Step 1 - Katzung Pharm

Front 1

Abciximab

Back 1

Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets

Used to prevent clotting after coronary angioplasty

Front 2

Acetaminophen

Back 2

Antipyretic analgesic

very weak cyclooxygenase inhibitor

not anti−inflammatory. Less toxic than aspirin but more dangerous in overdose (causes hepatic necrosis−antidote: acetylcysteine)

Front 3

Acetazolamide
dorzolamide

Back 3

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

Front 4

Acetylcholine

Back 4

Cholinomimetic prototype

transmitter in CNS, ENS, all ANS ganglia, parasympathetic postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and some skeletal muscle vasodilator synapses

Front 5

Acyclovir

Back 5

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

Front 6

Adenosine

Back 6

Antiarrhythmic

unclassified ("Group V"); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10−15 sec. Used for nodal reentry arrhythmias

Front 7

Allopurinol

Back 7

Antigout

inhibitor of xanthine oxidase; reduces production of uric acid

Front 8

Albuterol
metaproterenol
terbutaline

Back 8

Important β2−agonists

used mainly for asthma.

Front 9

Alprazolam

Back 9

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

Front 10

Alteplase (rt−PA)

Back 10

Thrombolytic

human recombinant tissue plasminogen activator. Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke.

Tox:
bleeding

Front 11

Amiloride

Back 11

K+−sparing diuretic

blocks Na+ channels in cortical collecting tubules

Front 12

Aminoglutethimide

Back 12

Nonsteroid inhibitor of steroid synthesis

reduces conversion of cholesterol to the hormone precursor, pregnenolone. Used in metastatic breast cancer

Front 13

Amiodarone

Back 13

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

Front 14

Amitriptyline

Back 14

Tricyclic antidepressant

blocks reuptake of norepinephrine and serotonin.

Tox:
atropine− like, postural hypotension, sedation; cardiac arrhythmias in overdose, additive effects with other CNS depressants

Front 15

Amoxicillin

Back 15

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

Front 16

Amphetamine

Back 16

Indirectly acting sympathomimetic

displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability.

Tox:
psychosis, HTN, MI, seizures

Front 17

Amphotericin B

Back 17

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)

Front 18

Ampicillin

Back 18

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

Front 19

Anistreplase (APSAC)

Back 19

Thrombolytic

bacterial streptokinase complexed with human plasminogen. Longer acting in body than other thrombolytics (rt−PA, streptokinase, urokinase).

Tox:
bleeding, allergy to streptococcal protein

Front 20

Aspirin

Back 20

NSAID prototype

inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti−inflammatory drug

Front 21

Atenolol

Back 21

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])

Front 22

Atropine

Back 22

Muscarinic cholinoceptor blocker prototype

lipid soluble, CNS effects.

Tox:
"red as a beet, dry as a bone, mad as a hatter," urinary retention, mydriasis

Front 23

Azithromycin

Back 23

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

Front 24

Baclofen

Back 24

GABA analog, orally active

spasmolytic; activates GABAB receptors in the spinal cord

Front 25

Benztropine

Back 25

Centrally acting antimuscarinic prototype for parkinsonism

Front 26

Bethanechol

Back 26

Muscarinic agonist

choline ester with good resistance to cholinesterase; used for atonic bowel or bladder

Front 27

Botulinum

Back 27

Toxin

enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins to block release of acetylcholine vesicles

Front 28

Bromocriptine

Back 28

Ergot derivative

dopamine agonist in CNS; inhibits prolactin release. Used in parkinsonism and hyperprolactinemia.

Tox:
CNS, dyskinesias, hypotension

Front 29

Bupivacaine

Back 29

Long−acting amide local anesthetic prototype

greater CV toxicity than most local anesthetics

Front 30

Buspirone

Back 30

Anxiolytic

atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability

Front 31

Captopril

Back 31

ACE inhibitor prototype

used in HTN, diabetic renal disease, and CHF.

