215 terms

First AID Pharm

Penicillin (MOA)
bind pbps, block transpeptidase cross-linking of cell wall, bacteria autolysin activity
Methicillin (toxicity)
interstitial nephritis
Ampicillin, Amoxicillin (clinical use)
Gram + and H. influenza, E. coli, Listeria, Proteus, Salmonella and enterococci
Ampicillin (toxicity)
pseudomembranous colitis
Ticarcillin, carbenicillin, pipercillin (clinical use)
Pseudomonas and gram - rods
use with clavulanic acid
B-lactamase inhibitors
clavulanic acid, sulbactam, tazobactam
used in combo with antipseudomonals and aminopencillins
Erthromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol
Vancomycin, Fluoroquinolones, Pencillin, Aminoglycosides, Cephalsporins, Metronidazole
Cephalosporins (MOA)
B-lactam drugs that inhibit cell wall synthesis but less suspectible to penicillins
1st generation Cephs (names and clinical use)
Cefazolin, Cephalexin
Gram + and Proteus, E. coli, Klebsiella
2nd generation Cephs (names)
Cefaclor, Cefoxitin, Cefuroxime, Cefamandole
(its a FACt i want a FOXy FURy MAN)
2nd generation Cephs (clinical use)
H. influenza, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia
3rd generation Cephs
Ceftriaxone, Cefotaxime, Ceftazidine
Cross the BBB
Covers serious gram - except LAMEs (Listeria, Atypical, MRSA, Enterococci)
4th generation Cephs
covers Pseudomonas and gram +
Cephs (toxicity)
Nephrotoxicity with aminoglycosides
disulfram like reaction
Aztrenam (clinical use)
Gram - rods
DOES NOT WORK ON gram + or anaerobes
No cross-sensitivity with pens and cephs
Imipenem/cilastatin (MAO)
B-lactamase resistant carbapenem.
Cilastatin inhibits dihydropeptidase I in the kidney
Imipenem and Meropenem (clinical use)
Broadest spectrum
used empiric therapy
DOC for Enterobacter
Vancomycin (MAO and clinical use)
inhibits cell wall mucopeptide formation by binding D-ala D-ala
used for MRSA and multidrug resistant gram +
Vancomycin (Resistance)
amino acid change from D-ala to D-lac
Vancomycin (Toxicity)
Nephrotoxicity, Ototoxicity, Thrombophlebitis, RED MAN SYNDROME
30S inhibitors
50S Inhibitors
Chloramphenicol, Clindamycin
Aminoglycosides (names and MAO)
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
inhibit initiation complex and cause misreading of mRNA
Aminoglycosides (clinical use and toxicity)
MUST HAVE OXYGEN--> ineffective against anaerobes
use for gram - rods
Nephrotoxicity, Ototoxicity, Neuromuscular blockade, Teratogen
Aminoglycosides (resistance)
transferase enzyme or enzymes that inactivate by adenylation, acetylation, and phosphorylation
Tetracyclines (MAO)
prevent attachment of aminoacyl tRNA
DON'T take with milk or iron due to divalent cations which inhibits absorption
Tetracyclines (clinical use)
Vibrio chlorea, acne, Chlamydia, Ureaplasma, Mycoplasma, H. Pylori, Borrelia, Rickettsia
Tetracylcine (toxicity)
teeth discoloration, inhibition of bone growth, photosensitivity
Macrolides (names and MAO)
ACE (azithromycin, clarithromycin, erythromycin)
inhibits protein synthesis by blocking translocation by binding 23S rRNA of the 50S
Macrolides (clinical use)
Mycoplasma, Legionalla, Chlamydia, Neisseria
Macrolides (toxicity)
Prolonged QT interval, GI discomfort, acute cholestatic hepatitis
Chloramphenicol (MAO and clinical use)
inhibits 50S peptidyltransferase
Chloramphenicol (toxicity)
Aplastic anemia
Gray baby syndrome due to lack of UDP-glucuronyl transferase
Clindamycin (MAO)
blocks peptide bond formation at 50S ribosomal subunit
Drugs used for VRSA
Streptogramins (quinupristin/dalfopristin)
Sulfonamides (MAO)
PABA antimetabolite
inhibits dihydropteroate synthetase
Sulfonamides (toxicity)
hemolysis in G6PD deficiency
