturally occurring and synthetic adrenocortical steroids, cause varied metabolic effects, modify the body's immune responses to diverse stimuli, and are used primarily for their anti-inflammatory effects in disorders of many organ systems.
Drug Characteristics: Fluticasone Oral Inhaler
Dose Adjustment Hepatic Not required Absorption F = 18-30% after MDI administration
Dose Adjustment Renal Not required Distribution Vd ∼4 L/kg after oral inhalation
Dialyzable Not dialyzable Metabolism Complete first-pass metabolism via CYP3A4/5
Pregnancy Category C Elimination Renal <5% with half-life of 11-12 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity or severe allergy to milk proteins (included in the inhalation powder); should not be used for primary treatment of status asthmaticus or other acute episodes of asthma requiring intensive intervention Black Box Warnings None
Class: Inhaled Corticosteroid and Long-Acting β2-Adrenergic Agonist Combination
Dosage Forms. Metered-Dose Inhaler (MDI): (Fluticasone/Salmeterol) 45 mcg/21 mcg/actuation, 115 mcg/21 mcg/actuation, 230 mcg/21 mcg/actuation; Aerosol Powder for Inhalation: (Fluticasone/Salmeterol) 55 mcg/14 mcg/actuation, 100 mcg/50 mcg/actuation, 113 mcg/14 mcg/actuation, 232 mcg/14 mcg/actuation, 250 mcg/50 mcg/actuation, 500 mcg/50 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Asthma: 1 disk or 2 MDI puffs q12h, starting at dose appropriate for asthma severity, adjust dose to patient response
Chronic obstructive pulmonary disease (COPD): fluticasone 250 mcg/salmeterol 50 mcg bid (disk formulation, max fluticasone 250 mcg/salmeterol 50 mcg bid)
Off-Label Uses.
None
MOA. Fluticasone is a synthetic trifluorinated corticosteroid with anti-inflammatory effects. It is a human glucocorticoid receptor agonist that inhibits multiple cell types and mediator production or secretion involved in asthma and COPD. Salmeterol is a long-acting β2-adrenergic agonist, stimulates intracellular adenylyl cyclase in catalyzing the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). The increased cyclic AMP levels result in the relaxation of bronchial smooth muscle and inhibition of the release of mediators of instantaneous hypersensitivity from mast cells.
Drug Characteristics: Fluticasone/Salmeterol
Dose Adjustment Hepatic Not required Absorption After inhalation, fluticasone F = 18% and salmeterol is undetectable
Dose Adjustment Renal Not required Distribution Both fluticasone and salmeterol are largely (>90%) protein bound
Dialyzable Not dialyzable Metabolism Fluticasone undergoes complete first-pass metabolism; salmeterol is extensively metabolized in the liver by CYP3A4/5
Pregnancy Category C Elimination Renal <5% for both components; fluticasone half-life after inhalation of 5-7 h, salmeterol half-life after oral administration of 5.5 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to any component of the product, including milk proteins (included in the inhalation powder); should not be used as primary treatment of status asthmaticus or acute episodes of asthma or COPD, posaconazole coadministration Black Box Warnings Increased asthma-related deaths
Class: Essential B Vitamin
Dosage Forms. Oral Tablet: 0.4 mg, 0.8 mg, 1 mg; Oral Capsule: 0.8 mg, 5 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Folic acid deficiency: Infants, 0.1 mg/d po; Children age <4 y, up to 0.3 mg/d po; Children ≥4 y of age, 0.4-1 mg/d po; Adults, 0.4-1 mg po daily
Off-Label Uses.
Prevention of neural tube defects: Females of childbearing potential, 0.4-0.8 mg po daily (starting at least 1 mo prior to pregnancy, continuing through 12 wk gestation); Females at high risk of pregnancy with neural tube defect (previous history or family history of pregnancy with neural tube defect), 4 mg po daily (starting at least 3 mo prior to pregnancy and continuing through 12 wk gestation)
Prevention of methotrexate toxicity: 5-27.5 mg po weekly
MOA. Folic acid is required for the conversion of deoxyuridylate to thymidylate, which is a rate-limiting step in DNA synthesis, which presents clinically as macrocytic anemia when red blood cells are unable to extrude their nucleus.
Drug Characteristics: Folic Acid
Dose Adjustment Hepatic Not required Absorption F = 76-93%
Dose Adjustment Renal Not required Distribution Stored in the liver and most tissues
Dialyzable Yes, hemodialysis Metabolism Metabolized in the liver to active metabolite, 5-methyltetrahydrofolate
Pregnancy Category A Elimination Renal 30%
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Folic Acid
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Folinic acid No
Class: ACE-I, Antihypertensive
Dosage Forms. Oral Tablet: 10 mg, 20 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
Heart failure: 5-10 mg po daily, may titrate to 40 mg po daily
Hypertension: Children 6-16 y of age and >50 kg, 5-10 mg po daily, may titrate to 40 mg po daily; Adults, 10 mg po daily, may titrate to 80 mg po daily
Off-Label Uses.
None
MOA. Fosinopril is a competitive ACE-I. It also reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, and can alter prostanoid metabolism, inhibit the sympathetic nervous system, and inhibit the tissue renin-angiotensin system.
Drug Characteristics: Fosinopril
Dose Adjustment Hepatic Not required Absorption F = 36%, food decreases rate (not extent) of absorption
Dose Adjustment Renal Moderate to severe renal dysfunction, initiate therapy at 5 mg po daily Distribution 99% protein bound
Dialyzable Poorly dialyzed, no supplemental dosing required Metabolism Metabolized in liver to active metabolite (fosinoprilat) not via CYP450
Pregnancy Category C (1st trimester), D (2nd and 3rd trimesters) Elimination Renal 50% (fosinoprilat) with half-life of 12 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, history of ACEI-induced angioedema, and hereditary or idiopathic angioedema, concomitant use with aliskiren in patients with diabetes Black Box Warnings Pregnancy
Medication Safety Issues: Fosinopril
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No FLUoxetine, Fosamax, furosemide, lisinopril No
Class: Loop Diuretic
Dosage Forms. Oral Tablet: 20 mg, 40 mg, 80 mg; Oral Solution: 8 mg/1 mL, 10 mg/1 mL
Common FDA Label Indication, Dosing, and Titration.
Edema related to heart failure, renal failure: Premature neonates (<29 wk), 1-2 mg/kg/dose po daily, may titrate to 6 mg/kg/dose; Premature neonates (>29 wk), 1-2 mg/kg/dose po 1-2 times per d, may titrate to 6 mg/kg/dose; Neonates, 1-3 mg/kg po q8h as needed; Infants and Children, initial, 0.5-2 mg/kg/dose po, may titrate at 6-8 h intervals to maintenance dose (max 6 mg/kg/dose); Adults, initial 20-80 mg po daily, may titrate to maintenance dose (max 600 mg/d)
Hypertension: Adults, 40 mg po BID, may titrate to patient response
Off-Label Uses.
None
MOA. Furosemide is a loop diuretic that is actively secreted via the nonspecific organic acid transport system into the lumen of the thick ascending limb of Henle's loop, where it decreases sodium reabsorption by competing for the chloride site on the Na+-K+-2Cl- cotransporter.
Drug Characteristics: Furosemide
Dose Adjustment Hepatic Not required, patients with hepatic failure may need higher doses to achieve diuresis Absorption F = 47-70%, food may lower Cmax and Tmax
Dose Adjustment Renal Not required, patients with renal failure may need higher doses to achieve diuresis Distribution Protein binding 91-99%
Dialyzable Not dialyzable Metabolism Minimal hepatic metabolism (10%)
Pregnancy Category C Elimination Renal 60-90% (unchanged), fecal 7-9%, bile 6-8% with a half-life of 30-120 min
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to furosemide; anuria Black Box Warnings Fluid and electrolyte loss
Medication Safety Issues: Furosemide
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Lanoxin, Lidex, Lomotil, Lovenox, Luvox No
Class: Gamma Aminobutyric Acid, Anticonvulsant
Dosage Forms. Oral Capsule: 100 mg, 300 mg, 400 mg; Oral Tablet: 300 mg, 600 mg, 800 mg; Oral Solution: 250 mg/5 mL, 300 mg/5 mL; Oral Tablet, Extended Release: 300 mg, 600 mg
Common FDA Label Indication, Dosing, and Titration.
Partial seizure, adjunct: Immediate release, Adults and Children ≥12 y of age, initial, 300 mg po tid, may titrate to 1800 mg/d in 3 divided doses (max 2400-3600 mg/d); Children 3-11 y of age, initial, 10-15 mg/kg/d in 3 divided doses, maintenance (Children 3-4 y of age), may titrate over 3 d to 40 mg/kg/d in 3 divided doses, maintenance (Children 5-11 y of age), may titrate over 3 d to 25-35 mg/kg/d in 3 divided doses
Postherpetic neuralgia: Immediate release, Adults, 300 mg po on day 1, 300 mg bid on day 2, 300 mg tid on day 3, may titrate dose to 1800 mg/d in 3 divided doses; extended release, 300 mg on day 1, 600 mg on day 2, 900 mg days 3-6, 1200 mg days 7-10, 1500 mg days 11-14, and 1800 mg po daily thereafter
Off-Label Uses.
Diabetic peripheral neuropathy: Adults, 900-3600 mg/d po
Restless leg syndrome: 300 mg po 2 h prior to bedtime
Neuropathic pain: Immediate release, 300 mg po daily, may titrate to 3600 mg po daily
MOA. Gabapentin is a cyclohexane compound that is structurally related to GABA; its mechanism of action is not known. Gabapentin does not interact with GABA receptors or alter the formation, release, degradation, or reuptake of GABA.
Drug Characteristics: Gabapentin
Dose Adjustment Hepatic Not required Absorption F = 27-60%, food increases absorption
Dose Adjustment Renal CrCl ≥60 mL/min, 900-3600 mg/d in 3 divided doses; CrCl 30-59 mL/min, 400-1400 mg/d in 2 divided doses; CrCl 15-29 mL/min, 200-700 mg/d given once daily Distribution Vd = 58 L; <3% protein bound
Dialyzable Hemodialysis: 100-300 mg/d given once daily; give supplemental dose postdialysis Metabolism Not metabolized
Pregnancy Category C Elimination Renal 76-81% (unchanged), fecal 10-23% with a half-life of 5-7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Class: Antihyperlipidemic
Dosage Forms. Oral Tablet: 600 mg
Common FDA Label Indication, Dosing, and Titration.
Coronary arteriosclerosis; prophylaxis-familial combined hyperlipidemia: 600 mg po bid
Familial type V hyperlipoproteinemia-Fredrickson type IV hyperlipoproteinemia: 600 mg po bid
Off-Label Uses.
None
MOA. Fibric acid derivatives activate PPARα, which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). Activation of PPARα also induces an increase in the synthesis of apoproteins A-I and A-II and HDL-cholesterol.
Drug Characteristics: Gemfibrozil
Dose Adjustment Hepatic Avoid in severe liver impairment Absorption Well absorbed, food reduces absorption, take on empty stomach
Dose Adjustment Renal CrCl 10-50 mL/min, administer 75% of the dose; CrCl <10 mL/min, reduce dose by 50% Distribution Vd = 60 L; 99% protein bound
Dialyzable Unknown Metabolism <20% hepatic, CYP3A4/5 substrate. Inhibitor of CYP1A2 (moderate), CYP2C19 (strong), CYP2C8 (strong), CYP2C9 (strong)
Pregnancy Category C Elimination Renal 70% with a half-life of 2 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to gemfibrozil, concurrent repaglinide or simvastatin, gallbladder disease, severe renal or hepatic dysfunction Black Box Warnings None
Medication Safety Issues: Gemfibrozil
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Levbid, Lipitor, Lodine No
Class: Vaccine, Inactivated, Bacterial
Dosage Forms. Lyophilized Powder for Intramuscular Injection: 10 mcg/0.5 mL (ActHIB and Hiberix); Suspension for Injection: 7.5 mcg/0.5 mL (PedvaxHIB); also available in combination with other pediatric vaccines
Common FDA Label Indication, Dosing, and Titration.
Prevention of invasive H. influenzae type B infection, Children: Dose schedule depends on product and timing of start of vaccination series. For ActHIB, doses at 2, 4, 6, and 12-15 mo of age as primary series. If PedvaxHIB used, doses at 2, 4, and 12-15 mo are used. If dosing begins later than 2 mo of age, adjusted dosing schedule used and number of doses changes. Hiberix can be used only for the last dose for Children 12 mo to 4 y of age
Off-Label Uses.
Prevention of invasive H. influenzae type B infection, Adults: 1 dose. May use any of the Hib conjugate vaccines for unvaccinated or partially vaccinated persons ≥5 y of age who have leukemia, malignant neoplasms, anatomic or functional asplenia (including sickle cell disease), HIV infection, or other immunocompromising conditions
Drug Characteristics: H. influenzae Type B Vaccine
Pregnancy Category Inactivated vaccines have not been shown to increase fetal risk ADME None known
Lactation Unlikely to be used in lactating woman; vaccines generally considered safe during lactation Pharmacogenetics None known
Contraindications Hypersensitivity to Hib vaccine or a component of the vaccine Black Box Warnings None
Medication Safety Issues: H. influenzae Type B Vaccine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No HepB, HPV No
Class: Vaccine, Inactivated, Viral
Dosage Forms. Intramuscular Suspension: Havrix, 720 ELISA units/0.5 mL, 1440 ELISA units/mL; Vaqta 25 units/0.5 mL, 50 units/1 mL; also available in combination with hepatitis B vaccine
Common FDA Label Indication, Dosing, and Titration.
Hepatitis A prophylaxis: Adults, Havrix 1440 ELISA units IM once, with a 2nd dose 6-12 mo later, or Vaqta 50 units IM once, with a 2nd dose 6-18 mo later; Children 12 mo to 18 y, Havrix 720 ELISA units IM once, with a 2nd dose 6-12 mo later, or Vaqta 25 units IM once, with a booster dose 6-18 mo later
Off-Label Uses.
Hepatitis A postexposure prophylaxis for individuals 1-40 y of age: Same regimen as for preexposure prophylaxis; vaccine series should be started within 2 wk of exposure
Drug Characteristics: Hepatitis A Vaccine
Pregnancy Category Inactivated vaccines have not been shown to increase fetal risk ADME None known
Lactation Infant risk is minimal Pharmacogenetics None known
Contraindications Hypersensitivity to hepatitis A vaccine or a component of the vaccine (neomycin) Black Box Warnings None
Medication Safety Issues: Hepatitis A Vaccine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No HepB, HPV4 No
Drug Interactions: Hepatitis A Vaccine
Typical Agents Mechanism Clinical Management
Moderate- to high-dose corticosteroids Steroids induce immunosuppression, potentially reducing efficacy of vaccine Consider delay of vaccination until corticosteroid therapy has been discontinued if possible
Immunosuppressing agents Immunosuppression, potentially reducing efficacy of vaccine Consider delay of vaccination until immunosuppressive therapy has been discontinued if possible
Class: Thiazide Diuretic, Antihypertensive
Dosage Forms. Oral Capsule: 12.5 mg; Oral Tablet: 12.5 mg, 25 mg, 50 mg
Common FDA Label Indication, Dosing, and Titration.
Edema; adjunct: Adults, 25-100 mg po daily in single or divided doses; Children, 1-2 mg/kg po daily in single or divided doses; Infants <6 mo of age may require doses up to 3 mg/kg po daily in 2 divided doses; Infants <2 y of age, max dose 37.5 mg/d; Children 2-12 y of age, max dose 100 mg/d
Hypertension: Adult, initial, 12.5-25 mg po daily, may titrate to 50 mg po daily in single or divided doses; Children, 1-2 mg/kg po daily in single or divided doses; Infants <6 mo of age may require doses up to 3 mg/kg po daily in 2 divided doses, max dose 37.5 mg/d; Infants <2 y of age, max dose 37.5 mg/d; Children 2-12 y of age, max dose 100 mg/d
Off-Label Uses.
Hypercalciuria: Adults, 25 mg po bid; Children, 1-2 mg/kg/d po
MOA. Thiazides increase sodium and chloride excretion by interfering with their reabsorption in the cortical diluting segment of the nephron.
Drug Characteristics: Hydrochlorothiazide
Dose Adjustment Hepatic Not required Absorption F = 60-80%, reduced in patients with hepatic, renal, or cardiac (heart failure) disease
Dose Adjustment Renal CrCl <10 mL/min, avoid Distribution Vd = 3.6-7.8 L/kg; 40% protein bound
Dialyzable Not dialyzable Metabolism Not metabolized
Pregnancy Category B Elimination Renal 50-70% (unchanged) with a half-life of 10-12 h (prolonged in patients with heart failure or renal disease)
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to hydrochlorothiazide or sulfonamide, concomitant dofetilide therapy, or anuric patients Black Box Warnings None
Medication Safety Issues: Hydrochlorothiazide
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No
HCTZ is an error-prone abbreviation
Maxide, Micronase
No
Class: Opioid Analgesic. C-II
Dosage Forms. Oral Tablet (With Acetaminophen): (Hydrocodone/Acetaminophen) 2.5 mg/325 mg, 5 mg/325 mg, 7.5 mg/325 mg, 10 mg/325 mg; Oral Elixir, Oral Solution (With Acetaminophen): (Hydrocodone/Acetaminophen) 7.5 mg/325 mg/15 mL, 10 mg/325 mg/15 mL; Oral Tablet, Extended Release (24 h), Abuse-Deterrent: 20 mg, 30 mg, 40 mg, 60 mg, 80 mg, 100 mg, 120 mg; Oral Capsule, Extended Release (12 h), Abuse-Deterrent: 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 50 mg
Common FDA Label Indication, Dosing, and Titration.
Pain, severe enough to require daily around-the-clock opioid: Adults, 10 mg q12h initially, may titrate to response
Off-Label Uses.
None
MOA. Hydrocodone is an opioid analgesic and antitussive with unknown mechanism of action, but it is thought to be related to the presence of opiate receptors in the CNS.
Drug Characteristics: Hydrocodone
Dose Adjustment Hepatic Severe: Start with 10 mg dose Absorption Well absorbed, minimal food effect
Dose Adjustment Renal Severe: Start with 10 mg dose Distribution Unknown
Dialyzable Not dialyzable Metabolism Prodrug activated to hydromorphone by CYP2D6, deactivated by CYP3A4/5
Pregnancy Category Avoid if possible, risk of neonatal abstinence syndrome Elimination Renal 26% with a half-life of 8 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, paralytic ileus, respiratory depression, severe asthma Black Box Warnings Addiction, abuse, misuse, REMS, respiratory depression, accidental ingestion, neonatal opioid withdrawal, alcohol, CYP3A4/5 interactions, hepatotoxicity, concurrent use with benzodiazepines
Medication Safety Issues: Hydrocodone
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
HD, HP, Plus, ESHYDROcodoneNoYesHYDROmorphone, oxyCODONEAvoid in certain
Class: Antihistamine
Dosage Forms. Oral Tablet: 10 mg, 25 mg, 50 mg; Oral Capsule: 25 mg, 50 mg, 100 mg; Oral Syrup: 10 mg/5 mL; Oral Solution: 10 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Anxiety: 50-100 mg po qid
Pruritus: 25 mg po tid-qid
Sedation: 50-100 mg po q4h prn
Off-Label Uses.
Seasonal allergic rhinitis: 10-25 mg po tid-qid
MOA. Hydroxyzine hydrochloride is a rapid-acting agent with probable action of suppressing activity in key locations of the CNS's subcortical area. Primary skeletal muscle relaxation, bronchodilator activity, antiemetic effects, and antihistaminic and analgesic effects have been demonstrated experimentally and confirmed clinically.