Tox:
hyperkalemia, fetal renal damage, cough ("sore throat")

Front 32

Carbachol

Back 32

Nonselective muscarinic and nicotinic agonist

choline ester with good resistance to cholinesterase; used for glaucoma (not a first−line drug)

Front 33

Carbamazepine

Back 33

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

Front 34

Cefazolin

Back 34

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

Front 35

Cefoxitin

Back 35

Second−generation cephalosporin

active against a wide spectrum of gram−negative bacteria including anaerobes (B fragilis). Does not enter the CNS

Front 36

Ceftriaxone

Back 36

Third−generation cephalosporin

active against resistant bacteria including gonococci, H influenzae, and other gram−negative organisms. Crosses the blood−brain barrier

Front 37

Celecoxib
rofecoxib

Back 37

First COX−II−selective NSAIDs. Reduced GI toxicity

Front 38

Chloramphenicol

Back 38

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

Front 39

Chloroquine

Back 39

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

Front 40

Chlorpheniramine

Back 40

Antihistamine H1 blocker prototype



Tox:
sedation, antimuscarinic

Front 41

Chlorpromazine

Back 41

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

Front 42

Cholestyramine
colestipol

Back 42

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

Front 43

Cimetidine

Back 43

H2 blocker prototype

used in acid−peptic disease.

Tox:
inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine

Front 44

Ciprofloxacin

Back 44

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

Front 45

Cisplatin

Back 45

Platinum−containing alkylating cancer chemotherapeutic agent. Used for several solid tumors (eg, testes, lung). Carboplatin is similar.

Front 46

Clindamycin

Back 46

Lincosamide antibiotic

bacteriostatic inhibitor of protein synthesis (50S); active against gram−positive cocci, B fragilis.

Tox:
GI distress, pseudomembranous colitis

Front 47

Clomiphene

Back 47

Estrogen partial agonist

synthetic used in infertility to induce ovulation

Front 48

Clonidine

Back 48

Alpha2 agonist

acts centrally to reduce SANS outflow, lowers BP.

Tox:
rebound HTN if stopped suddenly

Front 49

Clozapine

Back 49

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)

Front 50

Cocaine

Back 50

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

Front 51

Colchicine

Back 51

Microtubule assembly inhibitor

reduces mobility and phagocytosis by WBCs in gout− inflamed joints; useful in acute, not chronic gout.

Tox-
GI, hepatic, renal damage

Front 52

Cyclopentolate
tropicamide

Back 52

Antimuscarinics for ophthalmology

shorter duration than atropine (a few hours or less); cause cycloplegia and mydriasis

Front 53

Cyclophosphamide

Back 53

Antineoplastic, immunosuppressive

cell cycle−nonspecific alkylating agent.

Tox-
alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression

Front 54

Cyclosporine

Back 54

Immunosuppressant

antibiotic; inhibits interleukin−2 synthesis, suppresses T cells.

Tox-
HTN, hirsutism, nephrotoxicity (dose−limiting), seizures (in overdose). Not a myelosuppressant

Front 55

Dantrolene

Back 55

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

Front 56

DDAVP

Back 56

ADH analog

synthetic peptide used for pituitary diabetes insipidus

Front 57

DDT

Back 57

Insecticide

prevents inactivation of sodium channels, causes uncontrolled neuronal activity. Stored for years in body fat in mammals, birds, fish

Front 58

Deferoxamine

Back 58

Chelator

bacterial product; chelates iron very avidly, aluminum less so

Front 59

Dexfenfluramine

Back 59

5−HT reuptake inhibitor and receptor agonist previously used as anorexic.

Tox-
produced cardiac valve damage when used in combination with phentermine

Front 60

Dexamethasone

Back 60

Glucocorticoid

very potent, long−acting; no mineralocorticoid activity

Front 61

Diazepam

Back 61

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

Front 62

Didanosine (DDI)

Back 62

Antiviral

nucleoside inhibitor of HIV reverse transcriptase.

Tox-
peripheral neuropathy, pancreatitis

Front 63

Digitoxin

Back 63

Cardiac glycoside

half−life 168 h, excreted in the bile (partially as digoxin); subject to enterohepatic circulation. See digoxin

Front 64

Digoxin

Back 64

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

Front 65

Diltiazem

Back 65

Calcium channel (L−type) blocker prototype

like verapamil, has more depressant effect on heart than dihydropyridines (eg, nifedipine).

Tox-
AV block, CHF, edema, constipation

Front 66

Dimercaprol (BAL)

Back 66

Chelator (British AntiLewisite)

used for arsenic, lead, and mercury poisoning

Front 67

Dioxin (TCDD)

Back 67

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

Front 68

Diphenhydramine

Back 68

Antihistamine H1 blocker prototype

used in hayfever, motion sickness, dystonias.

Tox-
antimuscarinic, anti−alpha, sedative

Front 69

Disopyramide

Back 69

Group IA antiarrhythmic

used for ventricular arrhythmias.