kernicterus due to displacement of bilirubin
Trimethoprim (MAO and toxicity)
inhibits bacterial dihydrofolate reductase
toxicity: megaloblastic anemia, leukopenia, granulocytopenia
Polymyxins (MAO)
bind to cell membranes of bacteria and disrupt their osmotic properties
cationic, basic proteins that act like detergents
Polymyxins (clinical use and toxicity)
used for resistant gram - infections
neurotoxicity, acute tubular necrosis
Ethambutol (MAO)
inhibits arabinosyl transferase which polymerizes arabinose into arabinoglactan
Ethambutol (toxicity)
red green color blindness
Rifampin (MAO)
inhibits DNA-dependent RNA polymerase
Rifampin (toxicity)
hepatotoxicity, P-450 inducers, orange body fluids
DON'T USE with HIV patients bc affects mitochondrial synthesis of RNA
Tetracycline (resistance)
decrease uptake or increase transport out of cell
Macrolides (resistance)
methylation of rRNA
Azoles (MAO)
inhibit fungal sterol synthesis (blocks 14-alpha-demethylase)
Flucytosine (MAO and toxicity)
inhibits DNA synthesis by conversion to 5-fluorouracil
bone marrow suppression
Caspofugin (MAO and clinical use)
inhibits cell wall synthesis by inhibiting synthesis of B-glucan
used for invasive aspergillosis
Terbinafine (MAO and clinical use)
inhibits squalene epoxidase
used to treat dermatophytoses
Griseofulvin (MAO)
interferes microtubule function; disrupts mitosis
Griseofulvin (clinical use and toxicity)
dermatophytoses (oral treatment)
P-450 inducer, teratogenic, carcinogenic
Amantadine (MAO)
blocks viral penetration/uncoating
M2 protein
Amantadine (clinical use and toxicity)
Influenza A and Parkinson's disease
toxicity: ataxia, slurred speech, dizziness (DRUNK)
Zanamivir, Oseltamivir (MAO)
inhibit influenza neuraminidase
Acyclovir (MAO)
Inhibits DNA synthesis in HSV, VZV, and EBV. Activated by viral thymidine kinase (TK- strains are resistant).
Acyclovir (toxicity)
crystalline nephropathy
Ganciclovir (MAO)
Inhibits DNA synthesis. Effective against herpes viruses CMV and HSV; for CMV requires bioactivation via viral phosphotransferase.
Ganiciclovir (toxicity)
leukopenia, neutropenia, thrombocytopenia, renal toxicity
Foscarnet (MAO)
Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase.
Foscarnet (clinical use and toxicity)
Uses: CMV retinitis in immunocomp pts. when gancyclovir fails. Tox: Nephrotoxicity
Protease Inhibitors (-navir) (MAO)
inhibit maturation of new virus by blocking protease in progeny virus
ritonavir P450 inhibitor
Protease Inhibitors (toxicity)
GI intolerance, hyperglycemia, kidney stones, thrombocytopenia
NRTI (names)
Zidovudine, Abacavir, Didanosine (ddI), Lamivudine (3TC), Stavudine (d4T), and Zalcitabine (ddC
NNRTI (names)
Efavirenz, Declaviridine, Nevirapine
Reverse transcriptase inhibitors (MAO)
inhibit reverse transcriptase of HIV
inhibits 5' -->3' phosphodiester linkage formation
Reverse transcriptase inhibitors (toxicity)
bone marrow suppression, peripheral neuropathy, lactic acidosis (NRTI), rash (NNRTI)
Enfuviritide (MAO)
bind viral gp41 subunit
inhibit conformational change required for fusion with CD4 cells
Maraviroc (MAO)
blocks CCR5 protein on T-cell surface to prevent viral entry
Interferons (MAO)
Glycoproteins synthesized by virus-infected cells block replication of both RNA and DNA viruses
Interferon alpha
used in hep B and C, kaposi's sarcoma
interferon beta
Multiple sclerosis
interferon gamma
NADPH oxidase deficiency
Praziquantel (MAO and clinical use)
Increases membrane permeability to Ca2+ causing muscle contraction followed by paralysis.
Used for flukes and tapeworms
Ivermectin (MAO)
Intensifies GABA-mediated neurotransmission in nematodes, but no access to CNS in humans.