Drug Characteristics: Hydroxyzine
Dose Adjustment Hepatic Patients with chronic liver failure receive a lower dose; administer the lowest effective dose once daily only and increase carefully to avoid toxicity Absorption Rapidly absorbed after oral administration
Dose Adjustment Renal Not required Distribution Vd = 16 L/kg
Dialyzable Not dialyzable Metabolism Metabolized to cetirizine in the liver
Pregnancy Category Use alternative agents Elimination Renal 70% with a half-life of 3-20 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to cetirizine or hydroxyzine Black Box Warnings None
Medication Safety Issues: Hydroxyzine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No HydrOXYzine No No HydrALAZINE, hydroxyurea Highly anticholinergic; a
Class: NSAID
Dosage Forms. Oral Tablet: 100 mg, 200 mg, 400 mg, 600 mg, 800 mg; Oral Suspension: 100 mg/5 mL, 50 mg/1.25 mL; Oral Capsule: 200 mg; Oral Tablet, Chewable: 100 mg
Common FDA Label Indication, Dosing, and Titration.
Fever: Children 6 mo to 12 y of age, 5-10 mg/kg po q6-8h prn; Children ≥12 y of age and Adults, 200-400 mg po q4-6h prn, max 1200 mg/d for OTC use
Pain, headache: Children 6 mo to 12 y of age, 5-10 mg/kg po q6-8h prn; Children ≥12 y of age and Adults, 200-400 mg po q4-6h prn, max 1200 mg/d for OTC use
Osteoarthritis or rheumatoid arthritis: 1200-3200 mg/d po in 3-4 divided doses
Juvenile rheumatoid arthritis: 30-50 mg/kg/d divided qid, max 2400 mg/d
Off-Label Uses.
None
MOA. Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2), and reversibly alters platelet function and prolongs bleeding time.
Drug Characteristics: Ibuprofen
Dose Adjustment Hepatic Not required Absorption F = 90%, minimal food effect
Dose Adjustment Renal Severe renal dysfunction, avoid Distribution Vd = 0.1 L/kg; 99% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP2C19 substrate
Pregnancy Category C (1st and 2nd trimesters); D (3rd trimester) Elimination Renal 45-80% with a half-life of 1.8-2.2 h
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity to ibuprofen; concurrent use with ketorolac or pentoxifylline; asthma, urticaria, or allergic-type reaction following aspirin or other NSAID administration; CABG surgery, treatment of perioperative pain Black Box Warnings Cardiovascular events, GI toxicity, CABG
Medication Safety Issues: Ibuprofen
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
Junior, Migraine, 200, Prin No No No Halfprin, Neurontin Avoid chronic use
Class: NSAID
Dosage Forms. Oral Capsule, Immediate Release: 20 mg, 25 mg, 40 mg, 50 mg; Oral Capsule, Extended Release: 75 mg; Oral Suspension: 25 mg/5 mL; Rectal Suppository: 50 mg
Common FDA Label Indication, Dosing, and Titration.
Ankylosing spondylitis, osteoarthritis, rheumatoid arthritis: Immediate release, 25-50 mg po bid-tid, max 200 mg/d; extended release, 75 mg po daily bid
Acute pain (mild to moderate): Immediate release (Tivorbex), 20 mg po tid or 40 mg po bid-tid
Off-Label Uses.
Preterm labor, prevention: 25 mg po q6-12h
Acute gout exacerbation: 50 mg po (or pr) tid
MOA. Nonselective inhibitor of COX-1 and COX-2, and reversibly alters platelet function and prolongs bleeding time.
Drug Characteristics: Indomethacin
Dose Adjustment Hepatic Severe hepatic failure, use with caution Absorption F = 90%, no food effect
Dose Adjustment Renal CrCl <15 mL/min, use with caution Distribution Vd = 0.34-1.57 L/kg; 99% protein bound
Dialyzable Not dialyzable Metabolism 40% hepatic
Pregnancy Category C (<30 wk gestation), C/D (≥30 wk gestation, depending on product) Elimination Renal 60% with a half-life of 4.5 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity, concurrent use with ketorolac or pentoxifylline; asthma, urticaria, or allergic-type reaction following aspirin or other NSAID administration; CABG surgery, treatment of perioperative pain Black Box Warnings Cardiovascular events, GI toxicity, CABG
Medication Safety Issues: Indomethacin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No ER capsule No Imodium, Lincocin, Minocin, Vicodin Avoid
Class: Vaccine, Inactivated, Viral
Dosage Forms. Suspension for Intramuscular Injection: 0.5 mL vial (depending on annual decisions about composition, may be available as trivalent or quadrivalent product containing 3-4 strains of influenza A and B virus; high-dose formulations contain 60 mcg/0.5 mL of each vaccine antigen compared to 15 mcg/0.5 mL in the standard dose formulation); Suspension for Intradermal Injection: 0.1 mL in prefilled intradermal injection system
Common FDA Label Indication, Dosing, and Titration.
Prevention of influenza infection: Children 6 mo to 8 y of age who have not been vaccinated in the past, 2 doses separated by at least 4 wk during the 1st season they receive influenza vaccine; Children ≥6 mo of age and Adults ≤64 y of age, 1 dose of standard-dose formulation annually prior to or during influenza season; Adults >64 y of age, 1 dose of high-dose formulation annually prior to or during influenza season
Off-Label Uses.
None
Drug Characteristics: Influenza Virus Vaccine
Pregnancy Category C ADME None known
Lactation Infant risk is minimal Pharmacogenetics None known
Contraindications Hypersensitivity to influenza vaccine, egg protein or a component of the vaccine; some formulations may contain: gentamicin, kanamycin, neomycin, polymyxin, polysorbate 80, thimerosal; asthma, chronic medical conditions, immunosuppression Black Box Warnings None
Medication Safety Issues: Influenza Virus Vaccine
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
Quadrivalent, High-Dose, Intradermal No No No Flumazenil; vials and syringes often mistaken for tetanus toxoid, tuberculin skin test or insulin No
Class: Insulin
Dosage Forms. Injection Solution: 100 units/mL, 500 units/mL; Pen and Refills (Administration Device), Product Dependent: 100 units/mL, 200 units/mL, 300 units/mL; Powder for Inhalation: 4 units, 8 units, 12 units
Common FDA Label Indication, Dosing, and Titration.
Diabetes mellitus, Type 1 and 2: Subcutaneous dosing is individualized to patient needs
Off-Label Uses.
None
MOA. Insulin promotes cellular uptake of glucose, fatty acids, and amino acids, and their conversion to glycogen, triglycerides, and proteins.
Drug Characteristics: Insulin
Dose Adjustment Hepatic Not required Absorption See table in Clinical Pearls
Dose Adjustment Renal Not required Distribution Protein binding 5%
Dialyzable Not dialyzable Metabolism 50% hepatic, 30% renal, 20% adipose tissue
Pregnancy Category Product-dependent, but often used in pregnancy Elimination Renal 30% with a half-life of 1-5 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings Risk of acute bronchospasm with inhaled formulation
Medication Safety Issues: Insulin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
R = Regular, N = NPH, 70/30 = 70% NPH/30% R, U-500 (high concentration) HumuLIN, NovoLIN No Yes HumaLOG, HumuLIN, NovoLIN, NovoLOG Avoid sliding scale without concurrent basal or long-acting insulin
Drug Interactions: Insulin
Typical Agents Mechanism Clinical Management
Beta-blockers Altered glucose metabolism and increased risk of hypoglycemia Avoid propranolol; use others with caution and increased monitoring
Fluoroquinolones Altered glucose metabolism and increased risk of hypoglycemia and hyperglycemia Monitor and consider dose adjustments
MAOIs Stimulation of insulin secretion, hypoglycemic effects Monitor and consider dose adjustments
Somatostatin analogues Altered glucose metabolism and increased risk of hypoglycemia Monitor and consider dose adjustments
Psyllium Psyllium may delay absorption of glucose from meals, leading to less postprandial hyperglycemia and potentially allowing a reduced dosage of the antidiabetic agent
Class: Anticholinergic/Selective β2-Agonist Combination
Dosage Forms. Inhalation Solution: (Ipratropium/Albuterol) 0.5 mg/2.5 mg/3 mL; Spray for Oral Inhalation: (Ipratropium/Albuterol) 20 mcg/100 mcg/inhalation
Common FDA Label Indication, Dosing, and Titration.
Chronic obstructive pulmonary disease: Adults, 1 inhalation qid (max 6 inhalations/d) or 3 mL via nebulizer q6h (max 6 doses/d)
Off-Label Uses.
Asthma exacerbation: Adults, ipratropium 0.5 mg with albuterol 2.5 mg via nebulizer every 20 min × 3 doses, then prn
MOA. Albuterol is a selective β2-adrenergic agonist that produces bronchodilation, vasodilation, uterine relaxation, skeletal muscle stimulation, peripheral vasodilation, and tachycardia. Ipratropium is a competitive antagonist of acetylcholine at peripheral, but not central, muscarinic receptors. It appears to produce bronchodilation by inhibition of cholinergic receptors on bronchial smooth muscle.
Drug Characteristics: Ipratropium/Albuterol
Dose Adjustment Hepatic Not required Absorption F = 6.9% following inhalation; 90% of an inhaled dose is swallowed
Dose Adjustment Renal Not required Distribution Albuterol protein binding 10%
Dialyzable Not dialyzable Metabolism Albuterol is conjugated to an active metabolite; ipratropium is partially metabolized to 8 inactive metabolites
Pregnancy Category C Elimination Albuterol, renal 80-100% with a half-life of 4 h; Ipratropium, minimal renal, fecal 48% with a half-life of 2 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to albuterol, ipratropium, or any other components of the product, or to atropine or its derivatives, or levalbuterol; hypersensitivity to soya lecithin or related food products (eg, soybean, peanut products)
Class: Long-Acting Nitrate, Anti-Anginal
Dosage Forms. Oral Tablet, Extended Release: 30 mg, 60 mg, 120 mg; Oral Tablet, Immediate Release: 10 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Angina, prophylaxis: Adults, extended release, initial, 30-60 mg po daily, may titrate to maintenance of 120-240 mg po daily; immediate release, 20 mg po bid separated 7 h apart to decrease tolerance development
Off-Label Uses.
None
MOA. Isosorbide mononitrate (ISMN) is the active 5-mononitrate metabolite of isosorbide dinitrate. Nitroglycerin and other organic nitrates are converted to nitric oxide (NO) by vascular endothelium. NO activates guanylate cyclase, increasing cyclic GMP that in turn decreases intracellular calcium, resulting in direct relaxation of vascular smooth muscle.
Drug Characteristics: Isosorbide Mononitrate
Dose Adjustment Hepatic Not required Absorption F = 93%, food slows rate (but not extent) of absorption
Dose Adjustment Renal Not required Distribution Vd = 0.6L; <5% protein bound
Dialyzable Yes (hemodialysis) Metabolism >95% hepatic, CYP3A4/5 substrate
Pregnancy Category B Elimination Renal 96% (metabolites) with a half-life of 6 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to nitrates, concurrent use with PDEIs, concurrent use with riociguat Black Box Warnings None
Medication Safety Issues: Isosorbide Mononitrate
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
NoNoXR formulationNoImuran, Inderal LA, K-DurN
Class:Phenyltriazine Anticonvulsant
Dosage Forms. Oral Chewable Tablet: 5 mg, 25 mg; Oral Tablet: 25 mg, 100 mg, 150 mg, 200 mg; Oral Tablet, Extended Release: 25 mg, 50 mg, 100 mg, 200 mg, 250 mg, 300 mg; Oral Dispersible Tablet: 25 mg, 50 mg, 100 mg, 200 mg
Common FDA Label Indication, Dosing, and Titration.
Bipolar I disorder: Adults 25 mg daily × 2 wk, then 50 mg po daily × 2 wk, then 100 mg po daily × 1 wk, then 200 mg po daily; may titrate to 400 mg po daily; regimens containing valproic acid, 25 mg po qod × 2 wk, then 25 mg po daily × 2 wk, then 50 mg po daily × 1 wk, then 100 mg po daily; regimens without valproic acid but containing carbamazepine, phenytoin, phenobarbital, primidone, rifampin, lopinavir/ritonavir: 50 mg po daily × 2 wk, then 50 mg po bid × 2 wk, then 100 mg po bid × 1 wk, then 300 mg/d po in divided doses × 1 wk, then 400 mg/d po in 2 divided doses.
Partial seizure, adjunct or monotherapy, tonic-clonic seizure, Lennox-Gastaut syndrome, adjunctive: Adults and Children ≥12 y of age, immediate release, 100-500 mg/d po in 2 divided doses, extended release, 200-600 mg po daily; Children 2-12 y of age: immediate release, 1-15 mg/kg/d po in 1 or 2 divided doses, max 400 mg/d; dose initiation for combination regimens as noted above; dose titration required
Off-Label Uses.
None
MOA. Lamotrigine is a phenyltriazine derivative unrelated to other marketed antiepileptic drugs (AEDs). Lamotrigine inhibits voltage-dependent sodium channels, thereby stabilizing neuronal membranes and reducing the release of excitatory neurotransmitters such as glutamate and aspartate.
Drug Characteristics: Lamotrigine
Dose Adjustment Hepatic Moderate-severe without ascites, reduce dose by 25%; severe with ascites, reduce dose by 50% Absorption F = 98%, no effect of food on absorption
Dose Adjustment Renal Not required Distribution Vd = 0.9-1.3 L; 55% protein bound
Dialyzable Yes (hemodialysis), 20% removed Metabolism 90% hepatic and occurs by glucuronidation
Pregnancy Category C Elimination Renal 94% with a half-life of 25-70 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings Serious skin reactions
Class: Proton Pump Inhibitor
Dosage Forms. Oral Capsule, Delayed Release: 15 mg, 30 mg; Oral Disintegrating Tablet: 15 mg, 30 mg
Common FDA Label Indication, Dosing, and Titration.
Duodenal ulcer disease: 15 mg po daily × up to 4 wk
Gastric ulcer disease, treatment: 30 mg po daily × up to 8 wk
Helicobacter pylori GI tract infection, triple therapy: 30 mg po bid × 10-14 d in combination with amoxicillin 1000 mg and clarithromycin 500 mg po bid
Erosive esophagitis, GERD, treatment: Children 1-11 y of age and ≤30 kg, 15 mg po daily × 12 wk; Children >30 kg, 30 mg po daily × 12 wk; Children ≥12 y of age and Adults 30 mg po daily × 8-16 wk
Zollinger-Ellison syndrome: 60 mg po bid up to 180 mg/d
Off-Label Uses.
Heartburn ≥2 d/wk: 15 mg po daily for up to 14 d (OTC labeling)
Drug-induced GI disturbance: 15 mg po daily
MOA. Lansoprazole is a proton pump inhibitor (PPI) that, when protonated in the secretory canaliculi of the parietal cells, covalently binds to H++/K+-ATPase (proton pump), which is the final pathway for acid secretion.
Drug Characteristics: Lansoprazole
Dose Adjustment Hepatic Severe liver dysfunction, maxdose 15 mg po daily Absorption
F = 80%, brief delay in reaching peak if taken with food, but no effect of food on overall absorption
Dose Adjustment Renal Not required Distribution Vd = 14-18 L; 97% protein bound
Dialyzable Not dialyzable Metabolism 70-75% hepatic, CYP2C19 and 3A4/5 substrate
Pregnancy Category Can be used when clinically indicated Elimination Renal 15-25% with a half-life of 90 min
Lactation Weigh risks and benefits Pharmacogenetics Caution with CYP2C19 poor metabolizers
Contraindications Hypersensitivity Black Box Warnings None
Class: Selective β2-Agonist, Bronchodilator
Dosage Forms. Metered-Dose Inhaler: 0.045 mg/actuation; Nebulization Solution: 0.31 mg/3 mL, 0.63 mg/3 mL, 1.25 mg/3 mL, 1.25 mg/0.5 mL
Common FDA Label Indication, Dosing, and Titration.
Asthma, bronchospasm: Adults and Children ≥4 y of age, MDI, 2 inhalations q4-6h prn (max 2 inhalations q4h); by nebulizer, 0.63 mg TID (max 1.25 mg TID)
Off-Label Uses.
Asthma, acute exacerbation: Children ≥4 y of age, MDI, 4-8 inhalations q20min × 3 doses, then q1-4h prn; Adults, MDI, 4-8 inhalations po q20min up to 4 h, then q1-4h prn; by nebulizer, 1.25-2.5 mg q20min × 3 doses, then q1-4h prn
MOA. Activation of β2-adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of cyclic-3', 5'-adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation. Levalbuterol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles.
Drug Characteristics: Levalbuterol
Dose Adjustment Hepatic Not required Absorption F = 30% after oral administration
Dose Adjustment Renal Not required Distribution After inhalation, Vd is ∼1900 L
Dialyzable Not dialyzable Metabolism Oral doses undergo rapid metabolism in the GI tract; hepatic metabolism of inhaled doses
Pregnancy Category Select an alternative agent Elimination Renal 80-100% with a half-life of 5-7 min
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Class: Anticonvulsant
Dosage Forms. Tablet: 250 mg, 500 mg, 750 mg, 1 g; Tablet, Extended Release: 500 mg, 750 mg; Oral Solution: 100 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Myoclonic seizure, adjunct: Children ≥12 y of age and Adults, initial, 500 mg po bid, titrate to target dose of 3000 mg/d
Partial seizure, adjunct: Children ≥16 y of age and Adults, immediate release, initial, 500 mg po bid, max 3000 mg/d; extended release, initial, 1000 mg po qd, max 3000 mg/d; Children 4-15 y of age, immediate release, initial, 10 mg/kg po bid, max 60 mg/kg/d; Children 6 mo to 3 y of age, initial 10 mg/kg po bid, max 50 mg/kg/d; Children 1-5 mo of age, 7 mg/kg po bid, max 42 mg/kg/d
Tonic-clonic seizure, primary generalized, adjunct: Children ≥16 y of age and Adults, initial, 500 mg po bid, titrate to target dose of 3000 mg/d; Children 6-15 y of age, initial, 10 mg/kg po bid, titrate to target dose of 60 mg/kg/d
Off-Label Uses.
None
MOA. Levetiracetam is a pyrrolidine derivative that is structurally unrelated to other AEDs. Its mechanism of action is unclear and does not relate to any known mechanisms of neuronal excitation or inhibition. The action of levetiracetam in animal models of seizures and epilepsy is unique from other AEDs.
Drug Characteristics: Levetiracetam
Dose Adjustment Hepatic Not required Absorption F = 100%; minor effect of food on absorption
Dose Adjustment Renal CrCl <30 mL/min, reduce dose by 67%; CrCl = 30-50 mL/min, reduce dose by 50% Distribution <10% protein bound
Dialyzable Yes, supplemental dose recommended Metabolism Minimal and via hydrolysis
Pregnancy Category C Elimination Renal 66% (unchanged), fecal 20-25% with a half-life of 6-8 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Class: Antihistamine
Dosage Forms. Oral Solution: 2.5 mg/5 mL; Oral Tablet: 5 mg
Common FDA Label Indication, Dosing, and Titration.
Idiopathic urticaria, perennial, or seasonal allergic rhinitis: Children 6 mo to 5 y of age, 1.25 mg po daily; Children 6-11 y of age, 2.5 mg po daily; Children ≥12 y of age and Adults, 5 mg po daily; doses should be given in the evening
Off-Label Uses.
