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4.1.08

Key Drugs in Pharmacology

The following list is a compilation of the drugs that are most likely to appear on the USMLE examination
(and on UCSF exams as well). Abbreviations: ACE, angiotensin−converting enzyme; ANS, autonomic nervous system; AV, atrioventricular;
BP, blood pressure; BPH, benign prostatic hyperplasia; CHF, congestive heart failure; CNS, central nervous system;
CV cardiovascular system; ECG, electrocardiogram; ENS, enteric nervous system; EPS, extrapyramidal system; GI,
gastrointestinal; HR, heart rate; HTN, hypertension; MI, myocardial infarction; NM, neuromuscular; PANS,
parasympathetic autonomic nervous system; SANS, sympathetic autonomic nervous system; Tox, toxicity; WBC,
white blood cells.

Drug Properties
Abciximab Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets. Used to prevent
clotting after coronary angioplasty
Acetaminophen Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti−inflammatory. Less
toxic than aspirin but more dangerous in overdose (causes hepatic necrosis−antidote:
acetylcysteine)
Acetazolamide, dorzolamide Carbonic anhydrase inhibitor diuretic: produces a NaHCO3 diuresis, results in bicarbonate
depletion, and therefore has self−limited action. Used in glaucoma and mountain sickness.
Dorzolamide is a topical analog for glaucoma
Acetylcholine Cholinomimetic prototype: transmitter in CNS, ENS, all ANS ganglia, parasympathetic
postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and some
skeletal muscle vasodilator synapses
Acyclovir Antiviral: inhibits DNA synthesis in herpes simplex and varicella zoster. Requires
activation by viral thymidine kinase (TK− strains are resistant). Tox: behavioral effects and
nephrotoxicity (crystalluria), but not myelosuppression
Adenosine Antiarrhythmic: unclassified ("Group V"); parenteral only. Hyperpolarizes AV nodal
tissue, blocks conduction for 10−15 sec. Used for nodal reentry arrhythmias
Allopurinol Antigout: inhibitor of xanthine oxidase; reduces production of uric acid
Albuterol, metaproterenol,
terbutaline
Important â2−agonists; used mainly for asthma.
Alprazolam Benzodiazepine sedative−hypnotic: widely used in anxiety states, selectivity for panic
attacks and phobias; possible antidepressant actions. Tox: psychologic and physical
dependence, additive effects with other CNS depressants
Alteplase (rt−PA) Thrombolytic: human recombinant tissue plasminogen activator. Used in acute MI to
recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke. Tox:
bleeding
Amiloride K+−sparing diuretic: blocks Na+ channels in cortical collecting tubules
Aminoglutethimide Nonsteroid inhibitor of steroid synthesis: reduces conversion of cholesterol to the hormone
precursor, pregnenolone. Used in metastatic breast cancer



Amiodarone Group IA and III antiarrhythmic: broad spectrum, blocks sodium, potassium, calcium
channels, beta receptors. High efficacy and very long half−life (weeks−months). Tox:
deposits in tissues; hypo− or hyperthyroidism; pulmonary fibrosis
Amitriptyline Tricyclic antidepressant: blocks reuptake of norepinephrine and serotonin. Tox: atropine−
like, postural hypotension, sedation; cardiac arrhythmias in overdose, additive effects with
other CNS depressants
Amoxicillin Penicillin: wider spectrum than pen G with activity similar to ampicillin but greater oral
bioavailability; less adverse effects on GI tract than ampicillin. Susceptible to
penicillinases unless used with clavulanic acid. Tox: penicillin allergy
Amphetamine Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings.
Marked CNS stimulant actions; high abuse liability. Tox: psychosis, HTN, MI, seizures
Amphotericin B Antifungal: polyene drug of choice for most systemic mycoses; binds to ergosterol to
disrupt fungal cell membrane permeability. Tox: chills and fever, hypokalemia,
hypotension, nephrotoxicity (dose−limiting, possibly less with liposomal forms)
Ampicillin Penicillin: wider−spectrum than pen G, susceptible to penicillinases unless used with
sulbactam. Activity similar to pen G, plus E coli, H influenzae, P mirabilis, Shigella.
Synergy with aminoglycosides versus enterococci and listeria. Tox: penicillin allergy; more
adverse effects on GI tract than other penicillins; maculopapular skin rash
Anistreplase (APSAC) Thrombolytic: bacterial streptokinase complexed with human plasminogen. Longer acting
in body than other thrombolytics (rt−PA, streptokinase, urokinase). Tox: bleeding, allergy
to streptococcal protein
Aspirin NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet
agent as well as antipyretic analgesic anti−inflammatory drug
Atenolol Beta1−selective blocker: low lipid solubility, less CNS effect; used for HTN. (Note
mnemonic for beta1−selective blockers: their names start with A through M. [Exceptions:
carteolol & labetalol are not selective])
Atropine Muscarinic cholinoceptor blocker prototype: lipid soluble, CNS effects. Tox: "red as a
beet, dry as a bone, mad as a hatter," urinary retention, mydriasis
Azithromycin Antibiotic: similar to erythromycin, but greater activity versus chlamydia and streptococci;
long half−life due to tissue accumulation. Tox: GI distress, but no inhibition of drug
metabolism
Baclofen GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord
Benztropine Centrally acting antimuscarinic prototype for parkinsonism
Bethanechol Muscarinic agonist: choline ester with good resistance to cholinesterase; used for atonic
bowel or bladder
Botulinum Toxin: enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins
to block release of acetylcholine vesicles
Bromocriptine Ergot derivative: dopamine agonist in CNS; inhibits prolactin release. Used in
parkinsonism and hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
Bupivacaine Long−acting amide local anesthetic prototype: greater CV toxicity than most local
anesthetics
Buspirone Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal
potentiation of CNS depressants including ethanol; negligible abuse liability