Mebendazole (MAO)
Inhibits microtubule synthesis and glucose uptake in
Sodium Stibogluconate (MAO)
Inhibits glycolysis at PFK reaction. Used against LESHMANIA DONOVANI.
Nifurtimox (MAO and clinical use)
Forms intracellular oxygen radicals, which are toxic to the organism. Used against TRYPANOSOMA CRUZI.
Cyclosporine (MAO)
inhibits calcineurin --> prevents production of IL-2 and its receptor
Cyclosporine (toxicity)
nephrotoxic, gingival hyperplasia, hirtuism
Tacrolimus (FK506) MAO
binds to FK-binding protein --> inhibiting secretion of IL-2
Azathioprine (MAO)
precursor of 6-mercaptopurine
interfers with metabolism and synthesis of nucleic acids
Muromonab-CD3 (OKT3) MAO
monoclonoal antibody that binds to CD3 on the surface of T cells
Sirolimus (MAO
blocks tyrosine kinase. binds to mTOR.
inhibit T-cell proliferation in response to IL-2
Clinical use for Aldesleukin (interleukin2)
renal cell carcinoma
metastatic melanoma
Clinical use for erythropoietin
Anemia esp in renal failure
alpha 1 receptor
increase vascular smooth muscle contraction, pupil dilator muscle (mydriasis), increase intestinal and bladder sphincter muscle contraction, decrease renin release
alpha 2 receptor
decrease insulin release, decrease sympathetic outflow
Beta 1 receptor (heart and kidney)
increase HR, contractility, renin release
Beta 2 receptor
vasodilation, bronchodilation, increase heart rate and contractility, increase insulin release, decrease uterine tone
M2 (heart)
decrease HR and contractility of atria
M3 (peripheral)
increase exocrine gland secretions, miosis, accommodation
Cholinomimetic. Activates bowel and bladder smooth muscle. Resistant to AChE. Uses: Postoperative and neurogenic ileus and urinary retention
Cholinomimetic. ACh analog. Uses: Glaucoma, pupillary constriction, and relief of intraocular pressure.
Cholinomimetic. Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle). Resistant to AChE. Uses: Glaucoma, Sjoren, Stimulator of tears, sweat, and saliva.
Cholinesterase inhibitor. Increase endogenous ACh. Little CNS effect. Uses: Postoperative ileus and urinary retention, MG, reversal of neuromuscular blockade.
Glaucoma, crosses BBB. atropine overdose
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation.
Antidote: Atropine + pralidoxime
Muscarnic antagonists
Atropine, Benztropine, Scopolamine, Ipratropium, Oxybutyin, Methscopalamine
toxicity: "red as a beet, dry as a bone, blind as a bat, mad as a hatter, hot as a hare"
Don't use Atropine in ...
acute angle glaucoma in elderly
urinary retention
hyperthermia in infants
Nicotinic antagonist (blocks para and sympathetic). Uses: Ganglionic blocker. In experimental models, prevents vagal reflex responses to changes in blood pressure - prevents reflex brady.
Hexamethonium (toxicity)
Tox: Orthostatic Hypotension, Blurred vision, constipation, sex dysfunction
Epinephrine (MAO)
Direct sympathomimetics. affinity for all receptors. low doses (B1), high doses (alpha1).
Epinephrine (clinical use)
anaphylaxis, glaucoma (open angle), asthma, hypotension
Epinephrine (toxicity)
tachycardia, hypertension, MI, pulmonary edema and hemorrhage
Norepinephrine (MAO)
Adrenoceptor agonist prototype: acts at B1- and all A adrenoceptors
increase BP, TPR, HR and pulse pressure
Norepinephrine (clincal use and toxicity)
Tox: ischemia, arrhythmias, HTN, reflex bradycardia.
Isopropterenol (low dose epi)
B1 and B2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, tremor, angina.
Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow (low dose) and positive inotropic effects (moderate dose).
increase HR, contractility, conduction velocity and myocardial oxygen consumption
Dobutamine (clinical use)
shock, heart failure, cardiogenic shock
A1 > A2. Uses: Pupillary dilation, vasoconstriction, nasal decongestion
B2 selective agonist
Metaproterenol, Albuterol, Salmeterol, Terbutaline
Nonselective alpha blockers
Phenoxybenzamine (irreversible)
phentolamine (reversible)
Used in pheochromocytoma. Tox: excess hypotension; GI distress.