None
MOA. Levocetirizine, an enantiomer of cetirizine, is a low-sedating, long-acting H1-receptor antagonist that is a metabolite of hydroxyzine. It competitively inhibits the interaction of histamine with H1 receptors, thereby preventing the allergic response.
Drug Characteristics: Levocetirizine
Dose Adjustment Hepatic Not required Absorption F = 85%, limited effect of food on absorption
Dose Adjustment Renal CrCl = 30-50 mL/min, 2.5 mg po qod; CrCl = 10-29 mL/min, 2.5 mg po twice per wk; CrCl <10 mL/min, avoid Distribution Vd = 0.4 L/kg with 95% protein binding
Dialyzable Not dialyzable Metabolism Hepatic metabolism, <14%
Pregnancy Category Weigh risks and benefits Elimination Renal 85% (80% unchanged) with a half-life of 7-8 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to cetirizine, levocetirizine, hydroxyzine, patients with CrCl <10 mL/min, children <12 y with any renal impairment, any patient on hemodialysis Black Box Warnings None
Medication Safety Issues: Levocetirizine
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Cetirizine Beers Criteria No
Class: Fluoroquinolone Antibiotic
Dosage Forms. Oral Solution: 25 mg/mL; Oral Tablet: 250 mg, 500 mg, 750 mg
Common FDA Label Indication, Dosing, and Titration.
Bacterial prostatitis, chronic: 500 mg po daily × 28 d
Bacterial sinusitis, acute: 750 mg po daily × 5 d
Bronchitis, chronic, acute bacterial exacerbation: 500 mg po daily × 7 d
Community-acquired pneumonia: 500 mg po daily × 7-14 d, or 750 mg po daily × 5 d
Infection of skin and/or subcutaneous tissue (uncomplicated): 500 mg po daily × 7-14 d
Pyelonephritis, acute: 250 mg po daily × 10 d
Off-Label Uses.
Chlamydial infection: 500 mg po daily × 7 d
Traveler's diarrhea: 500 mg po daily × 1-3 d
MOA. Levofloxacin is a fluoroquinolone that inhibits bacterial DNA gyrase, an enzyme responsible for the unwinding of DNA for transcription and subsequent supercoiling of DNA for packaging into chromosomal subunits. It is highly active against aerobic, gram-negative bacilli.
Drug Characteristics: Levofloxacin
Dose Adjustment Hepatic Not required Absorption F = 99%, no food effect, take without regard to meals
Dose Adjustment Renal CrCl 20-50 mL/min, reduce dose by 50%; CrCl 5-19 mL/min, extend dosing interval to 48 h Distribution Bile, blister, CSF, gynecologic tissues, lung, prostate, synovial fluid, sputum, tonsils
Dialyzable Not dialyzable Metabolism Not metabolized
Pregnancy Category C Elimination Renal 87% with a half-life of 6-8 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to levofloxacin or other quinolones; concomitant tizanidine administration Black Box Warnings Myasthenia gravis, tendon inflammation and rupture, peripheral neuropathy, CNS effects, cardiac, dermatologic and hypersensitivity reactions, aortic dissections and ruptures
Medication Safety Issues: Levofloxacin
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names LevETIRAcetam Beers Criteria No
Class: Thyroid Supplement
Dosage Forms. Oral Tablet: 25 mcg, 50 mcg, 75 mcg, 88 mcg, 100 mcg, 112 mcg, 125 mcg, 137 mcg, 150 mcg, 175 mcg, 200 mcg, 300 mcg; Oral Capsule: 13 mcg, 25 mcg, 50 mcg, 75 mcg, 88 mcg, 100 mcg, 112 mcg, 125 mcg, 137 mcg, 150 mcg, 175 mcg, 200 mcg
Common FDA Label Indication, Dosing, and Titration.
Hypothyroidism: Oral, maintenance, individualized based on clinical response and serum TSH levels; Adults, 25-300 mcg po daily; Infants 0-3 mo of age, 10-15 mcg/kg/d po daily; Infants 3-6 mo of age, 8-10 mcg/kg/d po daily; Infants 6-12 mo of age, 6-8 mcg/kg/d po daily; Children 1-5 y of age, 5-6 mcg/kg/d po daily; Children 6-12 y of age, 4-5 mcg/kg/d po daily; Children ≥12 y of age, growth and puberty incomplete, 2-3 mcg/kg/d po daily; Children ≥12 y of age, growth and puberty complete, 1.6 mcg/kg/d
Thyroid-stimulating hormone suppression, pituitary: Thyroid cancer, doses >2 mcg/kg/d po are usually required to suppress TSH <0.1 milliunits/L
Off-Label Uses.
Toxicity due to radiotherapy: use same age-based dosing as hypothyroidism
MOA. Levothyroxine sodium is a synthetic thyroid hormone. The endogenous thyroid hormones, T3 and T4, diffuse into the cell nucleus and bind to thyroid receptor proteins attached to DNA. This hormone nuclear receptor complex activates gene transcription and synthesis of messenger RNA and cytoplasmic proteins.
Drug Characteristics: Levothyroxine
Dose Adjustment Hepatic Not required Absorption F = 40-80%, increases with fasting
Dose Adjustment Renal Not required Distribution Vd = 8.7-9.7 L; >99% protein bound
Dialyzable Not dialyzable Metabolism Approximately 80% of levothyroxine sodium is deiodinated into T3 in the liver, kidney, and other tissues. It can also be metabolized by conjugation with glucuronides and sulfates and then enter into enterohepatic recirculation
Pregnancy Category Treatment of choice for hypothyroidism during pregnancy Elimination
Renal 50% with a half-life of 7 d
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity, nontoxic diffuse goiter or nodular thyroid disease, thyrotoxicosis, acute MI, treatment of obesity or weight loss, uncorrected adrenal insufficiency; may precipitate acute adrenal crisis Black Box Warnings Not for weight reduction
Class: Glucagon-Like Peptide-1-Receptor Agonist
Dosage Forms. Solution, Pen Injector: 18 mg/3 mL
Common FDA Label Indication, Dosing, and Titration.
Diabetes, Type 2: 0.6 mg sq once daily for 1 wk, then increase to 1.2 mg sq once daily (max 1.8 mg sq once daily)
Chronic weight management: 0.6 mg sq once daily for 1 wk, then increase by 0.6 mg weekly to target of 3 mg sq once daily (if patient cannot tolerate dose escalation, consider extending escalation period by 1 additional wk, but 3 mg dose cannot be tolerated, discontinue as effectiveness has not been established at doses <3 mg/d); discontinue if ≥4% of body weight loss not achieved after 16 wk of treatment
Off-Label Uses.
None
MOA. Analog of glucagon-like peptide-1, which increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, slows gastric emptying, and increases satiety.
Drug Characteristics: Liraglutide
Dose Adjustment Hepatic None Absorption F = 55%
Dose Adjustment Renal Use with caution when initiating treatment in patients with renal dysfunction Distribution Vd = 13L, protein binding >98%
Dialyzable Unknown Metabolism Metabolized by dipeptidyl peptidase IV
Pregnancy Category Select another agent Elimination Renal 6%, fecal 5% with a half-life of 13 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, multiple endocrine neoplasia syndrome type 2, history or family history of medullary thyroid carcinoma Black Box Warnings Increased risk of thyroid cancer
Class: Amphetamine, CNS Stimulant. C-II
Dosage Forms. Oral Capsule: 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg, 70 mg; Oral Tablet, Chewable: 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg
Common FDA Label Indication, Dosing, and Titration.
Attention-deficit hyperactivity disorder (ADHD): 30 mg po daily in the morning, may titrate in 10-20 mg/d increments at weekly intervals to max dose of 70 mg po daily; discontinue if improvement not observed after 1 mo of dosage titration
Binge eating disorder (moderate to severe): 30 mg po daily in the morning, may titrate weekly in 20 mg increments to 50-70 mg po daily
Off-Label Uses.
None
MOA. Lisdexamfetamine is a prodrug converted to dextroamphetamine. The mechanism of action of dextroamphetamine in the treatment of ADHD is unknown. Amphetamines cause the release of dopamine and norepinephrine at presynaptic nerve terminals and may block the reuptake of norepinephrine and dopamine by competitive inhibition.
Drug Characteristics: Lisdexamfetamine
Dose Adjustment Hepatic Not required Absorption F = 100%, food has no effect on absorption
Dose Adjustment Renal GFR 15-30 mL/min/1.73 m2, max dose 50 mg/d; GFR <15 mL/min/1.73 m2 or ESRD, max dose 30 mg/d; Distribution Vd = 3.5-4.6 L/kg; 60% protein bound
Dialyzable Not dialyzable Metabolism Extensive metabolism in the blood by hydrolytic activity of red blood cells to dextroamphetamine and L-lysine
Pregnancy Category Avoid Elimination Renal 96%, fecal 0.3% with a half-life of <1 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity/idiosyncrasy to sympathomimetic amines; MAOIs; symptomatic cardiovascular disease or advanced arteriosclerosis; moderate-severe hypertension; hyperthyroidism; glaucoma; agitated states; history of drug dependence Black Box Warnings
Risk of abuse, misuse, diversion
Class: ACE-I, Antihypertensive
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg, 20 mg, 30 mg, 40 mg; Solution Oral: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Acute myocardial infarction: 5-10 mg po daily × 6 wk
Heart failure: 2.5-5 mg po daily, may titrate in 10 mg increments to 40 mg/d
Hypertension: Children 6-16 y of age, 0.07 mg/kg (max 5 mg/d) po daily, may titrate to 0.61 mg/kg/d (max 40 mg/d); Adults, 10 mg po daily, may titrate by doubling dose to 40 mg/d
Off-Label Uses.
None
MOA. Lisinopril is a competitive ACE-I. It also reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, and can alter prostanoid metabolism, inhibit the sympathetic nervous system, and inhibit the tissue renin-angiotensin system.
Drug Characteristics: Lisinopril
Dose Adjustment Hepatic Not required Absorption F = 25% (F = 16% in heart failure), no effect of food on absorption
Dose Adjustment Renal CrCl 10-30 mL/min: initial dose is 2.5 mg/d; CrCl <10 mL/min: initial dose is 2.5 mg/d; dialysis patients: initial dose is 2.5 mg/d, supplemental dose equivalent to 20% of daily dose after hemodialysis Distribution 25% protein bound
Dialyzable Yes (hemodialysis and peritoneal) Metabolism Not metabolized
Pregnancy Category Discontinue when pregnancy is noted Elimination Renal 50-70% with a half-life of 12 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to lisinopril or other ACE-Is, history of ACE-I-induced angioedema, and hereditary or idiopathic angioedema, concurrent use with aliskiren in diabetic patients, concurrent use with sacubitril Black Box Warnings Pregnancy
Class: Antimanic
Dosage Forms. Oral Capsule: 150 mg, 300 mg, 600 mg; Oral Tablet: 300 mg; Oral Tablet, Extended Release: 300 mg, 450 mg; Oral Solution: 300 mg/5 mL (as a citrate)
Common FDA Label Indication, Dosing, and Titration.
Bipolar disorder, maintenance therapy: Adults and Children >12 y of age, extended release, 900-1800 mg/d po in 2-3 divided doses; immediate release, initial 300 mg po daily, may titrate to 900-1800 mg po in 3-4 divided doses
Bipolar disorder, manic episode: Adults and Children >12 y of age, extended release, 1800 mg/d po in 2-3 divided doses; immediate release, 600 mg po tid
Off-Label Uses.
Depression: Adults and Children >12 y of age, extended release, 600-1200 mg/d po in 2-3 divided doses; immediate release, initial dose 300 mg po daily or bid, may titrate to 300 mg po bid-qid
MOA. Lithium's mechanism of antimanic effect is unknown; it alters the actions of several second-messenger systems (eg, adenylate cyclase and phosphoinositol). Alters cation transport across cell membrane in nerve and muscle cells and influences reuptake of serotonin and/or norepinephrine; second-messenger systems involving the phosphatidylinositol cycle are inhibited.
Drug Characteristics: Lithium
Dose Adjustment Hepatic Not required Absorption F = 90-100%, food has no effect on absorption
Dose Adjustment Renal CrCl 30-89 mL/min, initiate with low dose and titrate upward slowly with frequent monitoring; CrCl <30 mL/min, avoid use Distribution Vd = 1.4 L/kg, no protein binding
Dialyzable Yes, a maintenance dose should be given following hemodialysis Metabolism
Not metabolized
Pregnancy Category Avoid Elimination Renal 89-98%, fecal <1% with a half-life of 14-24 h (up to 2.43 d after long-term therapy)
Lactation Avoid Pharmacogenetics None known
ContraindicationsSevere debilitation, dehydration, or sodium depletion; significant cardiovascular disease; significant renal impairment; concomitant diuretic therapy Black Box Warnings Lithium levels required
Class: Angiotensin II Receptor Antagonist, Antihypertensive
Dosage Forms. Oral Tablet: 25 mg, 50 mg, 100 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertension: Adults, initial 50 mg po daily, may titrate to 100 mg po daily in divided doses; Children ≥6 y of age, 0.7 mg/kg po daily, max 50 mg po daily
Reduce risk of cerebrovascular accident, in hypertensive patients with left ventricular hypertrophy; prophylaxis, diabetic nephropathy: Initial, 50 mg po daily, may titrate to 100 mg po daily based on BP
Diabetic nephropathy: Initial, 50 mg daily, may titrate based on BP up to 100 mg po daily
Off-Label Uses.
Heart failure: Initial, 25 mg po daily, maintenance 50 mg po daily
Cardiovascular event risk, reduction: Adults, 50-100 mg po daily
Isolated systolic hypertension, left ventricular hypertension, nondiabetic kidney disease: 50 mg po daily
MOA. Losartan is a selective, reversible, competitive antagonist of the angiotensin II receptor (AT1), which is responsible for the physiologic effects of angiotensin II including vasoconstriction, aldosterone secretion, sympathetic outflow, and stimulation of renal sodium reabsorption.
Drug Characteristics: Losartan
Dose Adjustment Hepatic Starting dose, 25 mg po daily Absorption F = 33%, food slows absorption and decreases Cmax by 10%
Dose Adjustment Renal Not required Distribution Vd = 34 L; 99% protein bound
Dialyzable Not dialyzable Metabolism 14% hepatic, CYP2C9 and CYP3A4/5 substrate
Pregnancy Category Discontinue when pregnancy noted Elimination Renal 35%, fecal 60% with a half-life 2 h (6-9 h for active metabolite, 5-carboxylic acid)
Lactation Not recommended Pharmacogenetics None known
Contraindications Hypersensitivity to losartan or other angiotensin II receptor antagonists, pregnancy Black Box Warnings Pregnancy
Medication Safety Issues: Losartan
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Colace, Coreg Beers Criteria No
Class: HMG-CoA Reductase Inhibitor
Dosage Forms. Oral Tablet: 10 mg, 20 mg, 40 mg; Oral Tablet, Extended Release: 20 mg, 40 mg, 60 mg
Common FDA Label Indication, Dosing, and Titration.
Coronary arteriosclerosis, hypercholesterolemia, primary and mixed: Initial, 20 mg po daily, maintenance 10-80 mg po daily with the evening meal; max 80 mg/d; extended-release tablet: 20-60 mg po qhs
Familial hypercholesterolemia, heterozygous: Children 10-17 y of age, initial, 10 po daily, maintenance 10-40 mg po daily; max 40 mg/d
Off-Label Uses.
None
MOA. HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis.
Drug Characteristics: Lovastatin
Dose Adjustment Hepatic Active liver disease or unexplained persistent elevation of liver enzymes, avoid use Absorption F = <5% with immediate release, improved to 30% with ER, food decreases absorption
Dose Adjustment Renal CrCl <30 mL/min, use caution if giving doses >20 mg/d Distribution
>95% protein bound
Dialyzable Not dialyzable Metabolism 80-85% hepatic, CYP3A4/5 substrate
Pregnancy Category Contraindicated Elimination Renal <10% with a half-life of 2 h
Lactation Contraindicated Pharmacogenetics None known
Contraindications Hypersensitivity to lovastatin, active liver disease, pregnancy and lactation, concomitant use with strong CYP3A4/5 inhibitors, and unexplained persistent elevation of liver enzymes Black Box Warnings None
Medication Safety Issues: Lovastatin
Suffixes No Tall Man Letters No Do Not Crush Do not crush or chew ER formulations High Alert No Confused Names AtorvaSTATin Beers Criteria No
Class: Second-Generation (Atypical) Antipsychotic
Dosage Forms. Tablet, Oral: 20 mg, 40 mg, 60 mg, 80 mg, 120 mg
Common FDA Label Indication, Dosing, and Titration.
Depressive episodes associated with bipolar disorder: Adults, 20 mg po daily, may titrate to max 120 mg po daily
Schizophrenia: Adults, 40 mg po daily, may titrate to max 160 mg/d
Off-Label Uses.
Psychosis associated with dementia: 20 mg po daily
Major depressive disorder with mixed features: 20 mg po daily, may titrate to max 60 mg po daily
MOA. Lurasidone is an atypical antipsychotic agent (benzisothiazole-derivative). It exhibits relatively high affinity for dopamine D2 receptor and serotonin 5-HT7 and 5-HT2A receptors.
Drug Characteristics: Lurasidone
Dose Adjustment Hepatic Moderate dysfunction, max 80 mg/d; severe dysfunction, max 40 mg/d Absorption F = 9-19%; food enhances absorption
Dose Adjustment Renal CrCl <50 mL/min, initial 20 mg/d, max 80 mg/d Distribution
Vd = 6173 L; >99% protein bound
Dialyzable Unknown Metabolism Hepatic, 80%; major substrate of CYP3A4/5
Pregnancy Category Weigh risks and benefits Elimination Renal 9% with a half-life of 18-40 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity, concurrent strong CYP3A4/5 inducers and inhibitors
Black Box Warnings Dementia, suicidality
Medication Safety Issues: Lurasidone
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Lantus Beers Criteria Stroke risk; avoid except in schizophrenia or bipolar disorder
Class: Antiretroviral Agent, CCR5 Antagonist
Dosage Forms. Oral Tablet: 150 mg, 300 mg; Solution Oral: 20 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Treatment of CCR5-tropic HIV-1 infection, in combination with other antiretroviral agents: Adults and Children ≥2 y of age and ≥30 kg, 300 mg po bid
Off-Label Uses.
None
MOA. Selectively and reversibly binds to the chemokine (C-C motif receptor 5 [CCR5]) coreceptors located on human CD4 cells. CCR5 antagonism prevents interaction between the human CCR5 coreceptor and the gp120 subunit of the viral envelope glycoprotein, thereby inhibiting gp120 conformational change required for CCR5-tropic HIV-1 fusion with the CD4 cell and subsequent cell entry.
Drug Characteristics: Maraviroc
Dose Adjustment Hepatic Use with caution if moderate or severe hepatic impairment
Absorption F = 23-33%, food decreases absorption by 30-60%
Dose Adjustment Renal Reduce dose to 150 mg bid if CrCl <30 mL/min; avoid if on interacting meds
Distribution CSF
Dialyzable No Metabolism Hepatic, CYP3A4/5
Pregnancy Category B Elimination Fecal 20% (unchanged), renal 14-34% with a half-life of 14-18 h
Lactation Weight risks and benefits Pharmacogenetics Requires tropism test for the presence of CCR5 on patient CD4 cells
Contraindications Patients with CrCl <30 mL/min or ESRD who are taking potent CYP3A4/5 inhibitors or inducers Black Box Warnings Hepatotoxicity, severe rash, allergic reaction
Medication Safety Issues: Maraviroc
Suffixes No Tall Man Letters No Do Not Crush Oral Tablet High Alert
No Confused Names No Beers Criteria No
Class: Vaccine, Live, Viral
Dosage Forms. Lyophilized Powder for Subcutaneous Injection: 0.5 mL after reconstitution with supplied diluent; also available in combination with varicella vaccine
Common FDA Label Indication, Dosing, and Titration.