Tox-
strong antimuscarinic; may cause CHF

Front 70

Dopamine

Back 70

Neurotransmitter and agonist drug at dopamine receptors

used in shock to increase renal blood flow, stimulate heart

Front 71

Doxorubicin

Back 71

Antineoplastic

anthracycline drug (cell cycle−nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals.

Tox-
cardiotoxicity, myelosuppression

Front 72

Doxycycline

Back 72

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

Front 73

Echothiophate

Back 73

Organophosphate cholinesterase inhibitor

less lipid soluble than most organophosphates; used in glaucoma

Front 74

Edetate (EDTA)

Back 74

Chelating agent

used in lead poisoning.

Tox-
renal tubular necrosis

Front 75

Edrophonium

Back 75

Cholinesterase inhibitor

very short duration of action (15 min). Used to reverse NM blockade and as diagnostic test in myasthenia gravis

Front 76

Enoxaparin

Back 76

Low molecular weight heparin

Primary effect is anti−factor X. Other low molecular weight heparin−like products: dalteparin, danaparoid.

Tox-
bleeding

Front 77

Ephedrine

Back 77

Indirectly acting sympathomimetic

like amphetamine but less CNS stimulation, more smooth muscle effects

Front 78

Epinephrine

Back 78

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

Front 79

Ergonovine

Back 79

Ergot alkaloid

uterine effect prototype, causes prolonged uterine contraction. Used in post−partum bleeding

Front 80

Ergotamine

Back 80

Ergot alkaloid

vascular effect prototype, causes prolonged vasoconstriction, uterine contraction. Used in migraine, obstetrics

Front 81

Erythromycin

Back 81

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

Front 82

Ethacrynic acid

Back 82

Loop diuretic

not a sulfa derivative.

Tox-
like furosemide but does not increase serum uric acid.

Front 83

Ethanol

Back 83

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

Front 84

Ethosuximide

Back 84

Anticonvulsant

used in absence seizures; may block T−type Ca2+ channels in thalamic neurons.

Tox-
GI distress but safe in pregnancy

Front 85

Etidronate
pamidronate
alendronate

Back 85

Bisphosphonates

reduce turnover of bone calcium. Used in Paget’s disease, osteoporosis; alendronate increases bone formation.

Tox-
severe esophageal ulceration

Front 86

Fexofenadine

Back 86

2nd generation antihistamine

does not enter CNS, little or no sedation

Front 87

Finasteride

Back 87

Steroid inhibitor of 5α−reductase

inhibits synthesis of dihydrotestosterone, the active androgen in prostate. Used in BPH

Front 88

Flecainide

Back 88

Group IC antiarrhythmic prototype

used in ventricular tachycardia and rapid atrial arrhythmias with Wolff−Parkinson−White syndrome.

Tox-
arrhythmogenic, CNS excitation

Front 89

Fluconazole

Back 89

Imidazole antifungal

used for esophageal candidiasis and in coccidioidomycoses; high CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients

Front 90

Fludrocortisone

Back 90

Synthetic corticosteroid

high mineralocorticoid and moderate glucocorticoid activity; long duration of action

Front 91

Flumazenil

Back 91

Benzodiazepine receptor antagonist

used to reverse CNS depressant effects of benzodiazepines (overdose or when used in anesthesia)

Front 92

Fluorouracil

Back 92

Antineoplastic

pyrimidine antimetabolite (cell cycle−specific) causes "thymine−less" cell death; used mainly for solid or superficial tumors.

Tox-
GI distress, myelosuppression

Front 93

Fluoxetine

Back 93

Antidepressant

serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse effects and cardiotoxic potential than tricyclics.

Tox-
CNS stimulation, seizures in overdose

Front 94

Flutamide

Back 94

Androgen receptor inhibitor

nonsteroid used in prostatic carcinoma

Front 95

Furosemide

Back 95

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

Front 96

Foscarnet

Back 96

Antiviral

effective against CMV and HSV (including TK− strains);

Tox-
electrolyte imbalance, nephrotoxicity

Front 97

Ganciclovir

Back 97

Antiviral

effective against CMV; requires bioactivation via thymidine kinase.

Tox-
myelosuppression, nephrotoxicity

Front 98

Gemfibrozil
clofibrate

Back 98

Antilipemics

stimulate lipoprotein lipase in peripheral tissues. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia

Front 99

Gentamicin

Back 99

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

Front 100

Glipizide
glyburide

Back 100

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

Front 101

Glucagon

Back 101

Hormone product of pancreatic A cells

Increases blood sugar via increased cAMP

Front 102

Guanethidine

Back 102

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

Front 103

Haloperidol

Back 103

Antipsychotic butyrophenone

blocks brain dopamine D2 receptors.