Captopril ACE inhibitor prototype: used in HTN, diabetic renal disease, and CHF. Tox:
hyperkalemia, fetal renal damage, cough ("sore throat")
Carbachol Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to
cholinesterase; used for glaucoma (not a first−line drug)
Carbamazepine Anticonvulsant: tricyclic derivative used for tonic−clonic and partial seizures; blocks Na+
channels in neuronal membranes. Drug of choice for trigeminal neuralgia; back−up drug in
mania. Tox: CNS depression, hematotoxic, induces liver drug−metabolizing enzymes
Cefazolin 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
Cefoxitin Second−generation cephalosporin: active against a wide spectrum of gram−negative
bacteria including anaerobes (B fragilis). Does not enter the CNS
Ceftriaxone Third−generation cephalosporin: active against resistant bacteria including gonococci, H
influenzae, and other gram−negative organisms. Crosses the blood−brain barrier
Celecoxib, rofecoxib First COX−II−selective NSAIDs. Reduced GI toxicity
Chloramphenicol Antibiotic: broad spectrum agent; inhibits protein synthesis (50S); uses restricted to back−
up drug for bacterial meningitis, infections due to anaerobes, Salmonella. Tox: reversible
myelosuppression, aplastic anemia, gray baby syndrome
Chloroquine Antimalarial: blood schizonticide used for treatment and as a chemosuppressant where P
falciparum is susceptible. Tox: GI distress and skin rash at low doses; peripheral
neuropathy, skin lesions, auditory and visual impairment, quinidine−like myocardial
depression at high doses
Chlorpheniramine Antihistamine H1 blocker prototype: Tox: sedation, antimuscarinic
Chlorpromazine Phenothiazine antipsychotic drug prototype: blocks most dopamine receptors in the CNS.
Tox: atropine−like, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation,
seizures (in overdose), additive effects with other CNS depressants
Cholestyramine, colestipol Bile acid−binding resins: sequester bile acids in gut and divert more cholesterol from the
liver to bile acids instead of circulating lipoproteins. Tox: constipation, bloating; interfere
with absorption of some drugs
Cimetidine H2 blocker prototype: used in acid−peptic disease. Tox: inhibits hepatic drug metabolism;
antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine
Ciprofloxacin Fluoroquinolone antibiotic: bactericidal inhibitor of topoisomerases; active against many
gram−negative rods including E coli, H influenzae, Campylobacter, Enterobacter,
Pseudomonas, Shigella. Tox: CNS dysfunction, GI distress, superinfection, collagen
damage (avoid in children and pregnant women). Interactions: caffeine, theophylline,
warfarin
Cisplatin Platinum−containing alkylating cancer chemotherapeutic agent. Used for several
solid tumors (eg, testes, lung). Carboplatin is similar.
Clindamycin Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); active against
gram−positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis
Clomiphene Estrogen partial agonist: synthetic used in infertility to induce ovulation
Clonidine Alpha2 agonist: acts centrally to reduce SANS outflow, lowers BP. Tox: rebound HTN if
stopped suddenly



