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USMLE Complete Drugs
Terms in this set (194)
Monoclonal antibody to the platelet glycoprotein IIb/IIIa receptor that binds fibrin. Used to prevent clotting after coronary angioplasty and in acute coronary syndrome. Eptifibatide and tirofiban act similarly
Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti-inflammatory. Less GI distress than aspirin but dangerous in overdose. Tox: hepatic necrosis. Antidote: N-acetylcysteine.
Diuretic inhibits carbonic anhydrase in the proximal tubule; self- limited diuresis due to bicarbonate depletion. Used in glaucoma and mountain sickness. Dorzolamide and brinzolamide used topically for glaucoma.
Cholinomimetic prototype: transmitter in CNS, ENS, all ANS ganglia, parasympathetic postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and skeletal muscle endplate synapses.
Antiviral: inhibits DNA synthesis in herpes simplex virus (HSV) and varicella-zoster virus (VZV). Activated by viral thymidine
kinase (TK- strains are resistant). Tox: nephrotoxicity (crystalluria). Famciclovir, penciclovir, and valacyclovir are similar but with longer half-lives.
Antiarrhythmic: unclassified (miscellaneous group); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10-15 s. Used for nodal reentry arrhythmias. Tox: hypotension, flushing, chest pain
Typical beta-2 agonist; important use in asthma. Tox: tachycardia, arrhythmias, tremor. Other drugs with similar action: metaproterenol, salmeterol, terbutaline.
Bisphosphonate; stabilizes bone structure and increases bone mineral density. Used in postmenopausal and steroid-induced osteoporosis. Tox: esophageal ulceration. Other bisphosphonates (eg, etidronate, pamidronate) are used in Paget's disease.
Antigout: suicide inhibitor of xanthine oxidase; reduces production of uric acid. Used in gout and adjunctively in cancer chemotherapy.
Benzodiazepine sedative-hypnotic: used in anxiety states. Tox: psychological and physiologic dependence, additive effects with other CNS depressants.
Thrombolytic: human recombinant tissue plasminogen activator. Used in acute MI (to recanalize the occluded coronary artery), pulmonary embolism, stroke. Tox: bleeding.
K+-sparing diuretic: blocks Na+ channels in cortical collecting tubules.Tox: hyperkalemia.
Class III (and other classes) antiarrhythmic: broad spectrum; blocks sodium, potassium, calcium channels, beta receptors. High efficacy and very long half-life (weeks to months). Tox: deposits in tissues; skin coloration; hypo- or hyperthyroidism; pulmonary fibrosis.
Penicillin: wider spectrum than penicillin G with activity similar to ampicillin but greater oral bioavailability; fewer adverse effects on GI tract than ampicillin. Susceptible to penicillinases unless used with clavulanic acid. Tox: penicillin allergy.
Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability. Used in attention deficit hyperactivity disorder, for short-term weight loss, and for narcolepsy. Tox: psychosis, HTN, MI, seizures. Other indirect- acting sympathomimetics: ephedrine, pseudoephedrine.
Antifungal: polyene drug of choice for some systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability. Tox: chills and fever, hypotension, nephrotoxicity (dose limiting; less with liposomal forms).
Penicillin: wider spectrum than penicillin G, susceptible to penicillinases unless used with sulbactam. Activity similar to that of penicillin G, plus E coli, H influenzae, P mirabilis, Shigella. Synergy with aminoglycosides versus Enterococcus and Listeria. Tox: penicillin allergy; more adverse effects on GI tract than other penicillins; maculopapular skin rash.
Prototype aromatase inhibitor used in estrogen-dependent cancers (eg, breast cancer). Letrozole is similar.
NSAID prototype: inhibits cyclooxygenase (COX)-1 and -2 irreversibly. Antiplatelet agent as well as antipyretic, analgesic and anti-inflammatory drug. Tox: GI ulcers, allergy, bronchoconstriction, salicylism. Other NSAIDs: ibuprofen, indomethacin, ketorolac, naproxen, and piroxicam
Beta1 selective blocker: low lipid solubility, less CNS effect; used for HTN. (Names of b1 selective blockers start with A through M except for carteolol, carvedilol, and labetalol.) Tox: asthma, bradycardia, AV block, heart failure.
Muscarinic cholinoceptor blocker prototype: lipid-soluble, CNS effects. Tox: "red as a beet, dry as a bone, blind as a bat, mad as a hatter," urinary retention, mydriasis.
Macrolide antibiotic: similar to erythromycin but greater activity against H influenzaenfluenzae,, chlamydiae, and streptococci; long half-life because of tissue accumulation; renal elimination. Tox: GI distress but no inhibition of drug metabolism. Clarithromyin is similar but has a shorter half-life, inhibits drug metabolism, and is contraindicated in pregnancy.
GABA analog, orally active: spasmolytic; activates GABA-B receptors in the spinal cord.
Centrally acting antimuscarinic prototype for parkinsonism. Tox: excess antimuscarinic effects.
Toxins produced by Clostridium botulinum ; enzymes that cleave nerve terminal proteins (synaptobrevin, others) and block release of acetylcholine from vesicles. Injected to treat dystonia, smooth wrinkles, and reduce excessive sweating. Tox: neuromuscular paralysis.