Tox-
marked EPS dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines

Front 104

Halothane

Back 104

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

Front 105

Heparin

Back 105

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

Front 106

Hydralazine

Back 106

Antihypertensive

arteriolar vasodilator, orally active; used in HTN, CHF.

Tox-
Tachycardia, salt and water retention, lupus−like syndrome

Front 107

Hydrochlorothiazide

Back 107

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

Front 108

Ibuprofen

Back 108

NSAID prototype

short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation.

Tox-
peptic ulcer, renal damage

Front 109

Imipenem

Back 109

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)

Front 110

Imipramine

Back 110

Tricyclic antidepressant prototype

blocks reuptake of norepinephrine and serotonin.

Tox-
ANS (alpha and muscarinic) blockade, cardiac arrhythmias

Front 111

Indinavir

Back 111

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

Front 112

Indomethacin

Back 112

NSAID prototype

highly potent. Usually reserved for acute inflammation (eg, acute gout), not chronic; neonatal patent ductus arteriosus.

Tox-
GI (bleeding), renal damage

Front 113

Insulin

Back 113

Hypoglycemic peptide hormone of B (beta) cells of the pancreas

stimulates transport of glucose into cells and glycogen formation; inhibits lipolysis and protein catabolism

Front 114

Interferon−α

Back 114

Important cytokine for the treatment of hepatitis B and C infection.

Front 115

Ipodate

Back 115

Antithyroid

iodine−containing radiocontrast medium; also used in thyrotoxicosis. Reduces peripheral conversion of T4 to T3; may also reduce release of hormone from thyroid

Front 116

Ipratropium

Back 116

Antimuscarinic agent

aerosol for asthma, COPD. Good bronchodilator in 20−30% of patients. Not as effective as β2 agonists

Front 117

Isoniazid

Back 117

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)

Front 118

Isoproterenol

Back 118

Beta1, beta2 agonist catecholamine prototype

bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR.

Tox-
arrhythmias, angina

Front 119

Ketoconazole

Back 119

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

Front 120

Labetalol

Back 120

Alpha− and beta−blocker

used in HTN.

Tox-
AV block, hypotension

Front 121

Leuprolide

Back 121

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

Front 122

Levodopa

Back 122

Dopamine precursor

used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism).

Tox-
dyskinesias, hypotension, on−off phenomena, behavioral changes

Front 123

Lidocaine

Back 123

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

Front 124

Lithium

Back 124

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)

Front 125

Lovastatin

Back 125

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

Front 126

LSD

Back 126

Lysergic acid diethylamide, "Acid"

semisynthetic ergot derivative; orally active; hallucinogen

Front 127

Malathion

Back 127

Organophosphate insecticide cholinesterase inhibitor

pro−drug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products

Front 128

Meperidine

Back 128

Opioid analgesic

synthetic, equivalent to morphine in efficacy, but orally bioavailable. Strong agonist at mu opioid receptors; blocks muscarinic receptors.

Tox-
see morphine

Front 129

Mestranol

Back 129

Synthetic estrogen

used in many oral contraceptives

Front 130

Metformin
phenformin

Back 130

Oral biguanide hypoglycemics

mechanism not understood, different from sulfonylurea oral hypoglycemics. Some efficacy in the absence of functioning pancreatic B cells

Front 131

Methadone

Back 131

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

Front 132

Methotrexate

Back 132

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

Front 133

Methyldopa

Back 133

Antihypertensive

prodrug of methylnorepinephrine, a CNS−active α2 agonist. Reduces SANS outflow from vasomotor center.

Tox-
positive Coombs test, hemolysis

Front 134

Methysergide

Back 134

Ergot alkaloid

used as prophylactic in migraine.

Tox-
retroperitoneal and subendocardial fibroplasia

Front 135

Metoprolol

Back 135

Beta1−selective blocker

used in HTN and for prevention of post−MI sudden death arrhythmias

Front 136

Metronidazole

Back 136

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

Front 137

Mexiletine

Back 137

Group IB antiarrhythmic drug

like lidocaine but orally active

Front 138

Mifepristone (RU 486)

Back 138

Progesterone and glucocorticoid inhibitor

abortifacient, antineoplastic

Front 139

Minoxidil

Back 139

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 PGE1 derivative: orally active prostaglandin used to prevent peptic ulcers in patients taking

Front 140

Misoprostol

Back 140

NSAIDs for arthritis.