Clozapine Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5−HT2A
receptors; less EPS adverse effects than other antipsychotic drugs. Tox: ANS effects,
agranulocytosis (infrequent but significant)
Cocaine Indirectly acting sympathomimetic: blocks amine reuptake into nerve endings. Local
anesthetic (ester type). Marked CNS stimulation, euphoria; high abuse liability. Tox:
psychosis, cardiac arrhythmias, seizures
Colchicine Microtubule assembly inhibitor: reduces mobility and phagocytosis by WBCs in gout−
inflamed joints; useful in acute, not chronic gout. Tox: GI, hepatic, renal damage
Cyclopentolate, tropicamide Antimuscarinics for ophthalmology: shorter duration than atropine (a few hours or less);
cause cycloplegia and mydriasis
Cyclophosphamide Antineoplastic, immunosuppressive: cell cycle−nonspecific alkylating agent. Tox:
alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression
Cyclosporine Immunosuppressant: antibiotic; inhibits interleukin−2 synthesis, suppresses T cells. Tox:
HTN, hirsutism, nephrotoxicity (dose−limiting), seizures (in overdose). Not a
myelosuppressant
Dantrolene Blocks Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Used in muscle spasm
(cerebral palsy, multiple sclerosis, cord injury) and in emergency treatment of
hyperthermia caused by malignant hyperthermia, malignant neuroleptic syndrome, and
serotonin syndrome
DDAVP ADH analog: synthetic peptide used for pituitary diabetes insipidus
DDT Insecticide: prevents inactivation of sodium channels, causes uncontrolled neuronal
activity. Stored for years in body fat in mammals, birds, fish
Deferoxamine Chelator: bacterial product; chelates iron very avidly, aluminum less so
Dexfenfluramine 5−HT reuptake inhibitor and receptor agonist previously used as anorexic. Tox: produced
cardiac valve damage when used in combination with phentermine
Dexamethasone Glucocorticoid: very potent, long−acting; no mineralocorticoid activity
Diazepam Benzodiazepine prototype: binds to BDZ receptors of the GABAA receptor−chloride ion
channel complex; facilitates the inhibitory actions of GABA by increasing frequency of
channel opening. Uses: anxiety states, ethanol detoxication, muscle spasticity, status
epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS
depressants
Didanosine (DDI) Antiviral: nucleoside inhibitor of HIV reverse transcriptase. Tox: peripheral neuropathy,
pancreatitis
Digitoxin Cardiac glycoside: half−life 168 h, excreted in the bile (partially as digoxin); subject to
enterohepatic circulation. See digoxin
Digoxin Cardiac glycoside prototype: positive inotropic drug for CHF, half−life 40 h; renal
excretion; inhibits Na+/K+ ATPase, also a cardiac parasympathomimetic. Tox: calcium
overload arrhythmias, GI upset
Diltiazem Calcium channel (L−type) blocker prototype: like verapamil, has more depressant effect on
heart than dihydropyridines (eg, nifedipine). Tox: AV block, CHF, edema, constipation
Dimercaprol (BAL) Chelator (British AntiLewisite): used for arsenic, lead, and mercury poisoning