Ergot derivative: prototype dopamine agonist in CNS; inhibits prolactin release. Alternative drug in parkinsonism and hyperprolactinemia. Tox: CNS, dyskinesias, hypotension. Pergolide is similar.
Long-acting amide local anesthetic prototype: Tox: greater cardiovascular toxicity than most local anesthetics.
Anxiolytic: partial agonist that interacts with 5-HT1A receptors; slow onset (1-2 weeks). Minimal potentiation of CNS depressants, including ethanol; negligible abuse liability.
Angiotensin-converting enzyme (ACE) inhibitor prototype: used in HTN, diabetic nephropathy, and CHF. Tox: hyperkalemia, fetal renal damage, cough ("sore throat"). Other "prils" include benzepril, enalapril, lisinopril, quinapril.
Anticonvulsant: used for tonic-clonic and partial seizures;
blocks Na+ channels in neuronal membranes. Drug of choice for trigeminal neuralgia; backup drug in bipolar disorder. Tox: CNS depression, myelotoxic, induces liver drug-metabolizing enzymes, teratogenicity.
Adrenoceptor blocker: racemic mixture, one isomer a nonselective b-blocker and the other an a1 blocker. Possible
antioxidant actions. Prolongs survival in CHF. Tox: cardiovascular depression. Labetalol is similar.
First-generation cephalosporin prototype: bactericidal beta- lactam inhibitor of cell wall synthesis. Active against gram- positive cocci, E coli, K pneumoniae, but does not enter CSF. Tox: potential allergy; partial cross-reactivity with penicillins.
Second-generation cephalosporin: active against a wide spectrum of gram-negative bacteria, including anaerobes (B fragilis ). Does not enter the CNS. Cefotetan is similar.
Third-generation cephalosporin: active against many bacteria, including pneumococci, gonococci (a drug of choice), and gram- negative rods. Enters the CNS and is used in bacterial meningitis. Cefotaxime and ceftazidime are other third- generation cephalosporins.
Selective COX-2 inhibitor: acts mainly on enzymes of cells involved in inflammation. Used in rheumatoid arthritis and other inflammatory disorders. Tox: GI toxicity, but less than that of aspirin and other NSAIDs; nephrotoxicity similar to other NSAIDs, increased risk of CV events. Rofecoxib is similar.
Antibiotic: broad-spectrum agent; inhibits protein synthesis (50S); uses restricted to backup drug for bacterial meningitis, infections due to anaerobes, Salmonella. Tox: reversible myelosuppression, aplastic anemia, gray baby syndrome.
Antimalarial: used for treatment and as a chemosuppressant where P falciparum is susceptible. Binds to hemin, causing dysfunctional cell membranes; resistance resulting from efflux via P-glycoprotein pump. Tox: GI distress, skin rash at low doses; peripheral neuropathy, auditory and visual impairment, quinidine-like cardiotoxicity at high doses.
Antihistamine first-generation H1 blocker prototype: Tox: mild sedation, little antimuscarinic action.
Phenothiazine antipsychotic : blocks D2 dopamine receptors. Tox: atropine-like, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation, seizures (in OD), additive effects with other CNS depressants. Other phenothiazines: fluphenazine and trifluoperazine (antipsychotics), prochlorperazine (antiemetic), promethazine (preoperative sedation)
Bile acid-binding resin: sequesters bile acids in gut and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins. Tox: constipation, bloating; interferes with absorption of some drugs. Colestipol is similar
H2 blocker prototype: used in acid-peptic disease. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine.
Second-generation fluoroquinolone antibiotic: bactericidal inhibitor of topoisomerases; active against E coli, H influenzae, Enterobacter, Pseudomonas, Shigella. Tox: CNS dysfunction, GI distress collagen dysfunction (avoid in children and pregnant women). Interactions: inhibits metabolism of caffeine, theophylline, warfarin.
Platinum-containing alkylating anticancer drug. Used for solid tumors (eg, testes, lung). Tox: Neurotoxic and nephrotoxic. Carboplatin is similar.
Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); active against gram-positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis.
Tissue-selective estrogen receptor antagonist: synthetic, used in infertility to induce ovulation by blocking pituitary estrogen receptors. May result in multiple births.
Alpha2 agonist: acts centrally to reduce SANS outflow, lowers BP. Used in HTN and in drug dependency states. Tox: mild sedation, rebound HTN if stopped suddenly.
Blocks platelet ADP receptors irreversibly and inhibits platelet aggregation. Used in transient ischemic attacks and to prevent strokes and restenosis after placement of coronary stents. Tox: bleeding, neutropenia. Ticlopidine similar, but higher risk of neutropenia and thrombotic thrombocytopenic purpura (TTP).
Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors; fewer EPS adverse effects than other antipsychotic drugs. Tox: ANS effects, agranulocytosis (infrequent but significant).
Indirectly acting sympathomimetic: blocks amine reuptake into nerve endings. Local anesthetic (ester type). Marked CNS stimulation, euphoria; high abuse and dependence liability. Tox: psychosis, cardiac arrhythmias, seizures.
Microtubule assembly inhibitor: reduces mobility and phagocytosis by WBCs in gout-inflamed joints; used in gout. Tox: GI (often severe), hepatic, renal damage.