Prevention of measles, mumps, and rubella infections: Adults who do not have evidence of immunity, 1 dose (2nd dose indicated for adults born after 1957, health-care personnel, high risk); Children, 1 dose at 12-15 mo of age with a 2nd dose at 4-6 y of age, prior to entering school (second dose can be administered as soon as 28 d after initial dose in children)
Off-Label Uses.
None
Drug Characteristics: Measles, Mumps, Rubella Vaccine
Pregnancy Category C ADME None known
Lactation Generally considered safe during lactation Pharmacogenetics None known
Contraindications Hypersensitivity to MMR vaccine or a component of the vaccine (egg, gelatin, neomycin); immunosuppression; pregnancy Black Box Warnings None
Medication Safety Issues: Measles, Mumps, Rubella Vaccine
Suffixes MMR-II Tall Man Letters No Do Not Crush No High Alert
No Confused Names MMRV Beers Criteria No
Drug Interactions: Measles, Mumps, Rubella Vaccine
Typical Agents: Mechanism: Clinical Management
Moderate- to high-dose corticosteroids : Immunosuppression reduces vaccine efficacy and patients are at increased risk of measles infection : Delay MMR vaccine administration until corticosteroid therapy has been discontinued
Immunosuppressing agents : Immunosuppression reduces vaccine efficacy and patients are at increased risk of measles infection : Delay MMR vaccine administration until immunosuppressive therapy has been discontinued
Immune globulin or blood products : Interference with immune response to live vaccines : Delay MMR vaccine administration for a period of time depending on type and dose of immune globulin or blood product
Class: Progestin Hormone
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Abnormal uterine bleeding unrelated to menstrual cycle: 5-10 mg po daily × 5-10 d starting on days 16 or 21 of the menstrual cycle
Prevention of estrogen-induced endometrial hyperplasia: 5-10 mg po daily for 12-14 d starting on days 1 or 16 of the menstrual cycle, when estrogen is being administered
Secondary physiologic amenorrhea: 5-10 mg po daily × 5-10 d
Off-Label Uses.
Breast cancer, endometrial carcinoma: Dose is individualized
MOA. Medroxyprogesterone transforms proliferative into secretory endometrium. Androgenic and anabolic effects have been noted, but the drug is apparently devoid of significant estrogenic activity.
Drug Characteristics: Medroxyprogesterone
Dose Adjustment Hepatic Mild or moderate hepatic dysfunction, reduce dose or dose frequency; severe, contraindicated Absorption F = 0.6-10%, food increases AUC and Cmax
Dose Adjustment Renal Not required Distribution 86-90% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP3A4/5 substrate; induces CYP3A4/5
Pregnancy Category X Elimination Renal (as metabolites) with a half-life of 11-16 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to medroxyprogesterone, abnormal genital bleeding, history of estrogen- or progesterone-dependent neoplasia, active or history of DVT or PE, severe liver dysfunction, known or suspected pregnancy Black Box Warnings Cardiovascular, dementia risk, loss of BMD (Depo-Provera); breast cancer
Class: NSAID
Dosage Forms. Oral Tablet: 7.5 mg, 15 mg; Oral Capsule: 5 mg, 10 mg; Oral Suspension: 7.5 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Osteoarthritis: Tablets/Suspension, 7.5 mg po daily, may titrate to max 15 mg/d; capsules, 5 mg po daily, may increase to 10 mg daily
Rheumatoid arthritis: 7.5 mg po daily, may titrate to max 15 mg/d
Juvenile rheumatoid arthritis: Children ≥2 y of age, 0.125 mg/kg po daily, may titrate to max 7.5 mg/d
Off-Label Uses.
Gout: 15 mg po daily × 5-7 d, initiate within 24-48 h of onset of gout exacerbation
MOA. Nonselective inhibitor of COX-1 and COX-2 which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties; reversibly alters platelet function and prolongs bleeding time.
Drug Characteristics: Meloxicam
Dose Adjustment Hepatic Not required Absorption F = 89%, food has minimal effect on absorption
Dose Adjustment Renal Avoid if CrCl <20 mL/min Distribution Vd = 10-16 L; 99% protein bound
Dialyzable Not dialyzable, max dose 7.5 mg/d Metabolism Hepatic, minor substrate of CYP3A4/5
Pregnancy Category C (D ≥30 wk gestation) Elimination Renal with a half-life of 15-22 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to meloxicam; concurrent ketorolac, pentoxifylline use, asthma, allergic-type reaction following other NSAID use, CABG Black Box Warnings
Cardiovascular thrombotic events, serious GI bleeding and perforation, CABG
Medication Safety Issues: Meloxicam
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names No Beers Criteria Avoid Chronic Use
Class: N-Methyl-D-Aspartate (NMDA) Receptor Antagonist
Dosage Forms. Oral Solution: 10 mg/5 mL; Oral Tablet:5 mg, 10 mg; Oral Capsule, Extended Release: 7 mg, 14 mg, 21 mg, 28 mg
Common FDA Label Indication, Dosing, and Titration.
Alzheimer disease: Immediate release, 5 mg po daily, may titrate dose no more than once per week to target dose of 10 mg po bid; extended release, 7 mg po daily, may titrate dose no more than once per week to target dose of 28 mg po daily
Off-Label Uses.
Vascular dementia: Immediate release, 5 mg po daily, titrate to target dose of 10 mg po bid
MOA. Activation of NMDA receptors by glutamate is believed to contribute to the symptomatology of Alzheimer disease. Memantine is believed to act as an uncompetitive (open-channel) NMDA receptor antagonist that binds preferentially to the NMDA receptor-operated cation channels. There is no evidence that memantine prevents or slows neurodegeneration in patients with Alzheimer disease.
Drug Characteristics: Memantine
Dose Adjustment Hepatic Not required Absorption F = 100%, no effect of food on absorption
Dose Adjustment Renal CrCl <30 mL/min, immediate-release target dose of 5 mg po bid; extended-release target dose of 14 mg po daily Distribution Vd = 9-11 L; 45% protein bound
Dialyzable Not dialyzable Metabolism Hepatic 50% via glucuronidation
Pregnancy Category B Elimination Renal 50% (unchanged) with a half-life of 60-80 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Memantine
Suffixes XR Tall Man Letters No Do Not Crush XR Capsule High Alert
No Confused Names Mesalamine Beers Criteria No
Class: Vaccine, Inactivated, Bacterial
Dosage Forms.Solution for Intramuscular Injection: Quadrivalent conjugate vaccine (serogroups A, C, Y, W-135; MenACWY-DT, Menactra; MenACWY-CRM, Menveo) 0.5 mL; Monovalent vaccines (serogroup B; MenB-FHbp, Trumenba; MenB-4C, Bexsero) 0.5 mL
Common FDA Label Indication, Dosing, and Titration.
Prevention of invasive meningococcal disease caused by serotypes A, C, Y, W-135: Menveo is approved in adults and children between the ages of 2 mo and 55 y. Menactra is approved for adults and children between the ages of 9 mo and 55 y. While this is an approved indication, routine use is determined by CDC, professional society guidelines and current vaccination recommendations.
Prevention of invasive meningococcal disease caused by serotype B: Trumenba and Bexsero are approved in adults and children 10-25 y of age. While this is an approved indication, use is determined by CDC, professional society guidelines and current vaccination recommendations.
Off-Label Uses.
Prevention of invasive meningococcal disease caused by serotypes A, C, Y, W-135: Routine immunization of adolescents 11-12 y of age and a 2nd dose at 16 y of age of either Menactra or Menveo, 0.5 mL
Prevention of invasive meningococcal disease caused by serotypes A, C, Y, W-135 in individuals at high risk of invasive meningococcal disease or those at ongoing risk of exposure, in individuals with complement deficiencies, asplenia, HIV, individuals who work with Neisseria meningitides in the laboratory: Menactra or Menveo, 0.5 mL 2 doses 3 mo apart and then every 5 y
Prevention of invasive meningococcal disease caused by serotypes A, C, Y, W-135 for military recruits, travelers to or people who live in epidemic areas or endemic countries or 1st-y college students up to 21 y of age who live in dormitory and did not receive a dose at 16 y of age: Menactra or Menveo, single dose of 0.5 mL
Prevention of invasive meningococcal disease caused by serotype B in individuals 11-25 y of age at high risk of invasive serotype B meningococcal disease or during a serotype B outbreak: Bexsero, 0.5 mL per dose, given as 2 doses at least 1 mo apart; Trumenba, 0.5 mL per dose, given as 2 doses 6 mo apart (or 3 doses at 0, 1 and 6 mo during outbreak)
Drug Characteristics: Meningococcal Vaccine
Pregnancy Category B ADME Not known
Lactation Infant risk is minimal Pharmacogenetics None known
Contraindications Hypersensitivity to meningococcal vaccine or a component of the vaccine
Black Box Warnings None
Class: Biguanide, Hypoglycemic
Dosage Forms. Oral Tablet: 500 mg, 850 mg, 1000 mg; Oral Tablet, Extended Release: 500 mg, 750 mg, 1000 mg; Oral Solution: 500 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Diabetes mellitus, Type 2: Adults, immediate release, 500-1000 mg po bid, may titrate to maxdose 2250 mg/d; extended release, 500-2000 mg po daily, may titrate to max dose 2000 mg/d; Children ≥10 y of age, immediate release, 500-1000 mg po bid, may titrate to max dose 2000 mg/d
Polycystic ovary syndrome: 1500-2000 mg/d in 2 divided doses
Off-Label Uses.
None
MOA. Metformin is a biguanide antihyperglycemic agent. It does not affect insulin secretion; rather, it reduces hepatic glucose production and enhances glucose utilization by muscle.
Drug Characteristics: Metformin
Dose Adjustment Hepatic Severe hepatic insufficiency, avoid use Absorption F = 40-60%; immediate release: absorption reduced with food; extended release and oral solution: absorption enhanced with food
Dose Adjustment Renal eGFR <30 mL/min/1.73 m2, contraindicated; eGFR 30-45 mL/min/1.73 m2, use not recommended Distribution Vd = 654 L; not protein bound
Dialyzable Yes Metabolism Not metabolized
Pregnancy Category B Elimination Renal 90% with a half-life of 7-12 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to metformin, contrast media, eGFR <30 mL/min/1.73 m2, metabolic acidosis Black Box Warnings Lactic acidosis
Medication Safety Issues: Metformin
Suffixes XR Tall Man Letters MetFORMIN Do Not Crush Do not chew or crush ER formulation High Alert Yes Confused Names MetroNIDAZOLE
Beers Criteria No
Class: Opioid Analgesic. C-II
Dosage Forms. Oral Tablet: 5 mg, 10 mg; Oral Tablet, Soluble: 40 mg; Oral Solution: 5 mg/5 mL, 10 mg/5 mL, 10 mg/1 mL
Common FDA Label Indication, Dosing, and Titration.
Pain, chronic (moderate-severe): Opioid naive patients, 2.5 mg po q8h-q12h, may titrate to response
Drug detoxification, opioid abuse: 15-30 mg po q8h, titrate to response (usual range 80-120 mg/d); when used for treatment of opioid addiction (detoxification or maintenance), may only be dispensed by certified opioid treatment programs
Off-Label Uses.
None
MOA. Binds to opiate receptors in CNS, causing inhibition of ascending pain pathways, altering perception to pain, and produces generalized CNS depression. Methadone is a phenylethylamine opioid agonist qualitatively similar to morphine but with a chemical structure unrelated to the alkaloid-type structures of the opium derivatives. Analgesic activity of (R)-methadone is 8-50 times that of (S)-methadone, and (R)-methadone has a tenfold higher affinity for opioid receptors.
Drug Characteristics: Methadone
Dose Adjustment Hepatic Not required Absorption F = 85% with minimal food effect
Dose Adjustment Renal Not required Distribution Vd = 3.6 L/kg; 85-90% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP2B6 and 3A4/5 substrate, moderate CYP2D6 inhibitor
Pregnancy Category C Elimination Renal 10-20% with a half-life of 48-60 h
Lactation Usually compatible, peak concentration 4-5 h after dose Pharmacogenetics
None known
Contraindications Bronchial asthma, hypersensitivity to opioids, paralytic ileus, respiratory depression, hypercarbia Black Box Warnings Accidental ingestion; addiction, abuse, and misuse; QTc prolongation; respiratory depression; concurrent use with benzodiazepines; REMS; neonatal opioid withdrawal; conditions for use in opioid addiction; CYP interactions
Medication Safety Issues: Methadone
Suffixes Intensol Tall Man Letters No Do Not Crush Tablet for Suspension Confused Names Dexmethlyphenidate, Mephyton Beers Criteria No
Class: Antimetabolite
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg; Oral Solution:2.5 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Non-Hodgkin lymphoma, advanced (Burkitt lymphoma, stages I and II): 10-25 mg/d po for 4-8 d for several courses with a 7-10 d rest period
Psoriasis, severe: Initial, 2.5-5 mg q12h × 3 doses/wk, may titrate dose to 10-25 mg/wk po
Rheumatoid arthritis, severe: 7.5-15 mg po once weekly, may titrate by 5 mg/wk every 2-3 wk to max 20-30 mg/wk
Juvenile rheumatoid arthritis, polyarticular course: 10 mg/m2 po once weekly, may titrate to clinical response
Off-Label Uses.
Many cancers: Dose varies with cancer, stage, and concurrent chemotherapy
MOA. Reversibly inhibits dihydrofolate reductase (DHFR). Dihydrofolates are reduced to tetrahydrofolates by DHFR before they are used in DNA synthesis. Methotrexate interferes with DNA synthesis, repair, and cellular replication.
Drug Characteristics: Methotrexate
Dose Adjustment Hepatic Bilirubin = 3.1-5 mg/dL, reduce dose by 25%; bilirubin >5 mg/dL, avoid Absorption Dose-dependent, doses <40 mg/m2, F = 42%; doses >40 mg/m2, F = 17%
Dose Adjustment Renal CrCl = 10-50 mL/min, reduce dose by 50%; CrCl <10 mL/min: avoid
Distribution Vd = 0.4-0.8 L/kg; 50% protein bound
Dialyzable Yes, hemodialysis Metabolism Intracellular polyglutamation, excreted by OATP1B1
Pregnancy Category X Elimination Renal 48-100% with a dose-dependent half-life of 4-10 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to methotrexate, pregnancy, nursing, preexisting blood dyscrasias in patients treated for psoriasis and rheumatoid arthritis Black Box Warnings
Bone marrow suppression, renal impairment, hepatotoxicity, pneumonitis, GI toxicity, secondary malignancy, tumor lysis syndrome, dermatologic toxicity, opportunistic infections, radiotherapy
Class: CNS Stimulant. C-II
Dosage Forms. Oral Tablet: 5 mg, 10 mg, 20 mg; Oral Tablet, Chewable: 2.5 mg, 5 mg, 10 mg; Oral Tablet, Chewable, Extended Release: 20 mg, 30 mg, 40 mg; Oral Tablet, Extended Release: 10 mg, 18 mg, 20 mg, 27 mg, 36 mg, 54 mg, 72 mg; Oral Tablet, Extended Release, Disintegrating: 8.6 mg, 17.3 mg, 25.9 mg; Oral Tablet, Extended Release, 24 h: 18 mg, 20 mg, 27 mg, 36 mg, 54 mg, 72 mg; Oral Capsule, Extended Release: 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg; Oral Capsule Extended Release, 24 h: 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg; Oral Solution: 5 mg/5 mL, 10 mg/5 mL; Oral Suspension: 25 mg/5 mL; Patch: 10 mg/9 h, 15 mg/9 h, 20 mg/9 h, 30 mg/9 h; Patch, Transdermal: 10 mg/9 h, 15 mg/9 h, 20 mg/9 h, 30 mg/9 h
Common FDA Label Indication, Dosing, and Titration.
Attention-deficit hyperactivity disorder: Adults, immediate-release tablets, solution, and chewable tablets, 10-60 mg/d po divided 2-3 times daily, preferably 30-45 min before meals; Children ≥6 y of age, initial, 5 mg po bid, may titrate in increments of 5-10 mg at weekly intervals; doses above 60 mg/d not recommended
Attention-deficit hyperactivity disorder, no prior methylphenidate therapy: Adults and Children ≥6 y of age, extended release, 20 mg po daily, may titrate in increments of 10 mg at weekly intervals; max 60 mg/d
Narcolepsy: Adults, immediate-release tablets, solution, and chewable tablets, 10-60 mg/d po divided 2-3 times daily; sustained release; Adults and Children ≥6 y of age, 20-60 mg/d po divided q8h
Off-Label Uses.
Depression: 5-30 mg po daily
Fatigue, cancer related: 5 mg po bid (max 40 mg/d)
MOA. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.
Dose Adjustment Hepatic Not required Absorption F = 22-25%, minimal food effect
Dose Adjustment Renal Not required Distribution Vd = 2.6 L/kg; 10-30% protein bound
Dialyzable Not dialyzable Metabolism Extensive, predominately via de-esterification
Pregnancy Category C Elimination Renal 78-98% with a half-life of 3 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to amphetamines, anxiety, agitation, concurrent MAOIs, drug dependence, glaucoma, tics or history of Tourette syndrome, hypertension, angina, heart failure, concurrent halogenated anesthetics Black Box Warnings Abuse and dependence potential
Class: Adrenal Corticosteroid
Dosage Forms. Oral Tablet: 2 mg, 4 mg, 8 mg, 16 mg, 32 mg
Common FDA Label Indication, Dosing, and Titration.
Dosing for indications listed below: Adults, 4-48 mg po daily; Children, specific dosing parameters not specified; for all patients, adjust dose according to patient response.
Allergic states (eg, asthma, etc)
Dermatologic diseases (eg, exfoliative erythroderma, etc)
Endocrine disorders (eg, adrenocortical insufficiency, etc)
Gastrointestinal diseases (eg, regional enteritis, ulcerative colitis, etc)
Hematologic disorders (eg, acquired hemolytic anemia, etc)
Neoplastic diseases (eg, palliative management of leukemias and lymphomas, etc)
Nervous system (eg, multiple sclerosis, cerebral edema, etc)
Renal diseases (eg, idiopathic nephrotic syndrome, systemic lupus erythematosus, etc)
Respiratory diseases (eg, idiopathic eosinophilic pneumonia, etc)
Rheumatic disorders (eg, rheumatoid arthritis, etc)
Off-Label Uses.
None
MOA. Corticosteroids are naturally occurring and synthetic adrenocortical steroids cause varied metabolic effects, modify the body's immune responses to diverse stimuli, and are used primarily for their anti-inflammatory effects in disorders of many organ systems.