Dioxin (TCDD) Toxin: byproduct of the manufacture of herbicides 2,4−D and 2,4,5−T. Tox: extremely
potent carcinogen in guinea pigs; poorly documented in humans except for chloracne, a
skin disorder that occurs acutely upon exposure
Diphenhydramine Antihistamine H1 blocker prototype: used in hayfever, motion sickness, dystonias. Tox:
antimuscarinic, anti−alpha, sedative
Disopyramide Group IA antiarrhythmic: used for ventricular arrhythmias. Tox: strong antimuscarinic;
may cause CHF
Dopamine Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal
blood flow, stimulate heart
Doxorubicin Antineoplastic: anthracycline drug (cell cycle−nonspecific); intercalates between base pairs
to disrupt DNA functions and forms cytotoxic free radicals. Tox: cardiotoxicity,
myelosuppression
Doxycycline Tetracycline antibiotic: protein synthesis inhibitor (30S), more effective than other
tetracyclines against bacillary dysentery. Unlike other tetracyclines, it is eliminated mainly
in the feces. Tox: see tetracycline
Echothiophate Organophosphate cholinesterase inhibitor: less lipid soluble than most organophosphates;
used in glaucoma
Edetate (EDTA) Chelating agent: used in lead poisoning. Tox: renal tubular necrosis
Edrophonium Cholinesterase inhibitor: very short duration of action (15 min). Used to reverse NM
blockade and as diagnostic test in myasthenia gravis
Enoxaparin Low molecular weight heparin. Primary effect is anti−factor X. Other low molecular
weight heparin−like products: dalteparin, danaparoid. Tox: bleeding
Ephedrine Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more
smooth muscle effects
Epinephrine Adrenoceptor agonist prototype: product of adrenal medulla, some CNS neurons. Affinity
for all alpha and all beta receptors. Used in asthma; as hemostatic and adjunct with local
anesthetics; drug of choice in anaphylaxis
Ergonovine Ergot alkaloid: uterine effect prototype, causes prolonged uterine contraction. Used in
post−partum bleeding
Ergotamine Ergot alkaloid: vascular effect prototype, causes prolonged vasoconstriction, uterine
contraction. Used in migraine, obstetrics
Erythromycin Macrolide antibiotic: inhibitor of protein synthesis (50S); activity includes gram−positive
cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis. Tox: cholestatic
jaundice, inhibits liver drug−metabolizing enzymes, interactions with astemizole,
theophylline, terfenadine, warfarin
Ethacrynic acid Loop diuretic: not a sulfa derivative. Tox: like furosemide but does not increase serum uric
acid.
Ethanol Sedative−hypnotic: acute actions include impaired judgment, ataxia, loss of consciousness,
vasodilation, and cardiovascular and respiratory depression. Chronic use leads to
dependence and liver, cardiovascular, endocrine, gastrointestinal, hepatic, and nervous
system pathology. Note: zero−order elimination kinetics
Ethosuximide Anticonvulsant: used in absence seizures; may block T−type Ca2+ channels in thalamic
neurons. Tox: GI distress but safe in pregnancy



Etidronate, pamidronate,
alendronate
Bisphosphonates: reduce turnover of bone calcium. Used in Paget’s disease, osteoporosis;
alendronate increases bone formation. Tox: severe esophageal ulceration
Fexofenadine 2nd generation antihistamine; does not enter CNS, little or no sedation
Finasteride Steroid inhibitor of 5á−reductase: inhibits synthesis of dihydrotestosterone, the active
androgen in prostate. Used in BPH
Flecainide Group IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial
arrhythmias with Wolff−Parkinson−White syndrome. Tox: arrhythmogenic, CNS
excitation
Fluconazole Imidazole antifungal: used for esophageal candidiasis and in coccidioidomycoses; high
CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients
Fludrocortisone Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long
duration of action
Flumazenil Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of
benzodiazepines (overdose or when used in anesthesia)
Fluorouracil Antineoplastic: pyrimidine antimetabolite (cell cycle−specific) causes "thymine−less" cell
death; used mainly for solid or superficial tumors. Tox: GI distress, myelosuppression
Fluoxetine Antidepressant: serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse
effects and cardiotoxic potential than tricyclics. Tox: CNS stimulation, seizures in
overdose
Flutamide Androgen receptor inhibitor: nonsteroid used in prostatic carcinoma
Furosemide Loop diuretic prototype: blocks Na+/K+/2Cl− transporter; high efficacy; used in acute
pulmonary edema, refractory edematous states, hypercalcemia. Tox: ototoxicity, K+
wasting, hypovolemia, increased serum uric acid
Foscarnet Antiviral: effective against CMV and HSV (including TK− strains); Tox: electrolyte
imbalance, nephrotoxicity
Ganciclovir Antiviral: effective against CMV; requires bioactivation via thymidine kinase. Tox:
myelosuppression, nephrotoxicity
Gemfibrozil, clofibrate Antilipemics: stimulate lipoprotein lipase in peripheral tissues. Used in
hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia
Gentamicin 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 (post−antibiotic effect) and less toxic
Glipizide, glyburide Oral hypoglycemics: second generation, very potent. Like other sulfonylureas, act by
closing K channels in pancreatic B cells, causing depolarization and release of insulin.
Tox: hypoglycemia
Glucagon Hormone product of pancreatic A cells. Increases blood sugar via increased cAMP
Guanethidine Postganglionic sympathetic neuron blocker: enters nerve ending by means of uptake−1 and
is stored in the ending (effect reversed by TCAs, cocaine). Tox: severe orthostatic
hypotension, sexual dysfunction
Haloperidol Antipsychotic butyrophenone: blocks brain dopamine D2 receptors. Tox: marked EPS
dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines



Halothane General anesthetic prototype: inhaled halogenated hydrocarbon. Causes cardiovascular and
respiratory depression and relaxes skeletal and smooth muscle. Use has decreased due to
sensitization of heart to catecholamines, and occurrence (rare) of hepatitis and malignant
hyperthermia
Heparin Anticoagulant: large polymeric molecule with antithrombin, and anti−factor X activity.
Primary rapid onset, in vitro and in vivo anticoagulation. Antidote: protamine. See also
enoxaparin
Hydralazine Antihypertensive: arteriolar vasodilator, orally active; used in HTN, CHF. Tox:
Tachycardia, salt and water retention, lupus−like syndrome
Hydrochlorothiazide Thiazide diuretic prototype: acts in distal convoluted tubule; blocks Na+/Cl− transporter;
used in HTN, CHF, chronic renal stone syndrome. Tox: increased serum lipids, uric acid,
glucose; K+ wasting
Ibuprofen NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used
in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
Imipenem Antibiotic: carbapenem beta−lactam active against many aerobic and anaerobic bacteria
including penicillinase−producing organisms; a bactericidal inhibitor of cell wall synthesis.
Used with cilastatin (which inhibits metabolism by renal dehydropeptidases). Tox: allergy
(partial cross−reactivity with penicillins), seizures (overdose)
Imipramine Tricyclic antidepressant prototype: blocks reuptake of norepinephrine and serotonin. Tox:
ANS (alpha and muscarinic) blockade, cardiac arrhythmias
Indinavir Antiviral; HIV protease inhibitor used as component of combination regimens in AIDS.
Tox: anemia, nephrolithiasis, inhibits P−450 drug metabolism reactions. Other protease
inhibitors: ritonavir, nelfinavir, saquinavir
Indomethacin NSAID prototype: highly potent. Usually reserved for acute inflammation (eg, acute gout),
not chronic; neonatal patent ductus arteriosus. Tox: GI (bleeding), renal damage
Insulin Hypoglycemic peptide hormone of B (beta) cells of the pancreas: stimulates transport of
glucose into cells and glycogen formation; inhibits lipolysis and protein catabolism
Interferon−á Important cytokine for the treatment of hepatitis B and C infection.
Ipodate Antithyroid: iodine−containing radiocontrast medium; also used in thyrotoxicosis. Reduces
peripheral conversion of T4 to T3; may also reduce release of hormone from thyroid
Ipratropium Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20−30% of
patients. Not as effective as â2 agonists
Isoniazid 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)
Isoproterenol Beta1, beta2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always
causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias,
angina
Ketoconazole Antifungal azole prototype: active systemically; inhibits the synthesis of ergosterol. Used
for C albicans, dermatophytes and for non−life−threatening systemic mycoses. Tox:
hepatic dysfunction, inhibits steroid synthesis and P450−dependent drug metabolism
Labetalol Alpha− and beta−blocker: used in HTN. Tox: AV block, hypotension