Prazosin, Terazosin, "-osins"
Alpha1-selective blocker prototype: used in HTN and benign prostatic hyperplasia. Tox: first-dose orthostatic hypotension but less reflex tachycardia than nonselective a blockers.
Alpha 2 blockers
Mirtazapine (depression) and Yohimbine
Tox: sedation, increase serum cholesterol and appetite
(Inducers) Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically
Quinidine, Barbiturates, St. John's wort, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, Chronic alcohol use
metabolized faster where it doesn't work
(Inhibitors) Inhibit yourself from drinking beer from a KEG because it makes you Acutely SICk
Sulfonamides, Isoniazid, Cimetidine, Ketoconazole, Erythromycin, Grapefruit juice, Acute alcohol use
HMG-CoA reductase inhibitors (MAO)
inhibit cholesterol precursor, upregulates LDL receptors
HMG-CoA reductase inhibitors (toxicity)
myopathy (rhabdomyolysis)
Niacin (MAO)
inhibits lipolysis in adipose tissue.
reduces hepatic VLDL secretion into circulation
Niacin (toxicity)
flushed skin (decresed by aspirin)
Bile acid resins (cholestyramines)
Prevent intestinal reabsorption of bile acids. Liver must use cholesterol to make more
Bile acid resins (toxicity)
GI discomfort, decrease absorption of fat-soluble vitamins. GALLSTONES
Fibrates (MAO)
upregulate LPL--> increase in TG clearance
Fibrates (toxicity)
Antihypertensive. Arteriolar vasodilator, orally active. Uses: Severe HTN, CHF, HTN in preg (with Methyldopa). Metabolized by Acetylation. Tox: Tachycardia, Salt and H2O retention, Lupus like syndrome.
K+ channel opener that hyperpolarizes and relaxes vascular smooth muscle. Uses: Severe HTN, baldness. Tox: Hypertrychosis, Pericadial effusion, Reflex tachy, Angina, Salt retention.
Dyhydropiridine calcium channel blocker. Vasoselective (N>D>V). Uses: Hypertension, Angina, Printzmetal's angina, Reynaud's. Tox: Cardiac depression, AV block, edema, flushing, dizziness, constipation.Others: Amlodipine (HF), Nimodipine (subarachnoid hemmorhage), Nicardipine
D1 receptor antagonist. Relaxes smooth muscle. Powerful vasodilator. Uses: Hypertensive emergencies
Cardiac glycoside. Direct inhibitor of Na+/K+ pump leading to indirect inhibition of Na+/Ca++ exchanger and increasing intracellular calcium levels. Stim. vagus. T1/2 40hrs. Uses: CHF, A-fib. Tox: Calcium overload arrhythmias, GI upset.
Class 1A antiarrhythmic
Quinidine, Procainamide, Disopyramide
. Uses: Atrial and vetricular arrhythmias. Tox: Cinchonism - headache, tinnitus, Thrombocytopenia, Torsades. Others: Procainamide, Dysopyramide. Increase AP
Class 1B antiarrhythmic.
Lidocaine, Mexiletine, Tocainide
Selectively affects ischemic or depolarized vent. tissue. Uses: Acute V-arrhythmias (post MI) and digoxin tox. Tox: Local anesthetic, CNS stim/ dep, cardiovascular depression. Others: Mixeiletine (Oral), Tocainide. Decrease AP
Class 1C antiarrhythmic
Flecainide, Encainide, Propafenone
Class 1C antiarrhythmic. No effect on AP. Uses: V-tach and rapid SVT with WPW. Tox: Proarrhythmic (post MI), Prolongs refractory period in AV. Others: Encainide, Propafenone
Unclassified antiarrhythmic. Parenteral only. Hyperpolarizes AV nodal tissue causing block for 10 - 15 secs. Very short acting. Uses: Drug of choice in abolishing/ diagnosing SVT. Tox: flushing, hypotension, chest pain
Effective in torsades de pointes and digoxin toxicity.