Antineoplastic, immunosuppressive: cell cycle-nonspecific alkylating agent. Tox: alopecia, gastrointestinal distress, hemorrhagic cystitis (use mesna), myelosuppression
Immunosuppressant: antibiotic; inhibits synthesis of interleukins and interferon-g, suppressing T-cell activation. Tox: nephrotoxicity (dose limiting), hirsutism, hypertension, peripheral neuropathy, seizures (in overdose). Not a myelosuppressant. Tacrolimus is similar.
DNA technology products: aldesleukin (IL-2, used in renal cancer); erythropoietin (epoetin alfa, used in anemias); filgrastim (G-CSF, used in neutropenia); interferon-a (used in hepatitis B and C and in cancer), interferon-b (used in multiple sclerosis); oprelvekin (IL-11, used in thrombocytopenia); and sargramostim (GM-CSF, used in neutropenia).
Muscle relaxant: blocks Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Used in muscle spasm (cerebral palsy, multiple sclerosis, cord injury) and in emergency treatment of malignant hyperthermia.
ADH analog, selective for V2 receptors: used for pituitary diabetes insipidus and to increase factor VIII in bleeding disorders. Vasopressin (ADH), an agonist for V1 and V2 receptors, is used in pituitary diabetes insipidus and bleeding esophageal varicosities.
Glucocorticoid: very potent, long acting; no mineralocorticoid activity. Betamethasone is similar; triamcinolone has shorter half-life.
Benzodiazepine prototype: binds to BZ receptors of the GABAA receptor-chloride ion channel complex; facilitates the inhibitory actions of GABA by increasing the frequency of channel opening (compare phenobarbital). Uses: anxiety states, ethanol detoxification, muscle spasticity, status epilepticus. Tox: dependence, additive effects with other CNS depressants.
Cardiac glycoside prototype: positive inotropic drug for CHF, half-life 40 h; inhibits Na+/K+ ATPase, also a cardiac parasympathomimetic. Tox: calcium overload arrhythmias, GI upset.
Antihistamine (first-generation) H1 blocker: used in hay fever, motion sickness, dystonias. Tox: antimuscarinic, a adrenoceptor blocker, strong sedative. Doxylamine is similar.
Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow (low dose) and positive inotropic effects (moderate dose).
Antineoplastic: anthracycline drug (cell cycle-nonspecific); intercalates between base pairs to disrupt DNA functions, inhibits topoisomerases, and forms cytotoxic free radicals. Tox: cardiotoxicity, myelosuppression. Daunorubicin is similar.
Tetracycline antibiotic: protein synthesis inhibitor (30S), more effective than other tetracyclines against chlamydia and in Lyme disease. Unlike other tetracyclines, it is eliminated mainly in the feces. Tox: see tetracycline.
Cholinesterase inhibitor: very short duration of action (15 min). Used in diagnosis of myasthenia gravis and to distinguish myasthenic crisis from cholinergic crisis.
Nonnucleoside reverse transcriptase inhibitor (NNRTI): used in combination regimens for HIV. Tox: skin rash, CNS effects. Other NNRTIs: delavirdine, nevirapine.
LMW heparin. Primary effect is on factor Xa, less on thrombin. The aPTT test is unreliable. Other LMW heparin-like products: dalteparin, danaparoid, fondaparinux. Tox: bleeding.
COMT inhibitor: enhances levodopa access to CNS neurons; adjunctive use in Parkinson's disease. Tox: exacerbates levodopa effects. Tolcapone is similar in action and use but may be hepatotoxic.
Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more smooth muscle effects. In botanicals (eg, ma huang) and products for weight loss that are banned in the United States. Tox: hypertension, stroke, MI.
Adrenoceptor agonist prototype: product of adrenal medulla, some CNS neurons. Affinity for all a and all b receptors. Used in asthma; as hemostatic and as adjunct with local anesthetics; drug of choice in anaphylaxis. Tox: tachycardia, hypertension, MI, pulmonary edema and hemorrhage.
Ergonovine, ergotamine, methysergide: cause prolonged vasoconstriction and uterine contraction. Used in migraine and obstetrics. Tox: vasospasm (including coronaries).
Macrolide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); activity includes gram-positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis. Tox: cholestatic jaundice (avoid estolate in pregnancy), inhibits liver drug-metabolizing enzymes. Other macrolide antibiotics include azithromycin and clarithromycin.
DMARD: recombinant protein that binds TNF. Infliximab (see under Mabs) has a similar mechanism of action. Effective (by injection) in RA and possibly other severe inflammatory diseases. Tox: injection site reactions include erythema, itching, and swelling; possible increased infection rate.
A sedative-hypnotic. Acute actions include impaired judgment, ataxia, loss of consciousness, vasodilation, and cardiovascular and respiratory depression. Chronic use leads to dependence and dysfunction of multiple organ systems. Note: zero-order elimination kinetics.
Synthetic estrogen: used in many hormonal contraceptives; mestranol is similar
Anticonvulsant: used in absence seizures; may block T-type Ca2+ channels in thalamic neurons. Tox: GI distress; safe in pregnancy.
Short-acting synthetic opioid agonist (see morphine) used commonly in anesthesia and for chronic pain (transdermal form). Remifentanil and sufentanil are similar.