Tox-
diarrhea

Front 141

Morphine

Back 141

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

Front 142

Nafcillin

Back 142

Penicillinase−resistant penicillin prototype

used for suspected or known staphylococcal infections; not active against methicillin−resistant staphylococci.

Tox-
penicillin allergy

Front 143

Nalbuphine

Back 143

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

Front 144

Naloxone

Back 144

Opioid mu receptor antagonist

used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)

Front 145

Neostigmine

Back 145

Cholinesterase inhibitor prototype

quaternary nitrogen carbamate with little CNS effect

Front 146

Nevirapine

Back 146

Prototype nonnucleoside inhibitor of HIV reverse transcriptase (NNRTI)

Others : efavirenz, delavirdine

Front 147

Niacin

Back 147

Antilipemic

reduces release of VLDL from liver into circulation.

Tox-
flushing

Front 148

Nifedipine

Back 148

Calcium channel blocker prototype

vasoselective (less cardiac depression); used in angina, HTN.

Tox-
constipation, headache

Front 149

Nitroglycerin

Back 149

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

Front 150

Norepinephrine

Back 150

Adrenoceptor agonist prototype

acts at all alpha and at beta1 adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia.

Tox-
ischemia, arrhythmias, HTN

Front 151

Norfloxacin

Back 151

Fluoroquinolone antibiotic

inhibits bacterial DNA gyrase; active against many urinary pathogens including E coli, H influenzae, Klebsiella, Enterobacter, Pseudomonas, Serratia.

Tox-
see ciprofloxacin

Front 152

Norgestrel

Back 152

Progestin

used in many oral contraceptives and Norplant implantable contraceptive

Front 153

Olanzapine

Back 153

Atypical antipsychotic

high affinity antagonist at 5HT2A with minimal extrapyramidal side effects; improves both positive and negative symptoms of schizophrenia

Front 154

Omeprazole

Back 154

Antiulcer

irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in Zollinger−Ellison syndrome, gastroesophageal reflux disease (GERD)

Front 155

Ondansetron
granisetron

Back 155

5−HT3 receptor blockers

very important antiemetics for cancer chemotherapy; also used post−operatively to reduce vomiting

Front 156

Paraquat

Back 156

Toxic herbicide

very small oral (but not inhaled) doses cause lethal pulmonary fibrosis

Front 157

Parathion

Back 157

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)

Front 158

Penicillamine

Back 158

Chelator, immunomodulator

copper and sometimes lead, mercury, arsenic. Used in Wilson’s disease and rheumatoid arthritis

Front 159

Penicillin G

Back 159

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

Front 160

Phenobarbital

Back 160

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

Front 161

Phenoxybenzamine

Back 161

Alpha−blocker prototype

irreversible action. Used in pheochromocytoma

Front 162

Phentolamine

Back 162

Alpha−blocker prototype

reversible action. Used in pheochromocytoma

Front 163

Phenytoin

Back 163

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

Front 164

Physostigmine

Back 164

Cholinesterase inhibitor prototype

alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma

Front 165

Pilocarpine

Back 165

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

Front 166

Piroxicam

Back 166

NSAID with longest duration of action (t1/2 about 40 h)

Front 167

Pralidoxime

Back 167

Acetylcholinesterase regenerator

very high affinity for phosphorus in organophosphates

Front 168

Prazosin
terazosin
doxazosin

Back 168

Alpha1−selective blockers

used in HTN.

Tox-
first−dose orthostatic hypotension

Front 169

Prednisone

Back 169

Glucocorticoid prototype

potent, short−acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone

Front 170

Probenecid

Back 170

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

Front 171

Probucol

Back 171

Antilipemic

unknown mechanism; recently withdrawn but new evidence suggests efficacy in preventing restenosis of coronaries after angioplasty.

Tox-
causes arrhythmias

Front 172

Procainamide

Back 172

Group IA antiarrhythmic drug

short half−life; similar to quinidine but may cause lupus erythematosus

Front 173

Propranolol

Back 173

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

Front 174

Propylthiouracil

Back 174

Antithyroid drug prototype

reduces iodination of tyrosine and coupling of MIT and DIT in the thyroid; orally active.

Tox-
rash, agranulocytosis (rare)

Front 175

Prostacyclin

Back 175

PGI2

prostaglandin vasodilator and inhibitor of platelet aggregation

Front 176

Pyridostigmine

Back 176

Cholinesterase inhibitor

long−acting (8 h) quaternary carbamate; used in myasthenia gravis

Front 177

Quinidine

Back 177

Group IA antiarrhythmic prototype

used in atrial and ventricular arrhythmias.