Drug Characteristics: Methylprednisolone
Dose Adjustment Hepatic Not required Absorption Well absorbed
Dose Adjustment Renal Not required Distribution Vd = 1.5 L/kg
Dialyzable Not dialyzable Metabolism Hepatic, CYP3A4/5 substrate
Pregnancy Category C Elimination Primarily renal with a half-life of 2-3 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to methylprednisolone or other glucocorticosteroids, administration of live vaccines, fungal infections Black Box Warnings None
Class: Dopamine Antagonist
Dosage Forms. Oral Tablet: 5 mg, 10 mg; Oral Solution: 5 mg/5 mL, 10 mg/10 mL; Oral Dispersible Tablet: 5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Diabetic gastroparesis: 5-10 mg po 30 min before meals and at bedtime × 2-8 wk; max 12 wk duration
Gastroesophageal reflux disease: Adults, 10-15 mg po qid 30 min before meals and at bedtime; Neonates, 0.15 mg/kg po q6h; Infants, 0.1 mg/kg po tid-qid 10-30 min before meals and at hs, max dose 0.3-0.75 mg/kg/d × 2 wk-6 mo
Off-Label Uses.
Decreased lactation: 30-45 mg po daily × 7-15 d or 10-15 mg po tid × 7-15 d
Nondiabetic gastroparesis: 10 mg po 30 min before meals and at hs for 2-8 wk; max 12 wk duration
MOA. Metoclopramide stimulates motility of the upper GI tract without stimulating gastric, biliary, or pancreatic secretions. Its mode of action is unclear. It seems to sensitize tissues to the action of acetylcholine. It is also a dopamine receptor antagonist at dose >5 mg/kg.
Drug Characteristics: Metoclopramide
Dose Adjustment Hepatic Not required Absorption F = 80%, minimal food effect
Dose Adjustment Renal CrCl <40 mL/min, reduce dose by 50% Distribution Vd = 3.5 L/kg; 30% protein bound
Dialyzable 2-38% by hemodialysis Metabolism Hepatic, CYP2D6 substrate
Pregnancy Category B Elimination Renal 75-80%, with a half-life of 5-6 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2D6, maxtotal daily dose to 30 mg in poor CYP2D6 metabolizers, G6PD
Contraindications Hypersensitivity, GI hemorrhage, mechanical obstruction or perforation, pheochromocytoma, concomitant use with drugs likely to cause extrapyramidal reactions, epilepsy
Black Box Warnings Tardive dyskinesia
Class: β-Adrenergic Blocker, Cardioselective
Dosage Forms. Oral Tablet: 25 mg, 37.5 mg, 50 mg, 75 mg, 100 mg; Oral Tablet, Extended Release: 25 mg, 50 mg, 100 mg, 200 mg; Oral Capsule, Extended Release, 24 H Sprinkle: 25 mg, 50 mg, 100 mg, 200 mg
Common FDA Label Indication, Dosing, and Titration.
Angina: Adults, 50 mg po bid or 100 mg extended release po daily, may titrate at weekly intervals to max 400 mg total daily dose
Heart failure: Adults, NYHA Class II, 25 mg extended release po daily for 2 wk, may titrate to target of 200 mg/d; NYHA Class III-IV, 12.5 mg extended release po daily for 2 wk, may titrate to target of 200 mg/d
Hypertension: Adults, initial, immediate release, 50 mg po bid, may titrate up to 400 mg po per day in 2-3 divided doses; initial, extended release, 25-100 mg po daily, may titrate to 100-400 mg once daily; Children >6 y of age, 1 mg/kg po daily, may titrate to max 50 mg/d
AMI: Adults, immediate release, 25-50 mg po q6h-q12h, convert to bid dosing over 2-3 d, or to daily extended release dosing with a max dose of 200 mg po daily
Off-Label Uses.
Atrial fibrillation-ventricular rate control: Adults, immediate release 50-200 mg po daily, or extended release 50-400 mg po daily
Cardiac dysrhythmia: Adults, immediate release, 25-100 mg po bid; extended release, 50-400 mg po daily
MOA. Metoprolol is a cardioselective β-adrenergic blocker used in arrhythmias, hypertension, angina pectoris, and heart failure. It is also effective in decreasing post-MI mortality.
Drug Characteristics: Metoprolol
Dose Adjustment Hepatic Liver disease, titrate slowly Absorption F = 65-70%; food increases Cmax and AUC
Dose Adjustment Renal Not required Distribution Vd = 3-5 L; 12% protein bound
Dialyzable Yes, give maintenance dose after dialysis completed Metabolism Hepatic, CYP2D6 substrate
Pregnancy Category C Elimination Renal 95% (as metabolite) with a half-life of 3-7 h
Lactation Weigh risks and benefits Pharmacogenetics Use with caution in known CYP2D6 poor metabolizers
ContraindicationsHypersensitivity; severe bradycardia, 2nd- or 3rd-degree AV block, sick sinus syndrome; decompensated heart failure; cardiogenic shockBlack Box WarningsIschemic heart disease with abrupt withdrawal
Class: Nitroimidazole Antibiotic, Antiprotozoal
Dosage Forms. Oral Capsule:375 mg; Oral Tablet: 250 mg, 500 mg
Common FDA Label Indication, Dosing, and Titration.
Abscess, anaerobic: 7.5 mg/kg po q6h; max 4 g/d
Amebic dysentery, acute: Adults, 500-750 mg po q8h × 7-10 d; Children, 35-50 mg/kg/d po in 3 divided doses for 10 d; max 750 mg/dose
Bacterial vaginosis: 500 mg po bid × 7 d
Trichomoniasis (for patient and sex partner): 2 g po × 1 dose or 500 mg po bid × 7 d
Off-Label Uses.
Clostridium difficile infection, including pseudomembranous colitis, mild-moderate initial episode or 1st recurrence: 500 mg po tid × 10-14 d
Helicobacter pylori GI tract infection: 500 mg po tid in combination with a macrolide and a PPI ("triple therapy"), or 250 mg po qid with bismuth, tetracycline and a PPI ("quadruple therapy")
MOA. Metronidazole is a synthetic nitroimidazole active against Trichomonas vaginalis (trichomoniasis), Entamoeba histolytica (amebiasis), and Giardia lamblia (giardiasis); it is bactericidal against nearly all obligate anaerobic bacteria including Bacteroides fragilis.
Drug Characteristics: Metronidazole
Dose Adjustment Hepatic Severe hepatic dysfunction, consider dose reduction by 50%
Absorption F = 100%, food effects rate, but not extent of absorption
Dose Adjustment Renal CrCl <10 mL/min, reduce dose by 50% Distribution Abscess, bronchial fluids, peritoneal, saliva, crosses BBB
Dialyzable Yes, supplement after hemodialysis, Peritoneal dialysis—no adjustment Metabolism
Hepatic 30-60% via glucuronidation. Moderate CYP3A4/5 inhibitor
Pregnancy Category B Elimination Renal 60-80% (unchanged) with a half-life of 8 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to metronidazole, 1st trimester of pregnancy Black Box Warnings Carcinogenic
Class: Tetracycline Antibiotic
Dosage Forms. Oral Tablet: 50 mg, 75 mg, 100 mg; Oral Tablet, Extended Release: 45 mg, 55 mg, 65 mg, 80 mg, 90 mg, 105 mg, 115 mg, 135 mg; Oral Capsule: 50 mg, 75 mg, 100 mg; Oral Capsule, Extended Release, 24 H: 90 mg, 135 mg
Common FDA Label Indication, Dosing, and Titration.
Acne vulgaris: Immediate release, initiate with single 200 mg loading dose, then 100 mg bid; extended-release, 1 mg/kg/d po daily × 12 wk
Allergy to penicillin—bacterial infectious disease: Adults, initial, 200 mg po, followed by 100 mg po q12h; Children >8 y of age, 4 mg/kg po, followed by 2 mg/kg/dose q12h (max dose 200 mg/d), duration of therapy depends on indication
Off-Label Uses.
None
MOA. Tetracyclines are broad-spectrum bacteriostatic compounds that inhibit protein synthesis at the 30S ribosomal subunit. Activity includes gram-positive, gram-negative, aerobic, and anaerobic bacteria, as well as spirochetes, mycoplasmas, rickettsiae, chlamydiae, and some protozoa. Many bacteria have developed plasmid-mediated resistance. Most Enterobacteriaceae and Pseudomonas aeruginosa are resistant.
Drug Characteristics: Minocycline
Dose Adjustment Hepatic Not required Absorption F = 90%; can be taken without regard to food
Dose Adjustment Renal No specific recommendations, but consider dose reduction or extending the interval. Do not exceed 200 mg daily Distribution Aqueous humor, CSF, gingival fluids, sinus, saliva, tears
Dialyzable Not dialyzable Metabolism Hepatically metabolized, extent unknown
Pregnancy Category D Elimination Renal 5-12%, fecal 20-34% with a half-life of 16 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Minocycline
Suffixes No Tall Man Letters No Do Not Crush ER Formulations
Confused Names Indocin, Lincocin, Minizide, Niacin, Dyazide, Dynapen Beers Criteria No
Class: Antidepressant, α2-Antagonist
Dosage Forms. Oral Tablet: 7.5 mg, 15 mg, 30 mg, 45 mg; Oral Disintegrating Tablet: 15 mg, 30 mg, 45 mg
Common FDA Label Indication, Dosing, and Titration.
Depression: 15 mg po daily hs, may titrate to response in 15 mg increments q1-2wk to 45 mg po daily hs
Off-Label Uses.
Headache: 15 mg po daily hs, may titrate to response after 1 wk to 30 mg po daily hs
Panic disorder: 15 mg po daily hs, may titrate to response in 15 mg increments q1wk to 45 mg po daily hs
MOA. Mirtazapine is an antidepressant that antagonizes presynaptic α2-adrenergic auto- and heteroreceptors that are responsible for controlling the release of norepinephrine and serotonin (5-HT). It is also a potent antagonist of postsynaptic 5-HT2 and 5-HT3 receptors. The net outcome of these effects is increased noradrenergic activity and enhanced 5-HT activity, especially at 5-HT1A receptors. This unique mechanism of action preserves antidepressant efficacy but minimizes many of the adverse effects common to heterocyclic antidepressants and SSRIs.
Drug Characteristics: Mirtazapine
Dose Adjustment Hepatic Increase dose slowly as needed and tolerated Absorption
F = 50%; minimal effect of food on absorption
Dose Adjustment Renal CrCl <40 mL/min, increase dose slowly as needed and tolerated Distribution
Vd = 4.5 L/kg; 85% protein bound
Dialyzable Not dialyzable Metabolism Hepatic via CYP3A4/5, 2D6 and 1A2, as well as by demethylation and hydroxylation
Pregnancy Category C Elimination Renal 75% (as metabolites), fecal 15% with a half-life of 20-40 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to mirtazapine; concurrent use or use within 14 d of MAOI, linezolid, IV methylene blue use Black Box Warnings Suicidality; not for use in children
Class: CNS Stimulant. C-IV
Dosage Forms. Oral Tablet: 100 mg, 200 mg
Common FDA Label Indication, Dosing, and Titration.
Narcolepsy: 200 mg po daily in the morning, max 400 mg/d
Obstructive sleep apnea, improve excessive sleepiness; adjunct: 200 mg po daily in the morning, max 400 mg/d
Shift work-sleep disorder: 200 mg po daily 1 h before start of work shift, max 400 mg/d
Off-Label Uses.
Attention-deficit hyperactivity disorder: 200 mg po daily
Depression (antidepressant augmentation): 100 mg po daily × 3-7 d, then titrate to 200 mg po daily (max 400 mg/d)
MOA. The mechanism of action of modafinil is uncertain. Modafinil is a wakefulness-promoting agent acting as a CNS stimulant. It is chemically and pharmacologically unrelated to other CNS stimulants, such as methylphenidate, amphetamine, or pemoline.
Drug Characteristics: Modafinil
Dose Adjustment Hepatic Severe hepatic impairment, reduce dose by 50% Absorption
Rapid absorption, food slows absorption but does not affect extent
Dose Adjustment Renal CrCl <20 mL/min, initial dose 100-200 mg/d Distribution Vd = 0.9 L/kg; 60% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP3A4/5 substrate. Strong CYP2C19 inhibitor
Pregnancy Category C Elimination Renal 80% (10% unchanged), fecal 1% with a half-life of 7.5-15 h
Lactation Weigh risks and benefits Pharmacogenetics In CYP2D6 poor metabolizers, CYP2C19 is major alternative pathway for TCAs. Avoid concurrent use of TCAs and modafinil in CYP2D6 poor metabolizers
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Modafinil
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Plaquenil Beers Criteria No
Class: Intranasal Corticosteroid
Dosage Forms. Nasal Spray: 50 mcg/actuation
Common FDA Label Indication, Dosing, and Titration.
Seasonal and perennial allergic rhinitis: Children 2-11 y of age, 1 spray/nostril daily (100 mcg/d); Children ≥12 y of age and Adults, 2 sprays/nostril daily (200 mcg/d)
Nasal polyp: 2 sprays/nostril (50 mcg/spray) bid (400 mcg/d), reduce dose to 2 sprays/nostril daily if possible
Off-Label Uses.
Rhinosinusitis: Children ≥12 y of age and Adults, 2 sprays/nostril (50 mcg/spray) bid
MOA. Mometasone has anti-inflammatory, antipruritic, and vasoconstrictive properties. Corticosteroids are thought to act by the induction of phospholipase A2-inhibitory proteins, lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Drug Characteristics: Mometasone Nasal
Dose Adjustment Hepatic Not required Absorption Minimal (<2%) absorption after nasal administration
Dose Adjustment Renal Not required Distribution Not absorbed
Dialyzable Not dialyzable Metabolism Not absorbed
Pregnancy Category C Elimination Not absorbed
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Mometasone Nasal
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Beers Criteria No
Class: Leukotriene Receptor Antagonist
Dosage Forms. Oral Tablet: 10 mg; Oral Chewable Tablet: 4 mg, 5 mg; Oral Granules: 4 mg/packet
Common FDA Label Indication, Dosing, and Titration.
Asthma: Children 12 mo to 5 y of age, 4 mg po daily; Children 6-14 y of age, 5 mg po daily; Children ≥15 y of age and Adults, 10 mg po daily
Exercise-induced bronchoconstriction: Children 6-14 y of age, 5 mg po 2 h before exercise; Children ≥15 y of age and Adults, 10 mg po 2 h before exercise, max 1 dose/24 h
Seasonal allergic rhinitis: Children 2-5 y of age, 4 mg po daily; Children 6-14 y of age, 5 mg po daily; Children ≥15 y of age and Adults, 10 mg po daily
Off-Label Uses.
Atopic dermatitis: Children 2-5 y of age, 5 mg po daily; Children ≥12 y of age and Adults, 10 mg po daily
Urticaria (NSAID-induced or idiopathic): Adults, 10 mg po daily
MOA. Leukotrienes are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils, and bind to leukotriene receptors. Montelukast binds with leukotriene receptors to inhibit physiologic actions of leukotriene.
Drug Characteristics: Montelukast
Dose Adjustment Hepatic Not required Absorption F = 63-73%, food decreases bioavailability
Dose Adjustment Renal Not required Distribution Vd = 8-11 L; >99% protein bound
Dialyzable Not dialyzable Metabolism Hepatic via CYP3A4/5, 2C8 and CYP2C9
Pregnancy Category B Elimination Renal <1% with a half-life of 3-6 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Montelukast
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Oralair, SINEquan Beers Criteria No
Class: Opioid Analgesic. C-II
Dosage Forms. Oral Tablet: 15 mg, 30 mg; Oral Tablet, Extended Release: 15 mg, 30 mg, 60 mg, 100 mg, 200 mg; Oral Tablet, Extended Release, Abuse Deterrent: 15 mg, 30 mg, 60 mg, 100 mg; Oral Capsule, Extended Release, 24 h: 10 mg, 20 mg, 30 mg, 40 mg, 45 mg, 50 mg, 60 mg, 75 mg, 80 mg, 90 mg, 100 mg, 120 mg, 200 mg; Oral Solution: 10 mg/5 mL, 20 mg/5 mL, 20 mg/1 mL, 100 mg/5 mL; Rectal Suppository: 5 mg, 10 mg, 20 mg, 30 mg
Common FDA Label Indication, Dosing, and Titration.
Pain, chronic, moderate to severe: 10-20 mg po q12h, titrate to response; use immediate-release formulation to determine patient's morphine requirement and titrate to response. Extended-release products are administered every 12-24 h.
Off-Label Uses.
None
MOA. Morphine is a pure mu agonist. Mu receptors are responsible for analgesia, respiratory depression, miosis, decreased GI motility, and euphoria. In the CNS, it promotes analgesia and respiratory depression by decreasing brain stem respiratory centers' response to carbon dioxide tension and electrical stimulation. It also decreases gastric, biliary, and pancreatic secretion, induces peripheral vasodilation, and promotes opioid-induced hypotension due to histamine release.
Drug Characteristics: Morphine
Dose Adjustment Hepatic Severe impairment, extend dosing interval or start with lower doses
Absorption F = <40%, food slows rate, but not extent of absorption
Dose Adjustment Renal CrCl 10-50 mL/min, reduce dose by 25%; CrCl <10 mL/min, reduce dose by 50% Distribution Vd = 1-6 L/kg; 20-36% protein bound
Dialyzable Not dialyzable Metabolism Hepatic by glucuronidation
Pregnancy Category C Elimination Renal 90% (as metabolites) with a half-life of 15 h
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity to opioids, acute or severe asthma, paralytic ileus, respiratory depression, GI obstruction; concurrent use or use within 14 days of MAOI
Black Box Warnings Ethanol; addiction, abuse and misuse, REMS, respiratory depression, neonatal opioid withdrawal, accidental ingestion, concurrent use with benzodiazepines, medication errors
Class: Fluoroquinolone Antibiotic
Dosage Forms. Oral Tablet: 400 mg
Common FDA Label Indication, Dosing, and Titration.
Acute bacterial exacerbation of chronic bronchitis: 400 mg po daily × 5 d
Bacterial sinusitis, acute: 400 mg po daily × 10 d
Community-acquired pneumonia: 400 mg po daily × 7-14 d
Infection of skin and/or subcutaneous tissue: 400 mg po daily × 7-21 d
Complicated intra-abdominal infections: 400 mg po daily × 5-14 days
Off-Label Uses.
Tuberculosis: 400 mg po daily × 6 mo
MOA. Moxifloxacin is a fluoroquinolone that inhibits bacterial topoisomerase II and IV. It has a broad spectrum of activity, including gram-positive and gram-negative organisms, Chlamydia, and anaerobes. It is effective for respiratory tract infections caused by Streptococcus pneumoniae, Haemophilus influenzae, and others.
Drug Characteristics: Moxifloxacin
Dose Adjustment Hepatic Not required Absorption F = 90%, no food effect, take without regard to meals
Dose Adjustment Renal Not required Distribution Vd = 1.7-2.7 L/kg; abdominal tissue, bronchial mucosa CSF, sinus, sputum; 30-50% protein binding
Dialyzable Not dialyzable Metabolism 52% hepatic via glucuronide and sulfate conjugation
Pregnancy Category C Elimination Renal 20% with a half-life of 12 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings Myasthenia gravis, tendon inflammation and rupture peripheral neuropathy, aortic dissections, hypoglycemia, delirium
Medication Safety Issues: Moxifloxacin
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Avonex Beers Criteria No
Class: Topical Antibacterial
Dosage Forms. Topical Ointment: 2%; Topical Cream: 2%; Nasal Ointment: 2%
Common FDA Label Indication and Dosing.
Impetigo: Apply topically tid × 3-5 d, reevaluate if no response
Secondary skin infections: Apply topically tid × 10 d, reevaluate if no response in 3-5 d
Eradication of nasal colonization of MRSA during institutional outbreaks: Apply one-half of single use tube to each nostril bid × 5 d
Off-Label Uses.