Steroid inhibitor of 5a-reductase: inhibits synthesis of dihydrotestosterone. Used in benign prostatic hyperplasia and male-pattern baldness.
Class IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff-Parkinson- White syndrome. Tox: arrhythmogenic, CNS excitation.
Imidazole antifungal: inhibits ergosterol synthesis. Used in esophageal and vaginal candidiasis, in coccidioidomycosis, and in the prophylaxis and treatment of fungal meningitis. Adverse effects similar to those of ketoconazole (see later) but less severe.
Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action.
Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of benzodiazepines.
Antineoplastic: pyrimidine antimetabolite (cell cycle specific), causes "thymine-less" cell death; used mainly for solid or superficial tumors. Tox: GI distress, myelosuppression.
Antidepressant: selective serotonin reuptake inhibitor (SSRI) prototype. Tox: CNS stimulation, sexual dysfunction, seizures in overdose, serotonin syndrome. Other SSRIs: citalopram, escitalopram, paroxetine, sertraline.
Androgen receptor antagonist: used in prostatic carcinoma. Others: biclalutamide, nilutamide.
Loop diuretic prototype: blocks Na+/K+/2Cl_ transporter in thick ascending limb; high efficacy; used in acute pulmonary edema, refractory edematous states, hypercalcemia. Tox: ototoxicity, K+ wasting, hypovolemia, increased serum uric acid. Ethacrynic acid is similar but has less effect on uric acid.
Anticonvulsant: structural analog of GABA that facilitates its inhibitory actions in the CNS; used for partial seizures, for neuropathic pain, and in bipolar disorder. Tox: sedation, movement disorders.
Antiviral: effective against herpes viruses (cytomegalocirus [CMV] and herpes simplex virus [HSV]); for CMV requires bioactivation via viral phosphotransferase. Tox: myelosuppression, nephrotoxicity, neurotoxicity.
Fibrate antilipemic: activates PPAR-a nuclear receptors; lowers serum triglycerides via stimulation of lipoprotein lipase activity. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia. Tox: GI distress, cholelithiasis, skin rashes, increased risk of myopathy when combined with statins or niacin.
Aminoglycoside prototype: bactericidal inhibitor of protein synthesis (30S); active against many aerobic gram-negative bacteria. Narrow therapeutic window; dose reduction required in renal impairment. Tox: renal dysfunction, ototoxicity; once- daily dosing is effective (postantibiotic effect) and less toxic. Amikacin and tobramycin are similar.
Oral hypoglycemic: second-generation sulfonylurea, very potent. Blocks K+ channels in pancreatic B cells, causing depolarization and release of insulin. Tox: hypoglycemia, weight gain. Related drugs: glyburide and older sulfonylureas such as acetohexamide, chlorpropamide, and tolbutamide.
Hormone from pancreatic A cells. Increases blood sugar via increased cAMP. Used in hypoglycemia and as an antidote in b blocker overdose.
Antipsychotic butyrophenone: blocks brain dopamine D2 receptors. Tox: marked EPS dysfunction, hyperprolactinemia; fewer ANS adverse effects than phenothiazines.
General anesthetic prototype: inhaled halogenated hydrocarbon. Tox: cardiovascular and respiratory depression and relaxation of skeletal and smooth muscle. Use is declining because of sensitization of heart to catecholamines and occurrence (rare) of hepatitis.
Anticoagulant: large polymeric molecule with activity against thrombin and factor X. Rapid onset, in vitro and in vivo anticoagulation. Tox: bleeding. Antidote: protamine. See also Enoxaparin.
Antihypertensive: arteriolar vasodilator, orally active; used in severe HTN, CHF. Minoxidil, a similar but more powerful antihypertensive, is also used topically in baldness. Tox: tachycardia, salt and water retention, lupus-like syndrome (hydralazine).
Thiazide diuretic prototype: acts in distal convoluted tubule to block Na+/Cl_ transporter; used in HTN, CHF, nephrolithiasis. Tox: a sulfonamide; increased serum lipids, uric acid, glucose; K+ wasting.
DMARD: decreases leukocyte chemotaxis, stabilizes lysosomes, and traps free radicals. Tox: GI distress, ototoxicity, myopathy, neuropathy. Other older DMARDs: methotrexate, prednisone, sulfasalazine, gold salts, penicillamine.
NSAID: reversible inhibitor of cyclooxygenases with analgesic, antipyretic, and anti-inflammatory actions similar to aspirin, but no low-dose antiplatelet effect. Tox: similar to aspirin, but no salicylism and less acid-base imbalance.
Prototype carbapenem antibiotic: active against many aerobic and anaerobic bacteria; bactericidal inhibitor of cell wall synthesis. Used with cilastatin. Tox: allergy (partial cross- reactivity with penicillins), seizures. Meropenem and ertapenem are similar but do not require cilastatin and are less likely to cause seizures.
Tricyclic antidepressant (TCA): blocks reuptake of norepinephrine and serotonin. Tox: atropine-like, postural hypotension, sedation, cardiac arrhythmias in overdose, additive effects with other CNS depressants. Other TCAs: amitriptyline, clomipramine, doxepin.