Lispro, Aspart, Regular Insulin
Short acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
Intermediate acting insulin analog. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
Glargine, Detemir
Long acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
Blocks K+ channels in pancreatic B cells, causing depolarization and release of insulin. Uses: Only DM2. Tox: hypoglycemia, weight gain, cholestatic jaundice
Oral biguanide hypoglycemic. Decreases hepatic gluconeogenesis, Increase Glycolysis, and peripheral glucose uptake (insulin sensitivity). Uses: Oral, can be used in DM1. Minimal hypoglycemia or weight gain. Tox: Lactic acidosis. DON'T use in renal failure
Pioglitazone, Rosiglitazone
peroxisome proliferator-activator receptors (PPARs) enhances target tissue sensitivity to insulin.
Uses: DM2. Tox: weight gain, edema, hepatotoxicity, cardiotoxicity
Acarbose, Miglitol
Alpha-glucosidase inhibitors. Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia. Uses: DM2. Tox: GI disturbances.
Mimetic.(amylin analog) Decreases glucagon release. Uses: DM2. Tox: Hypoglycemia, nausea, diarrhea
GLP-1 analog. Increased insulin, decreased glucagon release. Uses: DM2. Tox: Nausea vomiting, pancreatitis, weight loss
Propylthiouracil, Methimazole
Antithyroid drug. Inhibits tyrosine iodination and coupling reactions. Orally active. Uses: Hyperthyroidism. Tox: Rash, agranulocytosis (rare). Methimazole is a possible teratogen
Levothyroxine, triodothyronine
Thyroid replacement. Uses: Hypothyrodism, myxedema. Tox: Tachycardia, heat intolerance, tremors, arrhythmias.
Decrease production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX2. Uses: Addisons disease, inflammation, immune suppression, asthma. Tox: Cushing's syndrome. Adrenal insufficiency when drug is stopped after chronic use.
Bismuth, Sulfralfate
Binds to ulcer base, provides physical protection, and allows HCO3- secretion to establish pH gradient in mucous layer. Uses: Ulcer healing and traveler's diarrhea.
PGE1 analog. Increased production of mucus and decreased acid secretion
Uses: Orally active prostaglandin used for GI ulcers caused by NSAIDs. Maintenance of ductus arteriousus and induction of labor. Tox: diarrhea, ABORTIFACIENT
Can affect absorption, bioavailability, or excretion of other drugs due to alteration of gastric/ urine pH. Tox: Aluminum Hyd.- conspitation, Mag Hyd. - Diarrhea, Cacium Carb - Hypercalcemia. All can cause hypokalemia.
A combination of Sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflammatory). Activated by colonic bacteria. Uses: UC, Crohn's. Tox: Malaise, nausea, sulfonamide toxicity, reversible oligospermia.
D2 receptor antagonist. Increase resting tone, contractility, LES tone, motility. Uses: Diabetic and post-surgery gastroparesis. Tox: Parkinsonian effects, Restlessness, Drowsiness, Drug interactions with Digoxin and diabetic agents.
chelating agent used in treatment of arsenic poisoning by displacing arsenic ions from sulfhydryl
Thrombolytic. Protein from streptococci that accelerates
plasminogen-to-plasmin conversion. Increase pT and pTT. Uses: Early MI, stroke. Tox: bleeding, allergy. Tox treated with Aminocaproic acid.
Thrombolytic. Human recombinant tissue plasminogen
activator. Used in acute MI (to recanalize the occluded
coronary artery), pulmonary embolism, stroke. Tox: bleeding. Others: Urokinase, APSAC
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. Others: Ticlopidine (higher risk
of neutropenia and TTP)
Alpha agonist used in Glaucoma. Decrease aqueous humor synthesis. No pupillary or visual changes.
B- blockers: Timolol, betaxolol, carteolol
Decrease aqueous humor synthesis. No pupillary or visual changes.
Prostaglandin used in Glaucoma. Increase outflow of aqueous humor. Tox: Darkens color of iris (browning)
Opioid Analgesics (MAO)
agonists at opoid receptors to modulate synaptic transmission-- open K+ channels, close Ca2+ channels --> decrease synaptic transmission
Inhibits release of ACh, NE, 5HT, glutamate, substance P
Opioid Analgesics (Clinical use)
Pain, cough suppression (dextromethorphan), diarrhea (loperamide and diphenoxylate), maintence program for addicts
Opioid Analgesics (Toxicity)
respiratory depression, pinpoint pupils, CNS depression
treat with naloxone
Partial agonist at opioid mu receptors, agonist at kappa receptors. Uses: Pain, causes less resp. depression than full agonists. Tox: Causes withdrawal if on full opioid agonist.