Surgical prophylaxis in MRSA carriers: Apply one-half of single tube to each nostril bid × 5 d
MOA. Mupirocin is an antibacterial agent active against a wide range of gram-positive bacteria including methicillin-resistant Staphylococcus aureus. It is also active against certain gram-negative bacteria. Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl transfer-RNA synthetase. Because of this unique mode of action, mupirocin demonstrates no in vitro cross-resistance with other classes of antimicrobial agents.
Drug Characteristics: Mupirocin
Dose Adjustment Hepatic Not required Absorption Minimal absorption after application to intact skin
Dose Adjustment Renal Not required Distribution Not absorbed
Dialyzable Not dialyzable Metabolism Not absorbed
Pregnancy Category B Elimination Not absorbed
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity Black Box Warnings None
Medication Safety Issues: Mupirocin
Suffixes AT Nasal Tall Man Letters No Do Not Crush No High Alert
No Confused Names Bacitracin, Baclofen, Bactrim Beers Criteria No
Class: NSAID
Dosage Forms. Oral Tablet: 220 mg, 250 mg, 275 mg, 375 mg, 500 mg, 550 mg; Oral Tablet, Delayed Release: 375 mg, 500 mg; Oral Tablet, Extended Release, 24 h: 375 mg, 500 mg, 750 mg; Oral Capsule: 220 mg; Oral Suspension: 125 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Osteoarthritis: 250-550 mg po bid, extended-release, 750-1000 mg po once daily
Rheumatoid arthritis: 250-550 mg po bid, extended-release, 750-1000 mg po once daily
Gout, acute: Immediate release, 250-275 mg po tid, or extended release, 1000 mg po daily
Fever: Adults and Children >12 y of age, 200-400 mg po q8-12h prn, to a max 600 mg daily
Pain: Adults, 500 mg po q12h or 25 mg po q6-8h
Off-Label Uses.
Migraine: Initial, 750 mg po; may administer an additional 250-500 mg prn, max 1250 mg/24 h
MOA. Nonselective inhibitor of COX-1 and COX-2.
Drug Characteristics: Naproxen
Dose Adjustment Hepatic Not required, use at lowest effective dose, reduced dose may be considered Absorption F = 95%, food has minimal effect on absorption
Dose Adjustment Renal Avoid if CrCl <30 mL/min Distribution Vd = 0.16 L/kg; >99% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic not via CYP450
Pregnancy Category C Elimination Renal 95%, fecal 3% with a half-life of 12-17 h (age dependent)
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to naproxen, other NSAIDs, aspirin or sulfonamides; asthma or allergic-type reaction following aspirin or other NSAID administration, CABG surgery, treatment of perioperative pain Black Box Warnings Cardiovascular and GI risk; thrombotic events
Class: β-Adrenergic Blocker, Cardioselective, B1 Selective
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertension: 5 mg po daily; may titrate q2wk to max 40 mg/d
Off-Label Uses.
None
MOA. Nebivolol is a long-acting cardioselective β1-adrenoceptor antagonist without intrinsic sympathomimetic activities. The mechanism of action of the antihypertensive response of nebivolol is not fully understood. Possible mechanisms include decreased heart rate, decreased myocardial contractility and vasodilation, and decreased peripheral vascular resistance.
Drug Characteristics: Nebivolol
Dose Adjustment Hepatic Moderate hepatic dysfunction, initial dose 2.5 mg po daily, titrate carefully Severe impairment, avoid Absorption F = 12% (extensive metabolizers), F = 96% (poor metabolizers); no effect of food on absorption
Dose Adjustment Renal CrCl <30 mL/min, initial dose 2.5 mg po daily, titrate carefully Distribution
Vd = 8-12 L/kg; 98% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, via CYP2D6
Pregnancy Category C Elimination Renal 38% (extensive metabolizers) to 67% (poor metabolizers) with a half-life of 12-19 h
Lactation Weigh risks and benefits Pharmacogenetics No dosage adjustment required for CYP2D6 poor metabolizers
Contraindications Hypersensitivity to nebivolol; severe bradycardia, 2nd- or 3rd-degree AV block, sick sinus syndrome; decompensated heart failure, cardiogenic shock; severe hepatic impairment Black Box Warnings None
Medication Safety Issues: Nebivolol
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names No Beers Criteria No
Class: Antihyperlipidemic
Dosage Forms. Oral Capsule, Extended Release: 250 mg, 500 mg; Oral Tablet: 50 mg, 100 mg, 250 mg, 500 mg; Oral Tablet, Extended Release: 250 mg, 500 mg, 750 mg, 1000 mg
Common FDA Label Indication, Dosing, and Titration.
Coronary arteriosclerosis, hypercholesterolemia: Extended release, 500 mg po daily hs, may titrate to 2000 mg/d
Dyslipidemia: Immediate release, 100-1000 mg po tid, may titrate to 3000 mg/d; extended release, 500-2000 mg po daily hs, may titrate to 2000 mg/d
Myocardial infarction, secondary prophylaxis: Extended release, 500-2000 mg po daily hs, may titrate to 2000 mg/d
Off-Label Uses.
Pellagra: 50-100 mg po tid-qid, may titrate to 500 mg/d po
MOA. Not well-defined. May involve partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity, which may increase the rate of chylomicron triglyceride removal from plasma. Niacin decreases the rate of hepatic synthesis of VLDL and LDL.
Drug Characteristics: Niacin
Dose Adjustment Hepatic Contraindicated in patients with significant or unexplained hepatic dysfunction Absorption F = 60%, fatty meals decrease absorption
Dose Adjustment Renal Not required Distribution Mainly to hepatic, renal and adipose tissues; <20% protein bound
Dialyzable Unknown Metabolism Hepatic, not via CYP450
Pregnancy Category C Elimination Renal 60-88% with a half-life of 20-45 min
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to niacin, active liver disease, PUD, arterial hemorrhage
Black Box Warnings None
Class: Dihyrdopyridine Calcium Channel Blocker
Dosage Forms. Oral Tablet, Extended Release, 24 h: 30 mg, 60 mg, 90 mg; Oral Capsule: 10 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertension: Adults, extended release, 30 mg po daily, may titrate to 90 mg/d po (Adalat CC) or 120 mg/d po (Procardia XL); Children, 0.25 mg/kg po daily in 1 or 2 divided doses, may titrate to 3 mg/kg/d po (max 180 mg/d)
Stable chronic angina: Immediate release, 10-20 mg po tid, may titrate to 20-30 mg po 3-4 times/d, max 160 mg/d; extended release, 30-60 mg po daily, may titrate to 120 mg/d po
Variant angina: Immediate release, 5-20 mg pot id; extended release, 30-60 mg po daily, may titrate to 120 mg/d po
Off-Label Uses.
Raynaud phenomenon: Extended release, 30-60 mg po daily
MOA. Nifedipine is a calcium ion influx inhibitor that selectively inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle. Nifedipine does not alter serum calcium concentrations.
Drug Characteristics: Nifedipine
Dose Adjustment Hepatic Clearance is reduced in patients with cirrhosis, use with caution
Absorption F = 40-77% (immediate release), 65-89% (extended release); complete absorption, food delays absorption of Adalat CC
Dose Adjustment Renal Not required Distribution Vd = 1.4-202 L/kg; 92-98% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic, CYP3A4/5 substrate
Pregnancy Category C Elimination Renal 60-80% with a half-life of 5 h (immediate release), 7 h (extended release)
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity, cardiogenic shock, STEMI, concomitant use of CYP3A4/5 inducers Black Box Warnings None
Class: Nitrofuran Antibiotic
Dosage Forms. Oral Capsule: 25 mg, 50 mg, 100 mg; Oral Suspension: 25 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Urinary tract infection, treatment: Adults and Children >12 y of age, Macrobid 100 mg po bid × 5-7 d; Furadantin, Macrodantin, 50-100 mg po q6h × 5-7 d; Children ≥1 mo of age, 5-7 mg/kg/d in divided doses q6h po × 7 d (max 400 mg/d)
Urinary tract infection, prophylaxis: Adults, 50-100 mg po daily hs; Children ≥1 mo of age, 1 mg/kg/d po in divided doses every 12-24 h (max dose 100 mg/d)
Off-Label Uses.
None
MOA. Nitrofurantoin is a synthetic nitrofuran that inactivates bacterial ribosomes and is bactericidal in urine at therapeutic doses. It is active against most bacteria that cause UTIs except nearly all strains of Pseudomonas are resistant.
Drug Characteristics: Nitrofurantoin
Dose Adjustment Hepatic Not required Absorption F = 94%, food increases absorption
Dose Adjustment Renal Contraindicated if CrCl <60 mL/min Distribution 60-90% protein bound
Dialyzable Yes, hemodialysis only Metabolism Metabolism in all tissues to inactive metabolite
Pregnancy Category B, contraindicated in pregnancy at term Elimination Renal 20-25% with a half-life of 1 h
Lactation Usually compatible Pharmacogenetics Those with G6PD deficiency are more likely to develop hemolytic anemia
Contraindications Hypersensitivity to nitrofurantoin, use in neonates or pregnant patients at term (38-42 wk) due to risk of hemolytic anemia, anuria or oliguria Black Box Warnings
None
Medication Safety Issues: Nitrofurantoin
Suffixes No Tall Man Letters No Do Not Crush Do not open capsules
High Alert No Confused Names Nitro-Bid, nitroglycerine, microK, Neurotin, nitroglycerin Beers Criteria Avoid in renal dysfunction and avoid long-term use
Class: Nitrate, Antianginal
Dosage Forms. Oral Capsule, Extended Release: 2.5 mg, 6.5 mg, 9 mg; Sublingual Tablet: 0.3 mg, 0.4 mg, 0.6 mg; Sublingual Packet: 400 mcg; Sublingual Solution:0.4 mg/actuation; Translingual Aerosol Solution: 400 mcg/spray; Transdermal Patch 24 Hour: 0.1 mg/h, 0.2 mg/h, 0.3 mg/h, 0.4 mg/h, 0.6 mg/h, 0.8 mg/h; Transdermal Ointment: 2%; Rectal Ointment: 0.4%
Common FDA Label Indication, Dosing, and Titration.
Angina, prophylaxis: Extended release, 2.5-6.5 mg po tid-qid; sublingual, 1 tab or 1-2 sprays 5-10 min before activity, which may induce angina; transdermal, 0.2-0.4 mg/h worn topically 12-14 h/d, may titrate to 0.8 mg/h worn topically
Angina, acute: Sublingual, 1 tab or 1-2 sprays at first sign of angina, repeat every 5 min if needed for total of 3 tabs or doses in 15 min
Anal fissure, chronic: Intra-anal, 1 inch ointment (equals 1.5 mg of nitroglycerin) q 12 h × 3 wk
Off-Label Uses.
None
MOA. Nitroglycerin is believed to be converted to nitric oxide (NO) by vascular endothelium. NO activates guanylate cyclase, increasing cyclic GMP that in turn decreases intracellular calcium, resulting in direct relaxation of vascular smooth muscle. In myocardial ischemia, nitrates dilate large epicardial vessels, enhance collateral size and flow, and reduce coronary vasoconstriction.
Drug Characteristics: Nitroglycerin
Dose Adjustment Hepatic Not required Absorption F = 38-75%, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 3 L/kg; 60% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, not via CYP
Pregnancy Category C Elimination Renal 22% with a half-life of 1-4 min
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to nitrates, concurrent use with PDEIs, symptomatic hypotension, marked bradycardia or tachycardia, severe anemia or increased intracranial pressure
Black Box Warnings None
Class: Tricyclic Antidepressant
Dosage Forms. Oral Capsule: 10 mg, 25 mg, 50 mg, 75 mg; Oral Solution: 10 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Depression: Adults, initiate at 25 mg po daily and titrate to 25 mg po tid-qid
Off-Label Uses.
Chronic pain: Adults, 10-25 mg once daily at bedtime
Diabetic neuropathy: 10-25 mg po daily, may titrate to 100 mg po daily
MOA. Nortriptyline is the demethylated metabolite of amitriptyline, a heterocyclic antidepressant that blocks presynaptic reuptake of norepinephrine with subsequent downregulation of adrenergic receptors. Heterocyclic antidepressants have less effect on serotonergic activity than on other neurotransmitters.
Drug Characteristics: Nortriptyline
Dose Adjustment Hepatic Not required Absorption F = 46-70%, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 21-31 L/kg; 86-95% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP2D6 substrate
Pregnancy Category C Elimination Renal 2% with a half-life of 14-51 h
Lactation Compatible Pharmacogenetics Caution in CYP2D6 poor metabolizers, or concurrently with CYP2D6 inhibitors
Contraindications Hypersensitivity to nortriptyline or other TCAs; MAOI concurrent use or use within 14 d; use during acute recovery period after MI, patient using linezolid or IV methylene blue
Black Box Warnings Suicidality
Medication Safety Issues: Nortriptyline
Suffixes No Tall Man Letters No Do Not Crush No High Alert No
Confused Names Amitriptyline, Demerol, Bentyl, Desipramine, Norpramin, Tambocor
Beers CriteriaHighly anticholinergic, Orthostatic Hypotension; avoid
Class: Thienobenzodiazepine, Atypical Antipsychotic
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg; Oral Disintegrating Tablet: 5 mg, 10 mg, 15 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Bipolar disorder, acute mixed or manic episodes and maintenance therapy: Adults, 10-15 mg/d po, may titrate in 5 mg/d increments (max 20 mg/d); Children 13-17 y of age, 2.5-5 mg/d po, may titrate in 2.5-5 mg/d increments (max 10 mg/d)
Schizophrenia: Adults, 5-10 mg/d po, may titrate in 5 mg/d increments at 1-wk intervals to 10-20 mg/d po; Children 13-17 y of age, 2.5-5 mg/d po, may titrate in 2.5-5 mg increments (max 10 mg/d)
Depression, treatment resistant, in combination with fluoxetine: Adults, 2.5-20 mg po daily
Off-Label Uses.
Chemotherapy-induced nausea and vomiting: Adults, 10 mg po on day 1 of chemotherapy followed by 10 mg po on days 2-4 in combination with other antiemetics
Tourette syndrome: Adults, 2.5-5 mg po daily, may titrate in 2.5-5 mg increments(max 20 mg/d); Children, 2.5-5 mg/d po, may titrate in 2.5-5 mg/d increments (max 10 mg/d)
MOA. Olanzapine is an atypical antipsychotic agent that is a potent serotonin-5-HT2 and dopamine-D2 antagonist. Antipsychotic effect is most likely related to blockade of postsynaptic dopaminergic receptors in the mesolimbic and prefrontal cortexes of the brain, although other neurotransmitter systems also are involved.
Drug Characteristics: Olanzapine
Dose Adjustment Hepatic Not required, except when used with fluoxetine (limit initial olanzapine dose to 2.5-5 mg daily) Absorption Well absorbed, food has no effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 1000 L; 93% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic via glucuronidation, CYP1A2 substrate
Pregnancy Category C Elimination Renal 57%, fecal 30% with a half-life of 21-54 h (half-life increases with age)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to olanzapine Black Box Warnings Mortality in elderly patients with dementia-related psychosis; DRESS
Medication Safety Issues: Olanzapine
Suffixes Zydis, REIprevv Tall Man Letters ZyPREXA, OLANZapine High Alert
NoConfused NamesCeleXA, ZyrTEC, Olsalazine, QUEtiapine, Reprexain, Zestril, Zelapar, ZolpidemBeers CriteriaStroke risk; avoid except in schizophrenia or bipolar disorder
Class: Antihyperlipidemic, Omega-3 Fatty Acids
Dosage Forms. Oral Capsule, Liquid Filled: 200 mg, 300 mg, 350 mg, 500 mg, 600 mg, 880 mg, 1000 mg, 1050 mg, 1200 mg; Oral Capsule, Delayed Release: 332.5 mg, 1000 mg; Oral Tablet, Chewable: 240 mg
Common FDA Label Indication, Dosing, and Titration.
Hypertriglyceridemia, adjunct to diet in adults with triglyceride levels 500 mg/dL or higher: 4 g po daily or divided into 2 doses
Off-Label Uses.
Coronary arteriosclerosis, hypertriglyceridemia: 4 g po daily or divided into 2 doses
Familial combined hyperlipidemia: 4 g po daily or divided into 2 doses
Heart failure: 4 g po daily or divided into 2 doses
Hyperlipidemia, hypertriglyceridemia, triglyceride levels <500 mg/dL: 4 g po daily or divided into 2 doses
MOA. Potential mechanisms of action include inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase, increased mitochondrial and peroxisomal β-oxidation in the liver, decreased lipogenesis in the liver, and increased plasma lipoprotein lipase activity. Lovaza may reduce the synthesis of triglycerides in the liver because eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are poor substrates for the enzymes responsible for TG synthesis, and EPA and DHA inhibit esterification of other fatty acids.
Drug Characteristics: Omega-3-Acid Ethyl Esters
Dose Adjustment Hepatic Not required Absorption Unknown
Dose Adjustment Renal Not required Distribution Unknown
Dialyzable Unknown Metabolism Oxidized in the liver similar to fatty acids derived from dietary sources; EPA: minor via CYP450
Pregnancy Category C Elimination Half-life (EPA) of approximately 37-89 h, (DHA) approximately 46 h
Lactation Compatible Pharmacogenetics None known
Contraindications Hypersensitivity to omega-3-acid ethyl esters, fish, or shellfish Black Box Warnings None
Class: Proton Pump Inhibitor
Dosage Forms. Oral Capsule, Delayed Release:10 mg, 20 mg, 40 mg; Oral Tablet, Delayed Release: 20 mg; Oral Packet: 2.5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Duodenal ulcer disease: 20 mg po daily × up to 4 wk
Gastric ulcer disease: 40 mg po daily × up to 8 wk
Helicobacter pylori GI infection: 20 mg po bid × 10-14 d in combination with amoxicillin 1000 mg and clarithromycin 500 mg po bid
Erosive esophagitis, GERD: Adults and Children ≥1 y of age and ≥20 kg, 20 mg po daily; Children ≥1 y of age, 5-10 kg, 5 mg po daily; Children ≥1 y of age, 10-20 kg, 10 mg po daily
Off-Label Uses.
Drug-induced GI disturbance, indigestion: 20-40 mg po daily
MOA. Omeprazole is a PPI that, when protonated in the secretory canaliculi of the parietal cells, covalently binds to H+/K+-ATPase (proton pump), which is the final pathway for acid secretion. Produces a profound and prolonged antisecretory effect and inhibits basal, nocturnal, and pentagastrin- and food-stimulated gastric acid secretion.
Drug Characteristics: Omeprazole
Dose Adjustment Hepatic Consider dose adjustment in hepatic impairment Absorption
F = 30-40%, food delays but does not reduce absorption
Dose Adjustment Renal Not required Distribution Vd = 0.34-0.37 L/kg; 95% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, CYP2C19 substrate
Pregnancy Category C Elimination Renal 77% with a half-life of 30-60 min
Lactation Weigh risks and benefits Pharmacogenetics CYP2C19 poor metabolizers have greater gastric acid suppression
Contraindications Hypersensitivity to omeprazole or esomeprazole Black Box Warnings
None
Class: Antiemetic
Dosage Forms. Oral Tablet: 4 mg, 8 mg, 24 mg; Oral Dispersible Tablet: 4 mg, 8 mg; Oral Solution: 4 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Chemotherapy-induced nausea and vomiting, highly emetogenic chemotherapy: 24 mg po 30 min prior to the start of chemotherapy
Chemotherapy-induced nausea and vomiting, moderately emetogenic chemotherapy: Adults and Children >12 y of age, 8 mg po 30 min prior to chemotherapy and repeated in 8 h, then 8 mg po q12h for 1-2 d postchemotherapy; Children 4-11 y of age, 4 mg po 30 min prior to chemotherapy, repeated 4 and 8 h after the 1st dose, then q8h for 1-2 d postchemotherapy
Prevention of postoperative nausea and vomiting: 16 mg po 1 h before anesthesia induction
Radiation-induced nausea and vomiting: 8 mg po 1-2 h prior to radiotherapy and q8h after 1st dose of radiation on each day of radiotherapy
Off-Label Uses.