Antiviral: HIV protease inhibitor (PI) used as a component of combination regimens in AIDS. Tox: anemia, nephrolithiasis, metabolic disorders, inhibits P450 drug metabolism. Other PIs: amprenavir, nelfinavir, ritonavir (major P450 inhibitor), and saquinavir.
NSAID: highly potent. Usually reserved for acute inflammation (eg, acute gout), not chronic; neonatal patent ductus arteriosus. Tox: GI (bleeding), renal damage.
Antimuscarinic agent: aerosol for asthma, chronic obstructive pulmonary disease (COPD). Good bronchodilator in 20-30% of patients. Not as efficacious as b2 agonists. Tox: dry mouth.
Antimycobacterial: primary drug in combination regimens for tuberculosis; used as sole agent in prophylaxis. Metabolic clearance via N-acetyltransferases (genetic variability). Tox: hepatotoxicity (age dependent), peripheral neuropathy (reversed by pyridoxine), hemolysis (in G6PD deficiency).
Beta1 and b2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, tremor, angina.
Anthelmintic: drug of choice for onchocerciasis and threadworm infections. Intensifies GABA-mediated neurotransmission in nematodes, but no access to CNS in humans. Tox: in onchocerciasis causes headache, fever, hypotension, joint pain.
Antifungal azole: inhibits the synthesis of ergosterol. Used for C albicans, dermatophytosis, and non-life-threatening systemic mycoses. Tox: hepatic dysfunction, inhibits steroid synthesis and P450-dependent drug metabolism. Others: fluconazole, itraconazole, and voriconazole have wider spectrum and less inhibition of hepatic cytochromes P450.
Nucleoside reverse transcriptase inhibitor (NRTI) also known as 3TC. Notable for use in chronic hepatitis B in addition to HIV infection.
Newer antiepiliptic drug for absence and partial seizures; also used in bipolar affective disorder. Tox: rash, possibly life threatening.
DMARD: dihydroorotate dehydrogenase inhibitor that arrests T- cell proliferation. Used orally in RA. Tox: diarrhea, increased liver enzymes.
GnRH analog: synthetic peptide used in pulse therapy to stimulate gonadal steroid synthesis (infertility); used in continuous or depot therapy to shut off steroid synthesis, especially in prostatic carcinoma and endometriosis. Goserelin and naferelin are similar.
Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism). Tox: dyskinesias, hypotension, on-off phenomena, behavioral changes.
Amide local anesthetic, medium-duration amide prototype: highly selective use-dependent class IB antiarrhythmic; used for nerve block and post-MI ischemic ventricular arrhythmias. Tox: CNS excitation. Mexiletine: like lidocaine, but orally active.
Antimanic prototype: a primary drug in mania and bipolar affective disorders; blocks recycling of the phosphatidylinositol second messenger system. Tox: tremor, diabetes insipidus, goiter, seizures (in overdose), teratogenic potential (Ebstein's malformations).
Second-generation H1 antihistamine: used in hay fever. Tox: Much less sedation than first-generation antihistamines; no ANS effects. Others: desloratadine, cetirizine, fexofenadine.
Angiotensin AT1 receptor blocker prototype: used in HTN. Effects and toxicity similar to those of ACE inhibitors but causes less cough. Other AT1 blockers: candesartan, eprosartan, irbesartan, olmisartan, telmisartan, and valsartan.
Antilipemic HMG-CoA reductase inhibitor prototype: acts in liver to reduce synthesis of cholesterol. Other "statins": atorvastatin, fluvastatin, pravastatin, rosuvastatin, simvastatin. Tox: liver damage (elevated enzymes), muscle damage.
Monoclonal antibodies include: abciximab, daclizumab (blocks IL-2 receptors, used in renal transplants), infliximab (binds TNF, used in RA and Crohn's disease), palivizumab (used in RSV), rituximab (used in non-Hodgkin's lymphoma), and trastuzumab (used in breast cancers with HER2/neu receptors).
Organophosphate insecticide cholinesterase inhibitor: prodrug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products. Other organophosphates: parathion converted to paraoxon, and the nerve gases (eg, soman, tabun).
Osmotic diuretic: used short term for reduction of intracranial pressure or to promote excretion of renal toxins. Tox: expansion of extracellular fluid volume with resulting hyponatremia, headache, nausea. With excessive use, dehydration and hypernatremia.
Anthelmintic: important drug for pinworm and whipworm infections. Inhibits microtubule synthesis and glucose uptake in nematodes. Tox: GI distress, caution in pregnancy. Albendazole (widely used) and thiabendazole (more toxic) are related anthelmintics.
Progestin used in combination with an estrogen for treatment of menopausal symptoms and used as a long-acting injection (Depo-Provera) for contraception.
Antimalarial: unknown mechanism of action. Used for prophylaxis against and treatment of chloroquine-resistant malaria. Tox: GI distress, dizziness, seizures in overdose, arrhythmias.
Opioid analgesic: synthetic, equivalent to morphine in efficacy but orally bioavailable. Strong agonist at mu opioid receptors; blocks muscarinic receptors; serotonergic activity. Tox: see morphine; normeperidine accumulation may cause seizures, serotonin sydrome with SSRIs.