Tramadol (MOA)
inhibits NE and serotonin reuptake (works at multiple receptors)
Phenytoin (MAO)
Anticonvulsant. Used for tonic-clonic and partial seizures;
blocks Na+ channels in neuronal membranes. Inhibit glutamate release from excitatory presynaptic neuron. Serum levels
variable because of first-pass metabolism and nonlinear
elimination kinetics
Phenytoin (toxicity)
sedation, diplopia, gingival
hyperplasia, hirsutism, peripheral neuropathy, nystagmus, megaloblastic anemia, teratogenic potential (cleft palate). Drug interactions
via induction of hepatic metabolism. CYP450 INDUCER.
Barbiturates (MAO)
Facilitate GABA by increasing DURATION of Cl- channel opening --> decrease neuron firing
Barbiturate (clinical use)
sedative for anxiety, seizures, insomia
Barbiturate (toxicity)
additive CNS depression with alcohol, respiratory and CV depression. Induction of P450
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.
Newer antiepiliptic drug for absence and partial seizures; also
used in bipolar affective disorder. Tox: Steven's Johnson rash, possibly life threatening.
Anticonvulsant: used for tonic-clonic and partial seizures;
blocks Na+ channels in neuronal membranes. DOC
for trigeminal neuralgia; backup drug in bipolar disorder. Tox:
CNS depression, myelotoxic, induces liver drug-metabolizing
enzymes, teratogenicity.
Valproic acid
Anticonvulsant: primary drug in clonic-tonic, absence, and
myoclonic seizure states. Also used commonly for bipolar
disorder. Tox: GI distress, hepatic necrosis (rare), teratogenic
(spina bifida), inhibits drug metabolism.
Anticonvulsant: primary in absence seizures; may block T-type Ca2+ channels in thalamic neurons. Tox: GI distress; safe in
Baclofen (MOA)
binds to GABAb. increase K+ efflux. hyperpolarization
Benzo's (MAO)
Facilitate GABAa action by increasing FREQUENCY of Cl- channel opening. decrease REM sleep
Benzo's (clinical use)
anxiety, spastic, status epilepticus, detox, night terrors and sleepwalking
Benzo's (toxicity)
treat overdose with Flumazenil
Anticonvulsant. Irreversibly inhibits GABA transaminase - increase in GABA.
General anestheti. 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. Others: Fluranes + NO.
Most common drug used for endoscopy. Used adjuntively with gaseous anesthetics and narcotics. May cause severe postoperative respiratory depression, decrease in BP, and amnesia.
PCP analog that acts as dissociative anesthetic. Block NMDA receptors. Cardovascular stimulant. Cause disorientaion, hallucination, and bad dreams. Increase cerebral blood flow.
Depolarizing neuromuscular relaxant. Short duration
(5 min) if patient has normal plasma cholinesterase (genetically
determined). No antidote. Implicated in malignant hyperthermia.
Nondepolarizing neuromuscular blocking agent. Competitive nicotinic blocker (ACh). Releases histamine and may cause hypotension. Analogs: pancuronium, atracurium, vecuronium, and other "-curiums" and "-oniums." Tox: respiratory paralysis. Antidote: cholinesterase inhibitor, eg, neostigmine.
Dantrolene (clinical use)
used in treatment of malignant hyperthermia and to treat neuroleptic malignant syndrome
Dantrolene (MAO)
prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle by blocking ryanodine receptors
Agonize dopamine receptors
Bromocriptine, pergolide, pramipexole, ropinirole
Prevent dopamine breakdown
Selegine (MAO type b inhibitor)
entacapone, tolcapone (COMT inhibitor)
Dopamine precursor: used in parkinsonism, usually combined
with carbidopa (a peripheral inhibitor of dopamine metabolism).