Leuprolide 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 prostate carcinoma
Levodopa Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral
inhibitor of dopamine metabolism). Tox: dyskinesias, hypotension, on−off phenomena,
behavioral changes
Lidocaine Local anesthetic, medium duration amide prototype: highly selective use−dependent Group
IB antiarrhythmic; used for nerve block and post MI ischemic ventricular arrhythmias.
Tox: CNS excitation
Lithium Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks
recycling of the phosphatidyl inositol second messenger system. Tox: tremor, diabetes
insipidus, goiter, seizures (in overdose), teratogenic potential (Ebstein’s malformations)
Lovastatin Antilipemic HMG−CoA reductase inhibitor prototype: acts in liver to reduce synthesis of
cholesterol. Other statins: atorvastatin, fluvastatin, pravastatin, simvastatin. Tox: liver
damage (elevated enzymes), muscle damage
LSD Lysergic acid diethylamide, "Acid:" semisynthetic ergot derivative; orally active;
hallucinogen
Malathion Organophosphate insecticide cholinesterase inhibitor: pro−drug converted to malaoxon.
Less toxic in mammals and birds because metabolized to inactive products
Meperidine Opioid analgesic: synthetic, equivalent to morphine in efficacy, but orally bioavailable.
Strong agonist at mu opioid receptors; blocks muscarinic receptors. Tox: see morphine
Mestranol Synthetic estrogen: used in many oral contraceptives
Metformin, phenformin Oral biguanide hypoglycemics: mechanism not understood, different from sulfonylurea
oral hypoglycemics. Some efficacy in the absence of functioning pancreatic B cells
Methadone Opioid analgesic: synthetic mu agonist, equivalent to morphine in efficacy, but orally
bioavailable with longer half−life (used to suppress withdrawal symptoms and in
maintenance programs). Tox: see morphine
Methotrexate Antineoplastic, immunosuppressant: cell cycle−specific drug that inhibits dihydrofolate
reductase. Major dose reduction required in renal impairment. Tox: gastrointestinal
distress, myelosuppression. Leucovorin rescue used to reduce toxicity after very high doses
Methyldopa Antihypertensive: prodrug of methylnorepinephrine, a CNS−active á2 agonist. Reduces
SANS outflow from vasomotor center. Tox: positive Coombs test, hemolysis
Methysergide Ergot alkaloid: used as prophylactic in migraine. Tox: retroperitoneal and subendocardial
fibroplasia
Metoprolol Beta1−selective blocker: used in HTN and for prevention of post−MI sudden death
arrhythmias
Metronidazole Antiprotozoal antibiotic: drug of choice in extraluminal amebiasis and trichomoniasis;
active against bacterial anaerobes including B fragilis and in antibiotic−induced colitis due
to C difficile. Tox: peripheral neuropathy, gastrointestinal distress, ethanol intolerance,
mutagenic potential
Mexiletine Group IB antiarrhythmic drug: like lidocaine but orally active
Mifepristone (RU 486) Progesterone and glucocorticoid inhibitor: abortifacient, antineoplastic



Minoxidil Antihypertensive: pro−drug of minoxidil sulfate, a high efficacy arteriolar vasodilator.
Used in HTN; topically for baldness. Tox: tachycardia, salt and water retention, pericardial
effusion
Misoprostol PGE1 derivative: orally active prostaglandin used to prevent peptic ulcers in patients taking
NSAIDs for arthritis. Tox: diarrhea
Morphine Opioid analgesic prototype: strong mu receptor agonist. Poor oral bioavailability. Effects
include analgesia, constipation, emesis, sedation, respiratory depression, miosis, and
urinary retention. Tolerance may be marked; high potential for psychologic and physical
dependence. Additive effects with other CNS depressants
Nafcillin Penicillinase−resistant penicillin prototype: used for suspected or known staphylococcal
infections; not active against methicillin−resistant staphylococci. Tox: penicillin allergy
Nalbuphine 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
Naloxone Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics
(overdose or when used in anesthesia)
Neostigmine Cholinesterase inhibitor prototype: quaternary nitrogen carbamate with little CNS effect
Nevirapine Prototype nonnucleoside inhibitor of HIV reverse transcriptase (NNRTI).Others : efavirenz,
delavirdine
Niacin Antilipemic: reduces release of VLDL from liver into circulation. Tox: flushing
Nifedipine Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina,
HTN. Tox: constipation, headache
Nitroglycerin Antianginal vasodilator prototype: releases 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
Norepinephrine Adrenoceptor agonist prototype: acts at all alpha and at beta1 adrenoceptors; used as
vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN
Norfloxacin Fluoroquinolone antibiotic: inhibits bacterial DNA gyrase; active against many urinary
pathogens including E coli, H influenzae, Klebsiella, Enterobacter, Pseudomonas,
Serratia. Tox: see ciprofloxacin
Norgestrel Progestin: used in many oral contraceptives and Norplant implantable contraceptive
Olanzapine Atypical antipsychotic; high affinity antagonist at 5HT2A with minimal extrapyramidal side
effects; improves both positive and negative symptoms of schizophrenia
Omeprazole Antiulcer: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach.
Used in Zollinger−Ellison syndrome, gastroesophageal reflux disease (GERD)
Ondansetron, granisetron 5−HT3 receptor blockers: very important antiemetics for cancer chemotherapy; also used
post−operatively to reduce vomiting
Paraquat Toxic herbicide: very small oral (but not inhaled) doses cause lethal pulmonary fibrosis
Parathion Organophosphate acetylcholinesterase inhibitor prototype: used as insecticide. Pro−drug:
converted in body to paraoxon. Other organophosphates: DFP, soman, tabun,
echothiophate. Tox: "DUMBELS" mnemonic (Chapter 7)