Oral biguanide hypoglycemic: is euglycemic and does not release insulin from pancreatic B cells; proposed mechanisms include decreased hepatic gluconeogenesis and stimulation of glycolysis. Minimal hypoglycemia or weight gain. Tox: GI distress, lactic acidosis possible but rare.
Opioid analgesic: synthetic mu agonist, equivalent to morphine in efficacy but orally bioavailable and with a longer half-life. Used as analgesic, to suppress withdrawal symptoms, and in maintenance programs. Tox: see morphine.
Antineoplastic, immunosuppressant: cell cycle-specific drug that inhibits dihydrofolate reductase. Major dose reduction required in renal impairment. Tox: GI distress, myelosuppression, crystalluria. Leucovorin rescue used to reduce toxicity.
Antihypertensive: prodrug of methylnorepinephrine, a CNS- active a2 agonist. Reduces SANS outflow from vasomotor center. Tox: sedation, positive Coombs test, hemolysis.
Antiprotozoal antibiotic: drug of choice in extraluminal amebiasis and trichomoniasis; effective against bacterial anaerobes, including B fragilis and in antibiotic-induced colitis resulting from C difficile. Tox: peripheral neuropathy, GI distress, ethanol intolerance, mutagenic potential.
Progestin and glucocorticoid receptor antagonist: abortifacient, postcoital contraceptive.
PGE1 derivative: orally active prostaglandin used for GI ulcers caused by NSAIDs. Tox: diarrhea.
Opioid analgesic prototype: strong mu receptor agonist. Poor oral bioavailability. Tox: constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychological and physiologic dependence. Additive effects with other CNS depressants.
Penicillinase-resistant penicillin: used for suspected or known staphylococcal infections; not active against MRSA. Tox: penicillin allergy. Others in group include methicillin (the prototype, rarely used), oxacillin, cloxacillin, and dicloxacillin.
Opioid: mixed agonist-antagonist analgesic that activates kappa and weakly blocks mu receptors. Effective analgesic but with lower abuse liability and less respiratory depressant effects than most strong opioid analgesics. Other mixed agonist- antagonists: buprenorphine, also a strong analgesic; pentazocine, much less analgesic activity.
Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia). Naltrexone (orally active), a related compound, is used in ethanol dependency states.
Cholinesterase inhibitor: prototype synthetic quaternary nitrogen carbamate with little CNS effect. Tox: excess cholinomimetic effects. Pyridostigmine is similar.
Antilipemic: reduces release of VLDL from liver into circulation. Lowers LDL cholesterol and triglycerides and raises HDL cholesterol. Tox: flushing, pruritus, liver dysfunction, increased risk of myopathy when combined with statins.
Dihydropyridine calcium channel blocker prototype: vasoselective (less cardiac depression than verapamil, diltiazem); used in angina, HTN. Tox: constipation, headache, gingival overgrowths, tachycardia, arrhythmias (avoid rapid-onset forms). Others in group include amlodipine (used in HF), nimodipine (used in subarachnoid hemorrhage), and nicardipine.
Endogenous vasodilator released from vascular endothelium; neurotransmitter. Mediates vasodilating effect of acetylcholine, histamine, and hydralazine. Active metabolite of nitroprusside and of nitrates used in angina. Used as pulmonary dilator in neonatal hypoxia. Tox: excessive vasodilation, hypotension
Antianginal vasodilator prototype: releases nitric oxide (NO) in smooth muscle of veins, less in arteries, and causes relaxation. Standard of therapy in angina (both atherosclerotic and variant). Tox: tachycardia, orthostatic hypotension, headache. Oral nitrates: isosorbide dinitrate, isosorbide mononitrate.
Adrenoceptor agonist prototype: acts at b1- and all a adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN.
Atypical antipsychotic; high-affinity antagonist at 5-HT2 receptors with minimal extrapyramidal side effects; improves both positive and negative symptoms of schizophrenia. Other atypicals: quetiapine (short half-life), risperidone (possible EPS dysfunction), sertindole (QT prolongation).
Proton pump inhibitor prototype: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in GI ulcers, Zollinger-Ellison syndrome, gastroesophageal reflux disease (GERD). Other "prazoles": lansoprazole, pantoprazole, rabeprazole. Tox: hypergastrinemia.
5-HT3 receptor blocker prototype: very important antiemetic for cancer chemotherapy; also used postoperatively to reduce vomiting. Tox: extrapyramidal effects. Other "setrons": granisetron, dolasetron.
Neuraminidase inhibitor: inhibits release and facilitates clumping of mature virions of influenza A and B and decreases their infectivity. Shortens duration of flu symptoms. Zanamivir is similar in action and use.
Muscarinic cholinoceptor blocker: used to relieve bladder spasm and incontinence. Tolterodine, weaker but more selective for M3 receptors, has similar uses.
Antineoplastic plant alkaloid: cell cycle (M phase)-specific agent; inhibits mitotic spindle disassembly. Tox: hematotoxicity, peripheral neuropathy, hypersensitivity reactions. Docetaxel is similar.
Chelator, immunomodulator: copper and sometimes lead, mercury, arsenic. Used in Wilson's disease and rheumatoid arthritis.
Penicillin prototype: active against common streptococci, gram- positive bacilli, gram-negative cocci, spirochetes (drug of choice in syphilis), and enterococci (if used with an aminoglycoside); penicillinase susceptible. Tox: penicillin allergy.