Tox-
cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic

Front 178

Quinine

Back 178

Antimalarial

blood schizonticide; no effect on liver stages. Isomer of quinidine, same toxicity

Front 179

Ranitidine

Back 179

H2 blocker

like cimetidine but less inhibition of hepatic drug metabolism; no antiandrogenic effects

Front 180

Reserpine

Back 180

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

Front 181

Rifampin

Back 181

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

Front 182

Risperidone
olanzapine
sertindole

Back 182

Newer atypical antipsychotics

Higher potency, more blocking of 5−HT2 receptors than older antipsychotic agents. Low extrapyramidal toxicity.

Front 183

Selegiline

Back 183

MAO−B inhibitor

selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Used in parkinsonism as adjunct

Front 184

Sildenafil

Back 184

Viagra

Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation causes erection. Important interaction with nitrates.

Front 185

Streptokinase

Back 185

Thrombolytic

protein from streptococci that accelerates plasminogen−to−plasmin conversion.

Tox-
bleeding, allergy

Front 186

Succimer (DMSA)

Back 186

Chelator

dimercaptosuccinic acid; used to chelate lead and arsenic

Front 187

Succinylcholine

Back 187

Depolarizing neuromuscular relaxant prototype

short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote (compare with tubocurarine)

Front 188

Sumatriptan
other "− triptans"

Back 188

5−HT1D receptor agonists

used to abort migraine attacks

Front 189

Tamoxifen
raloxifen

Back 189

Estrogen partial agonists "selective estrogen receptor modulators"

used in breast carcinoma, osteoporosis

Front 190

Tetracaine

Back 190

Local anesthetic

long−acting ester prototype

Front 191

Tetracycline

Back 191

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

Front 192

Tetrodotoxin

Back 192

Toxin

very potent sodium channel blocker; blocks action potential propagation in nerve, heart, and skeletal muscle. From puffer fish, California newt.

Tox-
paresthesias, paralysis

Front 193

Thiazides

Back 193

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

Front 194

Thioridazine

Back 194

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)

Front 195

Thyroxine
triiodothyronine

Back 195

Major hormones produced by the thyroid

stimulate metabolism, growth, and development

Front 196

Ticarcillin

Back 196

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

Front 197

Ticlopidine
clopidogrel

Back 197

Newer antiplatelet agents. Used to prevent strokes, postangioplasty occlusion.

Front 198

Tolbutamide
tolazamide
chlorpropamide
acetohexamide

Back 198

Oral hypoglycemics

older sulfonylurea group. (See glipizide.) Chlorpropamide has longest duration of action

Front 199

Trimethoprim− sulfamethoxazole

Back 199

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

Front 200

Tubocurarine

Back 200

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

Front 201

Tyramine

Back 201

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

Front 202

Valproic acid

Back 202

Anticonvulsant

used in absence, clonic−tonic, and myoclonic seizure states, migraine prophylactic.

Tox-
GI distress, hepatic necrosis (rare), teratogenic (spina bifida); inhibits drug metabolism

Front 203

Vancomycin

Back 203

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)

Front 204

Verapamil

Back 204

Calcium channel blocker prototype

blocks "L−type" channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias.

Tox-
AV block, CHF, constipation

Front 205

Vesamicol

Back 205

Inhibitor of vesicle ACh/H+ antiporter in cholinergic nerve endings

prevents storage of ACh. No clinical applications

Front 206

Vincristine

Back 206

Antineoplastic plant alkaloid

cell cycle (M phase)−specific agent; inhibits mitotic spindle formation.

Tox-
peripheral neuropathy. Compare with vinblastine, a congener that causes myelosuppression

Front 207

Warfarin

Back 207

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

Front 208

Zanamivir
oseltamivir

Back 208

Neuraminidase inhibitors

can be used to reduce severity and duration of influenza symptoms. Prevents penetration of the virion.

Front 209

Zidovudine (AZT)

Back 209

Antiviral

prototype nucleoside inhibitor of HIV reverse transcriptase (NRTI).

Tox
severe myelosuppression. Others: lamivudine, stavudine, didanosine, zalcitabine.

Front 210

Zolpidem

Back 210

Non−benzodiazepine hypnotic

acts via the BDZ1 (omega1) receptor subtype and is reversed by flumazenil; less amnesia and muscle relaxation; lower dependence liability