Penicillamine Chelator, immunomodulator: copper and sometimes lead, mercury, arsenic. Used in
Wilson’s disease and rheumatoid arthritis
Penicillin G Penicillin prototype: active against common streptococci, gram−positive bacilli, gram−
negative cocci, spirochetes, and enterococci (if used with an aminoglycoside);
penicillinase−susceptible. Tox: penicillin allergy
Phenobarbital Long−acting barbiturate prototype: used as a sedative and for tonic−clonic seizures.
Facilitates GABA−mediated neuronal inhibition (by increasing duration of channel
opening) and may block excitatory neurotransmitters. Partial renal clearance that can be
increased by urinary alkalinization. Chronic use leads to induction of liver drug−
metabolizing enzymes and ALA synthase. Tox: psychologic and physical dependence
liability; additive effects with other CNS depressants
Phenoxybenzamine Alpha−blocker prototype: irreversible action. Used in pheochromocytoma
Phentolamine Alpha−blocker prototype: reversible action. Used in pheochromocytoma
Phenytoin Anticonvulsant: used for tonic−clonic and partial seizures; blocks Na+ channels in neuronal
membranes. Serum levels variable due to first−pass metabolism and dose−dependent
nonlinear elimination kinetics. Tox: sedation, diplopia, gingival hyperplasia, hirsutism,
respiratory depression in overdose, teratogenic potential. Drug interactions via effects on
plasma protein binding or induction of hepatic metabolism
Physostigmine Cholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS
readily. Used in glaucoma
Pilocarpine Muscarinic agonist prototype: tertiary amine alkaloid. May cause paradoxical hypertension
by activating excitatory muscarinic EPSP receptors in postganglionic sympathetic neurons.
Used in glaucoma. Tox: muscarinic excess
Piroxicam NSAID with longest duration of action (t1/2 about 40 h)
Pralidoxime Acetylcholinesterase regenerator: very high affinity for phosphorus in organophosphates
Prazosin, terazosin,
doxazosin
Alpha1−selective blockers: used in HTN. Tox: first−dose orthostatic hypotension
Prednisone Glucocorticoid prototype: potent, short−acting; much less mineralocorticoid activity than
cortisol but more than dexamethasone or triamcinolone
Probenecid 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
Probucol Antilipemic: unknown mechanism; recently withdrawn but new evidence suggests efficacy
in preventing restenosis of coronaries after angioplasty.Tox: causes arrhythmias
Procainamide Group IA antiarrhythmic drug: short half−life; similar to quinidine but may cause lupus
erythematosus
Propranolol Nonselective beta−blocker prototype: local anesthetic action but no partial agonist effect.
Used in HTN, angina, arrhythmias, migraine, hyperthyroidism, tremor. Tox: asthma, AV
block, CHF
Propylthiouracil Antithyroid drug prototype: reduces iodination of tyrosine and coupling of MIT and DIT in
the thyroid; orally active. Tox: rash, agranulocytosis (rare)
Prostacyclin PGI2: prostaglandin vasodilator and inhibitor of platelet aggregation



Pyridostigmine Cholinesterase inhibitor: long−acting (8 h) quaternary carbamate; used in myasthenia
gravis
Quinidine Group IA antiarrhythmic prototype: used in atrial and ventricular arrhythmias. Tox:
cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic
Quinine Antimalarial: blood schizonticide; no effect on liver stages. Isomer of quinidine, same
toxicity
Ranitidine H2 blocker: like cimetidine but less inhibition of hepatic drug metabolism; no
antiandrogenic effects
Reserpine Antihypertensive: 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
Rifampin 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), flu−like syndrome with intermittent
dosing
Risperidone, olanzapine,
sertindole
Newer atypical antipsychotics. Higher potency, more blocking of 5−HT2 receptors than
older antipsychotic agents. Low extrapyramidal toxicity.
Selegiline MAO−B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no
tyramine interactions). Used in parkinsonism as adjunct
Sildenafil Viagra. Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation
causes erection. Important interaction with nitrates.
Streptokinase Thrombolytic: protein from streptococci that accelerates plasminogen−to−plasmin
conversion. Tox: bleeding, allergy
Succimer (DMSA) Chelator: dimercaptosuccinic acid; used to chelate lead and arsenic
Succinylcholine Depolarizing neuromuscular relaxant prototype: short duration (5 min) if patient has
normal plasma cholinesterase (genetically determined). No antidote (compare with
tubocurarine)
Sumatriptan, other "−
triptans"
5−HT1D receptor agonists: used to abort migraine attacks
Tamoxifen, raloxifen Estrogen partial agonists "selective estrogen receptor modulators": used in breast
carcinoma, osteoporosis
Tetracaine Local anesthetic: long−acting ester prototype
Tetracycline Antibiotic: tetracycline prototype; bacteriostatic inhibitor of protein synthesis (30S). Broad
spectrum, but many resistant organisms. Used for Lyme disease, mycoplasmal, chlamydial,
rickettsial infections, chronic bronchitis, acne, cholera; a back−up drug in syphilis. Tox: GI
upset and superinfections (Candida, staphylococci), antianabolic actions, Fanconi’s
syndrome (outdated drug), photosensitivity, dental enamel dysplasia
Tetrodotoxin Toxin: very potent sodium channel blocker; blocks action potential propagation in nerve,
heart, and skeletal muscle. From puffer fish, California newt. Tox: paresthesias, paralysis
Thiazides Diuretic prototype: block Na+/Cl− transporter in distal convoluted tubule; used in HTN,
CHF, chronic stone formers. Tox: K+ wasting; increased serum lipids, uric acid, and
glucose