Irreversible nonselective monoamine oxidase (MAO) inhibitor. Backup drug for atypical depression. Tox: Malignant hypertension with indirect-acting sympathomimetics and tyramine, serotonin syndrome with serotonergic drugs.
Long-acting barbiturate: used as a sedative and for tonic-clonic seizures. Facilitates GABA-mediated neuronal inhibition and may block excitatory neurotransmitters. Partial renal clearance that can be increased by urinary alkalinization. Chronic use induces liver drug-metabolizing enzymes and ALA synthase. Tox: psychological and physiologic dependence; additive effects with other CNS depressants.
Alpha-blocker prototype (nonselective): irreversible action. Phentolamine: competitive action. Used in pheochromocytoma. Tox: excess hypotension; GI distress.
Anticonvulsant: used for tonic-clonic and partial seizures; blocks Na+ channels in neuronal membranes. Serum levels variable because of first-pass metabolism and nonlinear elimination kinetics. Tox: sedation, diplopia, gingival hyperplasia, hirsutism, teratogenic potential. Drug interactions via induction of hepatic metabolism.
Acetylcholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma, atropine poisoning. Tox: convulsions, excess cholinomimetic effects. Others: neostigmine and pyridostigmine; DFP and echothiophate are organophosphates used rarely.
Muscarinic partial agonist prototype: tertiary amine alkaloid. May cause paradoxic hypertension by activating muscarinic excitatory postsynaptic potential receptors in postganglionic sympathetic neurons. Used in Sjögren's syndrome, xerostomia, glaucoma. Tox: muscarinic excess.
Thiazolidinedione stimulator of peroxisome proliferator-activator receptors (PPARs) enhances target tissue sensitivity to insulin. Used in type 2 diabetes. Less hypoglycemia and weight gain than sulfonylureas. Other "glitazones": rosiglitazone, troglitazone (the latter drug discontinued in United States because of hepatotoxicity).
Extended-spectrum penicillin active against selected gram- negative bacteria, including Pseudomonas aeruginosa (synergistic with aminoglycosides). Susceptible to penicillinases unless used with tazobactam. Tox: penicillin allergy.
Acetylcholinesterase regenerator (antidote for organophosphate poisoning): very high affinity for phosphorus in organophosphates. Tox: neuromuscular weakness.
Anthelmintic: important drug for trematode (fluke) and cestode (tapeworm) infections. Increases membrane permeability to Ca2+ causing muscle contraction followed by paralysis. Tox: headache, dizziness, GI distress, fever; potential abortifacient.
Alpha1-selective blocker prototype: used in HTN and benign prostatic hyperplasia. Tox: first-dose orthostatic hypotension but less reflex tachycardia than nonselective a blockers. Other "osins": terazosin, doxazosin.
Glucocorticoid prototype: potent, short acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone.
Uricosuric: inhibitor of renal weak acid secretion and reabsorption in S2 segment of proximal tubule; prolongs half- life of penicillin, accelerates clearance of uric acid. Used in gout. Sulfinpyrazole is similar.
Class IA antiarrhythmic drug prototype: short half-life, metabolized by N-acetyltransferase. Similar to quinidine but more cardiodepressant and may cause a lupus-like syndrome.
Nonselective b blocker prototype: local anesthetic action but no partial agonist effect. Used in HTN, angina, arrhythmias, migraine, hyperthyroidism, tremor. Tox: asthma, AV block, CHF.
Antithyroid drug prototype: inhibits tyrosine iodination and coupling reactions; orally active. Tox: rash, agranulocytosis (rare). Methimazole is similar but more lipid soluble.
PGI2 prostaglandin vasodilator and inhibitor of platelet aggregation. An analog, epoprostenol, is used in primary pulmonary HTN.
Antiprotozoal: antifol inhibiting DHF reductase and synergistic, via sequential blockade, with sulfadiazine against Toxoplasma gondiioplasma gondii. Folinic acid is needed to offset hematologic toxicity.
Class IA antiarrhythmic: used in atrial and ventricular arrhythmias. Tox: cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic (torsade de pointes).
Antimalarial: blood schizonticide; no effect on liver stages. Interferes with nucleic acid metabolism in plasmodium. Isomer of quinidine, same toxicity.
Selective estrogen receptor modulator (SERM): agonist at bone receptors (used in osteoporosis), antagonist at breast receptors (used in cancer) but does not stimulate endometrial receptors.
Oral hypoglycemic: blocks K+ channels in pancreatic B cells, causing depolarization and release of insulin. Used in type 2 diabetes alone or in combinations; rapid onset and short duration. Tox: hypoglycemia, increases liver enzymes.
Antihypertensive (rarely used): selective inhibitor of vesicle catecholamine-H+ antiporter; used in HTN, causes depletion of catecholamines and 5-HT from their stores. Tox: severe depression, suicide, ulcers, diarrhea. Guanethidine is similar, but blocks amine release.
Antimicrobial: inhibitor of DNA-dependent RNA polymerase used in drug regimens for tuberculosis and the meningococcal carrier state. Tox: hepatic dysfunction, induction of liver drug- metabolizing enzymes (drug interactions), flulike syndrome with intermittent dosing. Rifabutin similar but associated with fewer drug interactions.