Severe hyperemesis associated with pregnancy: 8 mg po q12h
MOA. Ondansetron is a selective 5-HT3 receptor antagonist. Serotonin receptors of the 5-HT3 type are present both peripherally and centrally in the chemoreceptor trigger zone. Cytotoxic chemotherapy releases serotonin from the enterochromaffin cells of the small intestine, initiating the vomiting reflex.
Drug Characteristics: Ondansetron
Dose Adjustment Hepatic Severe hepatic dysfunction, max daily dose 8 mg Absorption
F = 56%, food has minimal effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 2.2-2.5 L/kg
Dialyzable Unknown Metabolism Hepatic, CYP3A4/5 substrate
Pregnancy Category B Elimination Renal 5% with a half-life of 3-6 h
Lactation Weigh risks and benefits Pharmacogenetics Consider alternative antiemetic in CYP2D6 ultrarapid metabolizers
Contraindications Hypersensitivity to ondansetron, concomitant apomorphine or drugs that increase QTc interval Black Box Warnings None
Class: Oral Contraceptive
Product Contents: Oral Contraceptive- Monophasic
Estrogen Component : Progestin Component : Example Brand Names
Ethinyl estradiol 50 mcg : Norgestrel 0.5 mg : Ogestrel 0.5/50
Ethinyl estradiol 35 mcg : Norethindrone 1 mg : Ortho-Novum 1/35, Alyacen 1/35
Ethinyl estradiol 35 mcg : Norethindrone 0.5 mg : Brevicon, Wera
Ethinyl estradiol 35 mcg : Norethindrone 0.4 mg : Vyfemla, Balziva
Ethinyl estradiol 30 mcg : Drospirenone 3 mg : Ocella, Yasmin
Ethinyl estradiol 30 mcg : Norethindrone 1.5 mg : Loestrin 21 1.5/30, Junel Fe 1.5/30
Ethinyl estradiol 30 mcg : Norgestrel 0.3 mg : Low-Ogestrel, Cryselle 28
Ethinyl estradiol 30 mcg : Desogestrel 0.15 mg : Apri, Juleber
Ethinyl estradiol 30 mcg : Levonorgestrel 0.15 mg : Levora, Portia
Ethinyl estradiol 20 mcg : Drospirenone 3 mg : Yaz, Loryna
Ethinyl estradiol 20 mcg : Levonorgestrel 0.1 mg : Aviane, Lutera
Ethinyl estradiol 20 mcg : Norethindrone 1 mg : Loestrin Fe 1/20, Junel Fe 1/20
Dosage Forms. Oral Tablet: Monophasic products include tablets that each contains the same fixed ratio of an estrogen and progestin agent; products are either in 21-d or in 28-d cycles; may also include inert tablets containing either plain lactose or iron supplements, generally as 75-mg ferrous fumarate.
Common FDA Label Indication, Dosing, and Titration.
Contraception: 1 tablet po daily beginning either on the 1st Sunday after menstruation begins ("Sunday start") or on the 1st d of menstruation ("day 1 start"); tablets are taken sequentially, following the arrows marked on the dispenser
Off-Label Uses.
None
MOA. See Preface C Card: General Content Related to All Oral Contraceptives.
Class: Oral Contraceptive
Product Contents: Oral Contraceptive- Triphasic
Phase 1 : Phase 2 : Phase 3 : Example Brand Names
Ethinyl estradiol 35 mcg; norethindrone 0.5 mg (7 d) : Ethinyl estradiol 35 mcg; norethindrone 1 mg (9 d) : Ethinyl estradiol 35 mcg; norethindrone 0.5 mg (5 d) : Leena 7/9/5, Aranelle 7/9/5
Ethinyl estradiol 35 mcg; norethindrone 0.5 mg (7 d) : Ethinyl estradiol 35 mcg; norethindrone 0.75 mg (7 d) : Ethinyl estradiol 35 mcg; norethindrone 1 mg (7 d) : Ortho-Novum 7/7/7, Nortrel 7/7/7
Ethinyl estradiol 35 mcg; norgestimate 0.18 mg (7 d) : Ethinyl estradiol 35 mcg; norgestimate 0.215 mg (7 d) : Ethinyl estradiol 35 mcg; norgestimate 0.25 mg (7 d) : Ortho Tri-Cyclen, Tri-Sprintec, TriNessa
Ethinyl estradiol 25 mcg; norgestimate 0.18 mg (7 d) : Ethinyl estradiol 25 mcg; norgestimate 0.215 mg (7 d) : Ethinyl estradiol 25 mcg; norgestimate 0.25 mg (7 d) : Ortho Tri-Cyclen Lo, Tri-Lo-Marzia
Ethinyl estradiol 20 mcg; norethindrone 1 mg (5 d) : Ethinyl estradiol 30 mcg; norethindrone 1 mg (7 d) : Ethinyl estradiol 35 mcg; norethindrone 1 mg (9 d) : Estrostep Fe, Tri-Legest Fe
Dosage Forms. Oral Tablet: Triphasic products contain 3 sets of tablets, each phase containing a combination of varying doses of estrogen/progestin agents; products are either in 21-d or in 28-d cycles; may also include inert tablets containing either plain lactose or iron supplements, generally as 75-mg ferrous fumarate.
Common FDA Label Indication, Dosing, and Titration.
Contraception: 1 tablet po daily beginning either on the 1st Sunday after menstruation begins ("Sunday start") or on the 1st d of menstruation ("day 1 start"); tablets are taken sequentially, following the arrows marked on the dispenser
Acne vulgaris, moderate: In females at least 15 y of age who have achieved menarche and are unresponsive to topical antiacne medications, same dosing as for contraception (Ortho Tri-Cyclen and Estrostep Fe are the only products with this FDA-approved indication)
Off-Label Uses.
None
MOA. See Preface C Card: General Content Related to All Oral Contraceptives.
Class: Neuraminidase Inhibitor, Antiviral
Dosage Forms. Oral Capsule: 30 mg, 45 mg, 75 mg; Oral Suspension: 6 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Influenza virus types A and B, treatment: Children >1 y of age and <15 kg, 30 mg po bid × 5 d; Children >1 y of age and 15-23 kg, 45 mg po bid × 5 d; Children >1 y of age and 23-40 kg, 60 mg po bid × 5 d; Adults and Children >1 y of age and >40 kg, 75 mg po bid × 5 d
Influenza virus types A and B, prophylaxis: Same dose as for treatment; may dose for 6 wk during a community outbreak
Off-Label Uses.
Influenza virus types A and B, prophylaxis: Children >2 wk and <3 mo of age, 3 mg/kg/d for up to 6 wk during community outbreak
MOA. Oseltamivir is an inhibitor of influenza virus neuraminidase affecting release of viral particles.
Drug Characteristics: Oseltamivir
Dose Adjustment Hepatic Not required Absorption F = 75%, food has minimal effect on absorption
Dose Adjustment Renal CrCl = 10-30 mL/min, reduce dose to 30 mg po daily for treatment, 30 mg po qod for prophylaxis; CrCl 30-60 mL/min, reduce dose to 30 mg po bid for treatment, 30 mg po daily for prophylaxis Distribution Vd = 23-26 L; 42% protein bound
Dialyzable Yes Metabolism Oseltamivir phosphate is a prodrug that is extensively metabolized to oseltamivir carboxylate by ester hydrolysis
Pregnancy Category C Elimination Renal 99%, with a half-life of 1-3 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to oseltamivir Black Box Warnings None
Class: Dibenzazepine Carboxamide, Anticonvulsant
Dosage Forms. Oral Tablet: 150 mg, 300 mg, 600 mg; Oral Tablet, Extended Release 24 h: 150 mg, 300 mg, 600 mg; Oral Suspension: 300 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Partial seizure: Adults, 300 mg po bid, may titrate to 1200-2400 mg/d po (depending on formulation); Children 4-16 y of age, 8-10 mg/kg/d po in 2 divided doses, may titrate to 600 mg/d po; Children <4 y of age and <20 kg, 16-20 mg/kg/d po in 2 divided doses, may titrate to a max 60 mg/kg/d
Off-Label Uses.
Trigeminal neuralgia: 300 mg po bid-qid, may titrate to 2400 mg po daily
MOA. Oxcarbazepine is a 10-keto analogue of carbamazepine that exerts its anticonvulsant effect through an active 10-monohydroxy metabolite (MHD). Its mechanism of action is not known but likely involves blockade of voltage-dependent sodium channels and inhibition of repetitive neuronal firing.
Drug Characteristics: Oxcarbazepine
Dose Adjustment Hepatic Avoid extended release product in severe hepatic impairment Absorption F = 90%, food has no effect on absorption
Dose Adjustment Renal CrCl <30 mL/min, initiate at 50% of the usual dose and increase slowly
Distribution Vd = 49 L; 40-60% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic via, CYP3A4/5; inducer of CYP3A4/5, inhibitor of CYP2C19
Pregnancy Category C Elimination Renal >95% with a half-life of 2 h (immediate release), 8-13 h (extended release)
Lactation Weigh risks and benefits Pharmacogenetics Use alternative anticonvulsant in HLA-A31:01 positive or HLA-B15:02 positive patient, increased risk of Stevens-Johnson syndrome
Contraindications Hypersensitivity to oxcarbazepine Black Box Warnings None
Medication Safety Issues: Oxcarbazepine
Suffixes XR Tall Man Letters Oxcarbazepine Do Not Crush Extended-Release Tablets High Alert No Confused Names CarBAMazepine
Beers CriteriaAvoid in certain circumstances
Class: Opioid Analgesic. C-II
Dosage Forms. Oral Capsule: 5 mg; Oral Tablet, Immediate Release: 5 mg, 10 mg, 15 mg, 20 mg, 30 mg; Oral Tablet, Extended Release 12 h Abuse-Deterrent: 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg; Oral Capsule 12 h Abuse-Deterrent: 9 mg, 13.5 mg, 18 mg, 27 mg, 36 mg; Oral Solution: 5 mg/5 mL; Oral Concentrate: 100 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Pain, chronic, moderate to severe: Initial dose for opioid-naïve patient, immediate release, 5-15 mg po q4-6h prn pain; extended release, 10 mg po q12h prn pain; titrate to response
Off-Label Uses.
None
MOA. Oxycodone is pure mu agonist. Mu receptors are responsible for analgesia, respiratory depression, miosis, decreased GI motility, and euphoria. In the CNS, it promotes analgesia and respiratory depression by decreasing the brain stem respiratory centers' response to carbon dioxide tension and electrical stimulation. It also decreases gastric, biliary, and pancreatic secretion, induces peripheral vasodilation, and promotes opioid-induced hypotension due to histamine release.
Drug characteristics: Oxycodone
Dose Adjustment Hepatic Immediate release, initiate with low does and titrate with caution; extended release, initiate at one-third to one-half usual dose and titrate with caution Absorption
F = 60-87%; absorption enhanced by food
Dose Adjustment Renal CrCl <60 mL/min, reduce starting dose Distribution Vd = 2.6 L/kg; 45% protein bound
Dialyzable Unknown Metabolism Hepatic, CYP3A4/5 substrate
Pregnancy Category B Elimination Renal 20% with a half-life of 3-4 h (immediate release), 5-18 h (extended release)
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to oxycodone or other opioids, asthma, paralytic ileus, respiratory depression, hypercarbia Black Box Warnings Addiction, abuse potential; REMS, respiratory depression, accidental ingestion, neonatal withdrawal, CYP3A4/5 interaction, concurrent use with benzodiazepines, medication errors with oral solution
Class: Antipsychotic (Atypical)
Dosage Forms. Oral Tablet: 25 mg, 50 mg, 100 mg, 200 mg, 300 mg, 400 mg; Oral Tablet, Extended Release: 50 mg, 150 mg, 200 mg, 300 mg, 400 mg
Common FDA Label Indication, Dosing, and Titration.
Bipolar disorder or schizophrenia, therapy initiation: Adults, immediate release, 50 mg po bid × 1 d, increase 50 mg/d × 3 d, may titrate to 800 mg/d; Adults, extended release, 300 mg po hs × 1 d, then 600 mg po hs × 1 d, may titrate to 800 mg/d; Children 10-17 y of age, immediate release, 50 mg po × 1 d, then 100 mg po × 1 d, then 200 mg po × 1 d, then 300 mg po × 1 d, then 400 mg po × 1 d, may titrate to 600 mg/d
Bipolar disorder or schizophrenia, maintenance: Adults, immediate release: 400-800 mg/d po; Adults, extended release, 400-800 mg/d po; Children 10-17 y of age, regular release, titrate to lowest effective dose
Major depressive disorder, adjunct to antidepressants: Adults, extended release, 50 mg po daily hs, may titrate to 300 mg/d
Off-Label Uses.
Delirium in the critically ill: Adults, extended release, 50 mg po daily hs, may titrate to 300 mg/d
MOA. Quetiapine is an antagonist at multiple neurotransmitter receptors in the brain. It antagonizes serotonin 5-HT1A and 5-HT2, dopamine D1 and D2, histamine H1, and adrenergic α1 and α2 receptors. Efficacy in schizophrenia and bipolar disorder is due to the antagonism of a combination of D2 and 5-HT2 receptors.
Drug Characteristics: Quetiapine
Dose Adjustment Hepatic Regular release, initiate at 25 mg po daily; extended release, initiate at 50 mg po daily Absorption F = 9%, Cmax and AUC of extended-release tablet increased by high-fat meal
Dose Adjustment Renal Not required Distribution Vd = 6-14 L/kg; 83% protein bound
Dialyzable Not dialyzable Metabolism Hepatic via CYP3A4/5
Pregnancy Category C Elimination Renal 73% with a half-life of 6-7 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to quetiapine Black Box Warnings Mortality in elderly with dementia, suicidality, not approved for children <10 y
Class: Proton Pump Inhibitor
Dosage Forms. Oral Tablet, Delayed Release: 20 mg; Oral Capsule, Sprinkle: 5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Duodenal ulcer disease: 20 mg po daily × up to 4 wk
Helicobacter pylori GI infection: 20 mg po bid × 10-14 d in combination with amoxicillin 1000 mg and clarithromycin 500 mg po bid
Gastric hypersecretion: 60 mg po daily, may titrate to 60 mg po bid
GERD, erosive or ulcerative, for symptom control, initial treatment, or maintenance: Adults and Children >12 y of age, 20 mg po daily
Off-Label Uses.
Drug-induced GI disturbance, indigestion: 20 mg po daily
Gastric ulcer disease: 20-40 mg po daily
MOA. Rabeprazole is a proton pump inhibitor (PPI) that, when protonated in the secretory canaliculi of the parietal cells, covalently binds to H+/K+-ATPase (proton pump), which is the final pathway for acid secretion. Rabeprazole produces a profound and prolonged antisecretory effect and inhibits basal, nocturnal, and pentagastrin- and food-stimulated gastric acid secretion.
Drug Characteristics: Rabeprazole
Dose Adjustment Hepatic Required for hepatic dysfunction Absorption F = 52%, food delays absorption
Dose Adjustment Renal Not required Distribution 96% protein bound
Dialyzable Not dialyzable Metabolism Hepatic, substrate for CYP3A4/5, 2C19; moderate inhibitor of CYP2C8
Pregnancy Category B Elimination Renal 90% with a half-life of 1-2 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2C19 poor metabolizers have greater gastric acid suppression
Contraindications Hypersensitivity to rabeprazole Black Box Warnings None
Class: ACE-I, Antihypertensive
Dosage Forms. Oral Capsule: 1.25 mg, 2.5 mg, 5 mg, 10 mg
Common FDA Label Indication, Dosing, and Titration.
Heart failure post-MI: 1.25-2.5 mg po bid × 7 d, may titrate to 5 mg po bid
Hypertension: 2.5 mg po daily, may titrate to 2.5-20 mg po daily
Reduce risk of myocardial infarction, stroke, and death from cardiovascular causes: 2.5 mg po bid × 7 d, may titrate as tolerated to 10 mg daily
Off-Label Uses.
Diabetic nephropathy, kidney disease: 1.25-10 mg po daily
MOA. Ramipril is a competitive ACE-I. It is also a prodrug for the more potent ACE-I ramiprilat. ACE-I prevents conversion of angiotensin I to angiotensin II (a vasoconstrictor). It also reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, and inhibits the tissue renin-angiotensin system.
Drug Characteristics: Ramipril
Dose Adjustment Hepatic Not required Absorption F = 60%, food has no effect on absorption
Dose Adjustment Renal CrCl <40 mL/min: use 25% of normal dose, max 5 mg/d Distribution 73% protein bound
Dialyzable Yes Metabolism Hepatic to active metabolite (ramiprilat), not via CYP450
Pregnancy Category C (1st trimester), D (2nd and 3rd trimesters) Elimination Renal 50-60% with a half-life of 13-17 h (metabolite)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to ramipril or other ACE-Is, history of ACE-I-induced angioedema; concurrent sacubitril Black Box Warnings Pregnancy
Medication Safety Issues: Ramipril
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No Capsule No Amaryl, enalapril No
Class: Bisphosphonate
Dosage Forms. Oral Tablet: 5 mg, 30 mg, 35 mg, 150 mg; Oral Tablet, Delayed Release: 35 mg
Common FDA Label Indication, Dosing, and Titration.
Postmenopausal osteoporosis: Delayed release, 35 mg po once weekly immediately following breakfast; immediate release, 5 mg po daily, 35 mg po once weekly, or 150 mg po once a month; all with supplemental calcium and vitamin D
Paget disease: Immediate release, 30 mg po daily for 2 mo
Osteoporosis (glucocorticoid induced) prevention and treatment: Immediate release, 5 mg po daily
Osteoporosis (male): Immediate release, 35 mg po once weekly
Off-Label Uses.
None
MOA. Risedronate binds to bone hydroxyapatite and inhibits osteoclast activity at the cellular level, thereby modulating bone metabolism.
Drug Characteristics: Risedronate
Dose Adjustment Hepatic Not required Absorption F <1%, food impairs absorption, take 30-60 min prior to meal
Dose Adjustment Renal CrCl <30 mL/min, avoid Distribution Vd = 13.8 L; 24% protein bound
Dialyzable Unknown Metabolism Not metabolized
Pregnancy Category C Elimination Renal 50% with a half-life of 561 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Known hypersensitivity to risedronate, esophageal abnormalities that delay esophageal emptying, hypocalcemia, inability to sit or stand upright for at least 30 min Black Box Warnings None
Medication Safety Issues: Risedronate
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No Tablet, ER tablet No Alendronate, Actos No
Class: Benzisoxazole, Antipsychotic
Dosage Forms. Oral Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg; Oral Dispersible Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg; Oral Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Autistic disorder, irritability: Children ≥5 y of age and weighing <20 kg, 0.25 mg po daily, titrate to response; Children ≥5 y of age and weighing>20 kg, 0.5 mg po daily, titrate to response
Acute manic or mixed episodes of bipolar I disorder: Adults, 2-3 mg po daily, may titrate to 6 mg/d or 25-50 mg IM every 2 wk; Children ≥10 y of age, 0.5 mg po daily, may titrate to 6 mg/d
Schizophrenia: Adults, 1 mg po bid, may titrate to 18 mg/d or 25-50 mg IM every 2 wk; Children ≥13 y of age, 0.5 mg po daily, may titrate to 6 mg/d
Off-Label Uses.