Tox: dyskinesias, hypotension, on-off phenomena, behavioral
Alzheimers drug. NMDA receptor antagonist; Helps prevent excitotoxicity (mediated by Ca++). Tox: Dizziness, confusion, hallucinations
Alzheimers drug. Acetylcholinesterase inhibitors. Tox: Nausea, vomiting, insomnia.
Huntington drugs
Reserpine + tetrabenazine - amine depleting. Haloperidol - dopamine receptor antagonist. Dz - Increase dopamine, decrease GABA + ACh.
5-HT1D receptor agonist: used to abort migraine attacks. Tox:
coronary vasospasm, chest pain, or pressure. Other "triptans":
naratriptan, rizatriptan, zolmitriptan.
Haloperidol + azines
Antipsychotic: blocks brain dopamine D2 receptors (Increase cAMP). Uses: Schizophrenia, Psychosis, Acute mania, Tourette's. Tox: marked EPS dysfunction (Hal, Flu drugs), hyperprolactinemia; neuroleptic malignant syndrome, tardive dyskinesia
fever, encephalopathy, vitals unstable, elevated enzymes, rigidity of muscles
Tardive dyskinesia
Sterotypic oral-facial movements due to long-term antipsychotic use. Often irreversible
Atypical antipsychotic; high-affinity antagonist at 5-HT2 receptors with minimal extrapyramidal side effects; improves
both positive and negative symptoms of schizophrenia. Also OCD, Depression, mania, Tourrette's. Other atypicals: Quetiapine (short half-life), Risperidone (possible EPS dysfunction), Sertindole (QT prolongation).
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, Wt. gain, agranulocytosis (infrequent but significant).
Antimanic prototype: a primary drug in mania and bipolar affective disorders; blocks recycling of the phosphatidylinositol
second messenger system. Tox: tremor, hypothyroidism, diabetes insipidus, goiter, seizures (in overdose), nephrogenic diabetes insipidus, teratogenic potential (Ebstein's malformations).
Anxiolytic: partial agonist that interacts with 5-HT1A receptors; slow onset (1-2 weeks). Uses: GAD. Minimal potentiation of CNS depressants, including ethanol; negligible abuse liability.
TCAs (Imipramine, Amytriptyline, Clomipramine, Doxepin)
blocks reuptake of norepinephrine and serotonin. Uses: Major depression, bedwetting (Imi), OCD (Clop), fibromylagia.
TCAs (toxicity)
atropine-like, postural hypotension, sedation, cardiac arrhythmias in overdose, additive effects with other CNS depressants. 3-C: Convulsions, Coma, and Cardiotox.
SSRIs (Fluoxitine, Paroxitine, Sertaline, Citalopram) (MAO and clinical use)
selective serotonin reuptake inhibitor
Uses: Depression, OCD, Bulimia, Phobias.
SSRI (toxicity)
Tox: CNS stimulation, sexual dysfunction, seizures
in overdose, serotonin syndrome (SS). SS Tx: Cyproheptadine (Serotin receptor antagonist)
Venlafaxine, Duloxetine
Serotonin and NE reputake inhibitors. Uses: Depression. Venla - GAD. Dulo - Diabetic peripheral neruopathy. Tox: Hypertension
Phenelzine, Tranylcypromine, Isocarboxazid (MAO and clinical use)
Irreversible nonselective monoamine oxidase (MAO) inhibitor. Increases level of neurotransmitters. Uses: backup drug for atypical depression, hypochondrias
Phenelzine, Tranylcypromine, Isocarboxazid (toxicity)
Tox: malignant hypertension with indirect-acting sympathomimetics and tyramine, serotonin syndrome with serotonergic drugs.
MAO-B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Uses: Parkinson's disease. Tox: GI distress, CNS stimulation, dyskinesias, serotonin syndrome if used with selective serotonin reuptake inhibitors.
Atypical antidepressant. Used in smoking cessation. Increases NE and dopamine via unknown mech. Tox: Stimulant effect, headache, seizure in bulemic patients.
Atypical antidepressant. Alpha 2 agonist (increase release of NE + Ser) and potent Serotonin receptor antagonist. Used in anorexia. Tox: Sedation, Increased appetite, weight gain, ortho hypotension.
Atypical antidpressant. Primarily inhibits serotonin reuptake. Used for insomnia, as high doses are needed for anti-depressant effects. Tox: Sedation, nausea, priapism, postural hypotension