Dopamine receptor agonist: nonergot used in Parkinson's disease; more receptor selectivity and less toxicity than bromocriptine. Tox: dyskinesias, sedation. Pramipexole is similar.
MAO-B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Used in Parkinson's disease. Tox: GI distress, CNS stimulation, dyskinesias, serotonin syndrome if used with selective serotonin reuptake inhibitors.
Inhibits phosphodiesterase (PDE) 5, preventing breakdown of cGMP, which promotes vascular vasodilation. Used for erectile dysfunction. Tox: severe hypotension when combined with nitrates, impaired blue-green color vision.
Aldosterone receptor antagonist: K+-sparing diuretic action in the collecting tubules; used in aldosteronism, HTN, and female hirsutism (androgen receptor blocking action). Tox: hyperkalemia, gynecomastia. Eplerenone, used in HTN and HF, is a more selective aldo¬sterone antagonist.
Class III antiarrhythmic prototype: blocks IK channels. Used for atrial and ventricular arrhythmias. Tox: torsade de pointes arrhythmias. Others in group: ibutilide, dofetilide.
Antibiotics: Synercid is the combination of quinupristin and dalfopristin; bactericidal inhibitors of protein synthesis. IV use for drug-resistant gram-positive cocci including MRSA, VRE, and pneumococci. Tox: infusion-related pain, arthralgia, myalgia. Linezolid is used for drug-resistant gram-positive cocci, including PRSPstrains.
Thrombolytic: protein from streptococci that accelerates plasminogen-to-plasmin conversion. Tox: bleeding, allergy.
Depolarizing neuromuscular relaxant prototype: short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote (compare with tubocurarine). Implicated in malignant hyperthermia.
5-HT1D receptor agonist: used to abort migraine attacks. Tox: coronary vasospasm, chest pain, or pressure. Other "triptans": naratriptan, rizatriptan, zolmitriptan.
Selective estrogen receptor modulator (SERM): blocks estrogen (E) receptors in breast tissue; activates endometrial E receptors. Used in E receptor-positive cancers, possibly prophylactic in high-risk patients. Toremifene is similar.
Antibiotic: tetracycline prototype; bacteriostatic inhibitor of protein synthesis (30S). Used for mycoplasmal, chlamydial, rickettsial infections, chronic bronchitis, acne, cholera; a backup drug in syphilis. Tox: GI upset and superinfections, Fanconi's syndrome, photosensitivity, dental enamel dysplasia.
Toxin: potent sodium channel blocker; blocks action potential propagation in nerve, heart, and skeletal muscle. From puffer fish, California newt. Tox: paresthesias, paralysis. Saxitoxin (paralytic shellfish poison) is similar.
Trimethoprim- sulfamethoxazole (TMP-SMX)
Antimicrobial drug combination: causes synergistic sequential blockade of folic acid synthesis. Active against many gram- negative bacteria. Tox: mainly due to sulfonamide; includes hypersensitivity, myelotoxicity, kernicterus, and drug interactions caused by competition for plasma protein binding.
Nondepolarizing neuromuscular blocking agent prototype: competitive nicotinic blocker. Releases histamine and may cause hypotension. Analogs: pancuronium, atracurium, vecuronium, and other "-curiums" and "-oniums." Tox: respiratory paralysis. Antidote: cholinesterase inhibitor, eg, neostigmine.
Indirectly acting sympathomimetic prototype: releases or displaces norepinephrine from stores in nerve endings. Presence in certain foods may cause potentially lethal hypertensive responses in patients taking MAO inhibitors.
Anticonvulsant: primary drug in absence, clonic-tonic, and myoclonic seizure states. Also used commonly for bipolar disorder. Tox: GI distress, hepatic necrosis (rare), teratogenic (spina bifida), inhibits drug metabolism.
Glycopeptide bactericidal antibiotic: inhibits synthesis of cell wall precursor molecules. Drug of choice for methicillin- resistant staphylococci and effective in antibiotic-induced colitis. Dose reduction required in renal impairment (or hemodialysis). Tox: ototoxicity, hypersensitivity, renal dysfunction (rare).
Calcium channel blocker prototype: blocks L-type channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation. Diltiazem, like verapamil, has more depressant effect on heart than dihydropyridines (eg, nifedipine).
Antineoplastic plant alkaloid: cell cycle (M phase)-specific agent; inhibits mitotic spindle formation. Tox: peripheral neuropathy. Vinblastine, a congener, causes myelosuppression.
Oral anticoagulant prototype: causes synthesis of nonfunctional versions of the vitamin K-dependent clotting factors (II, VII, IX, X). Tox: bleeding, teratogenic. Antidote: vitamin K, fresh plasma.
Antiviral: prototype NRTI used in combinations for HIV infections and in prophylaxis for needlesticks and vertical transmission. Tox: severe myelosuppression. Other NRTIs: abacavir, didanosine (ddI),lamivudine (3TC), stavudine (d4T), and zalcitabine (ddC).
Nonbenzodiazepine hypnotic, acts via the BZ1 receptor subtype and is reversed by flumazenil; less amnesia and muscle relaxation and lower dependence liability than benzodiazepines. Zaleplon is similar, but shorter acting.
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