Thioridazine Antipsychotic phenothiazine: blocks most dopamine receptors in the CNS. Tox: atropine−
like effects (marked), ECG abnormalities, postural hypotension, retinal pigmentation,
sedation, additive effects with other CNS depressants (but less EPS dysfunction than other
phenothiazines)
Thyroxine, triiodothyronine Major hormones produced by the thyroid: stimulate metabolism, growth, and development
Ticarcillin Extended spectrum penicillin active against selected gram−negative bacteria including
Pseudomonas aeruginosa (synergistic with aminoglycosides). Susceptible to penicillinases
unless used with clavulanic acid. Tox: penicillin allergy
Ticlopidine, clopidogrel Newer antiplatelet agents. Used to prevent strokes, postangioplasty occlusion.
Tolbutamide, tolazamide,
chlorpropamide,
acetohexamide
Oral hypoglycemics: older sulfonylurea group. (See glipizide.) Chlorpropamide has longest
duration of action
Trimethoprim−
sulfamethoxazole
Antimicrobial drug combination: causes synergistic sequential blockade of folic acid
synthesis. Active against many gram−negative bacteria including Aeromonas,
Enterobacter, H influenzae, Klebsiella, Moraxella, Salmonella, Serratia, Shigella. Possible
back−up agent for methicillin−resistant staphylococci. Tox: mainly due to sulfonamide;
includes hypersensitivity, hematotoxicity, kernicterus, and drug interactions due to
competition for plasma protein binding
Tubocurarine Nondepolarizing neuromuscular blocking agent prototype: competitive nicotinic blocker.
Releases histamine and may cause hypotension. Analogues: pancuronium, atracurium,
vecuronium, and other "−curiums" and "−curoniums." Antidote: cholinesterase inhibitor,
eg, neostigmine
Tyramine Indirectly acting sympathomimetic prototype: releases or displaces norepinephrine from
stores in nerve endings. Usually inactive by the oral route because of high first pass effect
but will cause potentially lethal hypertensive responses in patients taking MAO inhibitors
Valproic acid Anticonvulsant: used in absence, clonic−tonic, and myoclonic seizure states, migraine
prophylactic. Tox: GI distress, hepatic necrosis (rare), teratogenic (spina bifida); inhibits
drug metabolism
Vancomycin 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)
Verapamil Calcium channel blocker prototype: blocks "L−type" channels; cardiac depressant and
vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation
Vesamicol Inhibitor of vesicle ACh/H+ antiporter in cholinergic nerve endings: prevents storage of
ACh. No clinical applications
Vincristine Antineoplastic plant alkaloid: cell cycle (M phase)−specific agent; inhibits mitotic spindle
formation. Tox: peripheral neuropathy. Compare with vinblastine, a congener that causes
myelosuppression
Warfarin 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
Zanamivir, oseltamivir Neuraminidase inhibitors that can be used to reduce severity and duration of influenza
symptoms. Prevents penetration of the virion.



Zidovudine (AZT) Antiviral: prototype nucleoside inhibitor of HIV reverse transcriptase (NRTI). Tox: severe
myelosuppression. Others: lamivudine, stavudine, didanosine, zalcitabine.
Zolpidem Non−benzodiazepine hypnotic, acts via the BDZ1 (omega1) receptor subtype and is
reversed by flumazenil; less amnesia and muscle relaxation; lower dependence liability

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