Posttraumatic stress disorder: 0.5-8 mg po daily
Tourette syndrome: 0.25-0.5 mg po daily, may titrate to max dose 6 mg po daily
MOA. Risperidone is a potent serotonin-5-HT2 antagonist with weaker dopamine-D2 antagonism. Whereas typical antipsychotics are dopamine antagonists, the additional serotonin antagonism increases efficacy for negative symptoms of schizophrenia and reduces the likelihood of extrapyramidal symptoms.
Drug Characteristics: Risperidone
Dose Adjustment Hepatic Severe hepatic impairment, initiate at 0.5 mg po bid, titrate slowly Absorption F = 70%, food has no effect on absorption
Dose Adjustment Renal Severe renal impairment, initiate at 0.5 mg po bid, titrate slowly Distribution Vd = 1-2 L/kg; 90% protein bound
Dialyzable Not dialyzable Metabolism Hepatic via CYP2D6, to active metabolite (9-hydroxyrisperidone), p-glycoprotein substrate
Pregnancy Category C Elimination Renal 70% with a half-life of 3-20 h
Lactation Weigh risks and benefits Pharmacogenetics CYP2D6 poor metabolizers have higher risperidone and lower metabolite levels; limited clinical implication as both parent and metabolite are active
Contraindications Hypersensitivity to risperidone, agents that increase QT interval Black Box Warnings Mortality in elderly with dementia, DRESS
Medication Safety Issues: Risperidone
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
Consta, M-TabRisperiDONE, RisperDALDispersible tabletNoReserpine, rOPINIRoleStroke risk; avoid except in schizophrenia or bipolar disorder
Class: Anticoagulant, Factor Xa inhibitor
Dosage Forms. Oral Tablet: 2.5 mg, 10 mg, 15 mg, 20 mg
Common FDA Label Indication, Dosing, and Titration.
Prevention of thromboembolism in patients after orthopedic surgery: 10 mg po daily beginning at least 6 h after surgery × 12-14 d for knee replacement or 35 d for hip replacement; if CrCl 30-50 mL/min no dose adjustment, use with caution; do not use if CrCl <30 mL/min
Prevention of thromboembolism in patients with nonvalvular atrial fibrillation: 20 mg po daily if CrCl >50 mL/min; 15 mg po daily if CrCl 15-50 mL/min; do not use if CrCl <15 mL/min
Treatment and secondary prevention of DVT or pulmonary embolism: 15 mg po bid × 21 d, then 20 mg po daily; do not use if CrCl <30 mL/min
Coronary artery disease (stable) or peripheral artery disease: 2.5 mg po bid
Off-Label Uses.
Acute coronary syndrome: 2.5 mg po bid
MOA. Rivaroxaban is an orally bioavailable factor Xa inhibitor that selectively blocks the active site of factor Xa and does not require a cofactor (such as anti-thrombin III) for activity. Activation of factor X to factor Xa via the intrinsic and extrinsic pathways plays a central role in the cascade of blood coagulation.
Drug Characteristics: Rivaroxaban
Dose Adjustment Hepatic Avoid use in moderate to severe dysfunction Absorption F = 66-100%; food increases extent of absorption at higher doses
Dose Adjustment Renal Dose adjustments based on indication, see above Distribution Vd = 50 L; 95% albumin bound
Dialyzable Use in ESRD should be avoided; hemodialysis removes 60% of drug in 2-3 h Metabolism Hepatic via CYP3A4/5, p-glycoprotein substrate
Pregnancy Category C Elimination Renal 66% with a half-life of 5-9 h
Lactation Weigh risks and benefits Pharmacogenetics Factor V Leiden; similar efficacy and safety to those without mutation
ContraindicationsActive bleedingBlack Box WarningsPremature discontinuation increases thrombotic risk, risk of spinal/epidural hematoma
Class: Dopamine Agonist
Dosage Forms. Oral Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg, 5 mg; Oral Tablet, Extended Release 24 h: 2 mg, 4 mg, 6 mg, 8 mg, 12 mg
Common FDA Label Indication, Dosing, and Titration.
Parkinson disease: Immediate release, 0.25 mg po tid × 1 wk, then 0.5 mg po tid × 1 wk, then 0.75 mg po tid × 1 wk, then 1 mg po tid, then may titrate to 24 mg/d; extended release, 2 mg po daily × 1-2 wk, then may titrate to 24 mg/d
Restless legs syndrome: Immediate release only, 0.25 mg po daily hs × 2 d, then 0.5 mg po daily hs × 5 d, then 1 mg po daily × 1 wk, then 1.5 mg po daily hs for 1 wk, then 2 mg po daily hs, then may titrate to 4 mg po daily hs
Off-Label Uses.
None
MOA. Ropinirole is a nonergoline dopamine agonist that has a higher specificity to D3 than to D2 and D4 subtypes of dopamine receptors. The drug has a moderate affinity for opioid receptors and has insignificant effects on D1, 5-hydroxytryptamine 1 (5-HT1), 5-HT2, benzodiazepine, GABA, muscarinic, α1-, α2-, and β-adrenoreceptors. It is suggested that ropinirole stimulates the postsynaptic D2-type receptor found in the brain's caudate putamen in Parkinson disease.
Drug Characteristics: Ropinirole
Dose Adjustment Hepatic Use with caution Absorption F = 45-55%, food increases Tmax and Cmax
Dose Adjustment Renal Lower maximum dose in patients on dialysis Distribution Vd = 7.5 L/kg; 40% protein bound
Dialyzable Unknown Metabolism Hepatic via CYP1A2
Pregnancy Category C Elimination Renal >80% with a half-life of 6 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity to ropinirole Black Box Warnings None
Medication Safety Issues: Ropinirole
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
XLrOPINIRoleExtended-release tabletsNoRisperDAL, risperiDONE
Class: HMG-CoA Reductase Inhibitor
Dosage Forms. Oral Tablet: 5 mg, 10 mg, 20 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
Hyperlipidemia: Adults, 10-20 mg po daily, may titrate to 40 mg po daily; Children 10-17 y of age, 5-20 mg po daily, may titrate to 20 mg po daily
Disorder of cardiovascular system, primary prophylaxis, familial hypercholesterolemia, homozygous, hypertriglyceridemia, mixed dyslipidemia: 10-20 mg po daily, may titrate to 40 mg po daily
Off-Label Uses.
None
MOA. HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol can also decrease because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
Drug Characteristics: Rosuvastatin
Dose Adjustment Hepatic Use with caution; contraindicated in active liver disease or unexplained increased LFTs Absorption F = 20%, food slows absorption
Dose Adjustment Renal CrCl <30 mL/min, initial dose 5 mg po daily, may titrate to 10 mg po daily Distribution Vd = 134 L; 88% protein bound
Dialyzable Not dialyzable Metabolism Minimal hepatic
Pregnancy Category X Elimination Fecal 90% with a half-life of 13-20 h
Lactation Contraindicated Pharmacogenetics SLCO1B1 poor metabolizers with high rosuvastatin concentrations; clinical significance unknown
Contraindications Hypersensitivity to rosuvastatin, active liver disease, pregnancy or lactation Black Box Warnings None
Medication Safety Issues: Rosuvastatin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No atorvaSTATin No
Class: Neprilysin Inhibitor, Angiotensin II Receptor Antagonist
Dosage Forms. Oral Tablet: (Sacubitril/Valsartan) 24 mg/26 mg, 49 mg/51 mg, 97 mg/103 mg
Common FDA Label Indication, Dosing, and Titration.
Heart failure with reduced ejection fraction: Sacubitril 49 mg/valsartan 51 mg po bid, may titrate to sacubitril 97 mg/valsartan 103 mg po bid
Off-Label Uses.
None
MOA. Sacubitril is a prodrug that inhibits neprilysin through the active metabolite LBQ657, leading to increased levels of peptides, including natriuretic peptides. Valsartan is a selective, reversible, competitive antagonist of the angiotensin II receptor, which is responsible for the physiologic effects of angiotensin II, including vasoconstriction, aldosterone secretion, sympathetic outflow, and stimulation of renal sodium reabsorption.
Drug Characteristics: Sacubitril/Valsartan
Dose Adjustment Hepatic Moderate, sacubitril 24 mg/valsartan 26 mg twice daily; severe, avoid Absorption Sacubitril, F >60%; Valsartan, F = 25%, food does not affect absorption
Dose Adjustment Renal eGFR <30 mL/min/1.73 m2: sacubitril 24 mg/valsartan 26 mg twice daily Distribution Sacubitril, Vd = 103 L; Valsartan, Vd = 75 L; 95% protein bound
Dialyzable Unknown Metabolism Sacubitril, converted to active metabolite by esterases; Valsartan, minimal liver metabolism
Pregnancy Category Can cause injury or death to developing fetus. Discontinue if pregnancy occurs Elimination Sacubitril, renal 52-68%, bile 40% with a half-life of 11.5 h; Valsartan, renal 7-13%, bile 89% with a half-life of 6-9 h
Lactation Avoid Pharmacogenetics None known
Contraindications Hypersensitivity, history of angioedema, pregnancy, concomitant ACE inhibitors, aliskiren Black Box Warnings
Class: SSRI Antidepressant
Dosage Forms. Oral Tablet: 25 mg, 50 mg, 100 mg; Oral Concentrate: 20 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Depression: 50 mg po daily, may titrate to 200 mg/d
OCD: Children 6-12 y of age, 25 mg po daily, may titrate to 200 mg/d; Children 13-17 y of age and Adults, 50 mg po daily, may titrate to 200 mg/d
Panic disorder, posttraumatic stress disorder, social phobia disorder: 25 mg po daily for 1 wk, then titrate to 50 mg po daily, may titrate to 200 mg/d
Premenstrual dysphoric disorder: 50 mg po daily continuously or only during luteal phase, may titrate to 100 mg/d
Off-Label Uses.
Binge eating disorder: 25 mg po daily after lunch × 3 d, then titrate to 50 mg po daily, may titrate to 200 mg/d
Bulimia nervosa: 50 mg po daily for 1 wk, may titrate to 200 mg/d
Generalized anxiety disorder: 25 mg po daily for 1 wk, may titrate to 200 mg/d
MOA. Sertraline is an SSRI that indirectly results in a downregulation of β-adrenergic receptors. It has no clinically important effect on noradrenergic or histamine receptors and no effect on MAO. It lacks stimulant, cardiovascular, anticholinergic, and convulsant effects.
Drug Characteristics: Sertraline
Dose Adjustment Hepatic Lower dose or dose less frequently Absorption F = 100%, food has minimal effect on absorption
Dose Adjustment Renal Not required Distribution Vd = 20 L/kg; 99% protein bound
Dialyzable Not dialyzable Metabolism Extensive hepatic via CYP2D6 to 1 active metabolite; CYP2D6 substrate; moderate inhibitor of CYP2B6, 2C19, and 2D6
Pregnancy Category Weigh risks and benefits Elimination Renal 40-45% with a half-life of 24 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to sertraline; concomitant use of pimozide, thioridazine, or MAOIs Black Box Warnings Suicidality, not approved for depression in children; approved for OCD in children >6 y
Class: Erectile Dysfunction Agent, Pulmonary Hypertension Agent
Dosage Forms. Oral Tablet: 20 mg, 25 mg, 50 mg, 100 mg; Oral Suspension: 10 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Erectile dysfunction: 25-100 mg po prn 1 h prior to anticipated sexual activity
Pulmonary hypertension (WHO group I): 5-20 mg po tid
Off-Label Uses.
Pulmonary hypertension (WHO group II-IV): 5-20 mg po tid
MOA. Inhibition of phosphodiesterase type 5 (PDE5) by sildenafil increases the amount of cyclic guanosine monophosphate (GMP) enhancing erectile function and pulmonary vasculature relaxation. Penile erection during sexual stimulation is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum and vasodilation in the pulmonary bed.
Drug Characteristics: Sildenafil
Dose Adjustment Hepatic Avoid use in severe liver disease Absorption F = 41%, food has minimal effect on absorption
Dose Adjustment Renal CrCl <30 mL/min, 25 mg po if used for ED. Not required for pulmonary artery hypertension (PAH) Distribution Vd = 105 L; 96% protein bound
Dialyzable Unknown Metabolism Hepatic via CYP3A4/5
Pregnancy Category Avoid Elimination Renal 13% with a half-life of 4 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to phosphodiesterase inhibitors, concurrent nitrates, concurrent HIV protease inhibitors when used for treating pulmonary hypertension, concurrent guanylate cyclase stimulators
Class: HMG-CoA Reductase Inhibitor
Dosage Forms. Oral Tablet: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg; Oral Suspension: 20 mg/5 mL, 40 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Hyperlipidemia: 20-40 mg po daily in the evening
Primary and secondary preventions of atherosclerotic cardiovascular disease: 20-40 mg po daily in the evening
Secondary prevention of cardiovascular events: 5-40 mg po daily in the evening
Familial hypercholesterolemia (homozygous): Children (boys and postmenarchal girls 10-17 y of age), 10 mg po daily, may titrate to 40 mg po daily in the evening; Adults, 20-40 mg po daily in the evening
Off-Label Uses.
None
MOA. HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol also can decrease because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
Drug Characteristics: Simvastatin
Dose Adjustment Hepatic Contraindicated in active liver disease Absorption F <5%
Dose Adjustment Renal Severe renal impairment, initiate at 5 mg po daily Distribution 95% protein bound
Dialyzable Unknown Metabolism Extensive hepatic into 3 active metabolites; CYP3A4/5 substrate
Pregnancy Category X Elimination Fecal 60% with a half-life of 2 h
Lactation Contraindicated Pharmacogenetics None known
Contraindications Hypersensitivity to simvastatin, active liver disease, pregnancy and lactation Black Box Warnings None
Medication Safety Issues: Simvastatin
Suffixes Tall Man Letters Do Not Crush High Alert Confused Names Beers Criteria
No No No No Zoloft, ZyrTEC atorvaSTATin No
Class: Polymerase Inhibitor (Anti-HCV)
Dosage Forms. Oral Tablet: 400 mg
Common FDA Label Indication, Dosing, and Titration.
Chronic hepatitis C (CHC) infection with genotype 1, 2, 3, 4 as part of combination therapy: 400 mg po once daily, in combination with ribavirin or ribavirin and peginterferon alfa. Duration varies by CHC genotype. Guidelines for HCV treatment are constantly evolving. Refer to AASLD-IDSA recommendations for testing, managing, and treating hepatitis C at http://www.hcvguidelines.org for most recent dosing guidance
Off-Label Uses.
None
MOA.A direct-acting antiviral agent against the hepatitis C virus. It inhibits HCV NS5B RNA-dependent RNA polymerase, essential for viral replication, and acts as a chain terminator.
Drug Characteristics: Sofosbuvir
Dose Adjustment Hepatic Not required Absorption F is unknown; food has no effect on Cmax or AUC
Dose Adjustment Renal Primary metabolite accumulates in renal dysfunction, but no dose adjustments are required Distribution Protein binding 61-65%
Dialyzable Yes, hemodialysis Metabolism Hepatic, P-glycoprotein substrate
Pregnancy Category Contraindicated in combination with ribavirin Elimination Renal 78% (active metabolite) with a half-life of 0.4 h (parent compound), 27 h (active metabolite)
Lactation Not recommended Pharmacogenetics HCV genotype determines treatment regimen; IFNL3 (IL28B) predicts response to interferon if used in regimen
Contraindications Because of ribavirin risk, do not use in pregnant women, or men whose female partners are pregnant Black Box Warnings
Class: Potassium-Sparing Diuretic; Selective Aldosterone Blocker
Dosage Forms. Oral Tablet: 25 mg, 50 mg, 100 mg; Oral Suspension: 25 mg/5 mL
Common FDA Label Indication, Dosing, and Titration.
Heart failure, NYHA class III-IV: 12.5-25 mg po daily, may titrate to max 50 mg
Edema associated with heart failure: 100 mg po daily in single or divided doses, may titrate to 400 mg/d
Nephrotic syndrome: 100 mg po daily in single or divided doses, may titrate to 400 mg/d
Hypertension: 50-100 mg po daily in single or divided doses, may titrate to 400 mg/d
Hypokalemia: 25-100 mg po daily
Off-Label Uses.
Ascites, cirrhosis of liver: 100 mg po daily in single or divided doses, may titrate to 400 mg/d
Acne vulgaris: 50-200 mg po daily
Hirsutism: 50-200 mg po daily for 20 d/mo
MOA. Spironolactone is a steroidal competitive aldosterone antagonist that acts from the interstitial side of the distal and collecting tubular epithelium to block sodium-potassium exchange, producing a delayed and mild diuresis. The diuretic effect is maximal in states of hyperaldosteronism. Excretion of sodium and chloride excretion is increased; excretion of potassium and magnesium is decreased. Spironolactone has mild antihypertensive activity and has demonstrated a beneficial effect in NYHA class III and IV heart failure.
Drug Characteristics: Spironolactone
Dose Adjustment Hepatic Alternate-day dosing may be considered Absorption F = 73%, food increases absorption
Dose Adjustment Renal CrCl <30 mL/min, not recommended Distribution 90% protein bound
Dialyzable Not dialyzable Metabolism Hepatic to active metabolites
Pregnancy Category Use alternative agents Elimination Renal 47-57% with a half-life of 1.4 h
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to spironolactone, anuria, acute renal insufficiency, hyperkalemia Black Box Warnings
Class: Antimigraine Serotonin Receptor Agonist
Dosage Forms. Oral Tablet: 25 mg, 50 mg, 100 mg; Nasal Solution: 5 mg/actuation; Patch, Transdermal: 6.5 mg/4 h; Exhaler Powder, Nasal: 11 mg per nosepiece; Solution, for Subcutaneous Injection: 3 mg/0.5 mL, 4 mg/0.5 mL, 6 mg/0.5 mL
Common FDA Label Indication, Dosing, and Titration.
Migraine: Oral, 25-100 mg po at onset of migraine, may repeat after 2 h prn; max 200 mg/d; Nasal, 5-20 mg in 1 nostril, may repeat after 2 h; max 40 mg/d; sq, 6 mg sq; max 12 mg/d; Transdermal, apply 1 patch, may apply a 2nd after 2 h; max 2 patches/d
Cluster headaches: 6 mg sq once; max 12 mg/d
Off-Label Uses.
None
MOA. Sumatriptan binds with high affinity to serotonin (5HT) subtypes 1B, 1D, and 1F receptors. It has no significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of pro-inflammatory neuropeptide release.
Drug Characteristics: Sumatriptan
Dose Adjustment Hepatic Hepatic dysfunction, max single dose 50 mg Absorption F = 15%, high-fat meal increases F
Dose Adjustment Renal Not required Distribution Vd = 2.4 L/kg; 14-21% protein bound
Dialyzable Unknown Metabolism Hepatic via monoamine oxidase
Pregnancy Category C Elimination Renal 60% with a half-life of 2.5 h
Lactation Usually compatible Pharmacogenetics None known
Contraindications Hypersensitivity to sumatriptan, cerebrovascular syndromes, hemiplegic or basilar migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled hypertension, MAOIs, ergot alkyloids