Pharm

Question 1

Abciximab

Answer 1

Monoclonal antibody that inhibits the binding of platelet glycoprotein IIb/IIIa (GPIIb/IIIa) to fibrinogen. Used to prevent clotting after coronary angioplasty and in acute coronary syndrome. Eptifibatide and tirofiban are also GPIIb/IIIa inhibitors. (34)

Question 2

Acetaminophen

Answer 2

Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti-inflammatory. Less GI distress than aspirin but dangerous in overdose. Tox: hepatic necrosis. Antidote: acetylcysteine. (36)

Question 3

Acetazolamide

Answer 3

Carbonic anhydrase-inhibiting diuretic acting in the proximal convoluted tubule: produces a NaHCO3 diuresis, results in bicarbonate depletion and metabolic acidosis. Has self-limited diuretic but persistent bicarbonate-depleting action. Used in glaucoma and mountain sickness. Tox: paresthesias, hepatic encephalopathy. Dorzolamide and brinzolamide are topical analogs for glaucoma. (15)

Question 4

Acetylcholine

Answer 4

Cholinomimetic prototype: transmitter in CNS, ENS, all ANS ganglia, parasympathetic postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and skeletal muscle end plate synapses. (6, 7)

Question 5

Acyclovir

Answer 5

Antiviral: inhibits DNA synthesis in herpes simplex virus (HSV) and varicella-zoster virus (VZV). Requires activation by viral thymidine kinase (TK− strains are resistant). Tox: behavioral effects and nephrotoxicity (crystalluria) but minimal myelosuppression. Famciclovir, penciclovir, and valacyclovir are similar but with longer half-lives. (49)

Question 6

Adenosine

Answer 6

Antiarrhythmic: miscellaneous group; parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10–15 s. Used for nodal reentry arrhythmias. Tox: hypotension, flushing, chest pain. (14)

Question 7

Albuterol

Answer 7

Prototypic rapid-acting β2 agonist; important use in acute asthma. Tox: tachycardia, arrhythmias, tremor. Other drugs with similar action: metaproterenol, terbutaline. Slow-acting analogs: formoterol, salmeterol; used for prophylaxis. (9, 20)

Question 8

Alendronate

Answer 8

Bisphosphonate: chronic treatment with low doses increases bone mineral density and reduces fractures. Higher doses lower serum calcium. Used in osteoporosis and for the hypercalcemia in Paget’s disease and malignancies. Tox: esophageal irritation at low oral doses. Renal dysfunction and osteonecrosis of the jaw in high doses. Other bisphosphonates include etidronate, pamidronate, risedronate, etc. (42)

Question 9

Allopurinol

Answer 9

Irreversible inhibitor of xanthine oxidase; reduces production of uric acid. Used in gout and adjunctively in cancer chemotherapy. Inhibits metabolism of purine analogs (eg, mercaptopurine, azathioprine). Febuxostat is similar. (36)

Question 10

Alteplase (t-Pa)

Answer 10

Thrombolytic: human recombinant tissue plasminogen activator. Used to recanalize occluded blood vessels in acute MI, severe pulmonary embolism, stroke. Reteplase and tenecteplase are similar. Streptokinase is a bacterial protein with thrombolytic properties. Tox: bleeding. (34)

Question 11

Amiloride

Answer 11

K+-sparing diuretic: blocks epithelial Na+ channels in cortical collecting tubules. Tox: hyperkalemia. (15)

Question 12

Amiodarone

Answer 12

Group 3 (and other groups) antiarrhythmic: broad spectrum; blocks sodium, potassium, calcium channels, β receptors. High efficacy and very long half-life (weeks to months). Tox: deposits in tissues; skin coloration; hypo- or hyperthyroidism; pulmonary fibrosis; optic neuritis. (14)

Question 13

Amphetamine

Answer 13

Indirect-acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability. Used in ADHD, for short-term weight loss, and for narcolepsy. Tox: psychosis, HTN, MI, seizures. Other indirect-acting sympathomimetics that displace catecholamines: ephedrine, pseudoephedrine, methylphenidate, tyramine. (9, 32)

Question 14

Amphotericin B

Answer 14

Antifungal: polyene commonly a drug of choice for systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability. Tox: chills and fever, hypotension, nephrotoxicity (dose limiting; less with liposomal forms). (48)

Question 15

Ampicillin

Answer 15

Penicillin: wider spectrum than penicillin G, susceptible to penicillinases unless used with sulbactam. Activity similar to that of penicillin G, plus E coli, H influenzae, P mirabilis, Shigella. Synergy with aminoglycosides versus Enterococcus and Listeria. Tox: penicillin allergy; more adverse effects on GI tract than other penicillins; maculopapular skin rash. Amoxicillin has greater oral bioavailability and less GI effects; also used with clavulanate, a penicillinase inhibitor. (43)

Question 16

Anastrozole

Answer 16

Aromatase inhibitor: prototype inhibitor of the enzyme that converts testosterone to estradiol. Used in estrogen-dependent breast cancer. Letrozole is similar; exemestane is an irreversible aromatase inhibitor. (40, 54)

Question 17

Aspirin

Answer 17

NSAID prototype: inhibits cyclooxygenase (COX)-1 and -2 irreversibly. Antiplatelet agent as well as antipyretic, analgesic and anti-inflammatory drug. Tox: GI ulcers, nephrotoxicity, rash, hypersensitivity leading to bronchoconstriction, salicylism. Other NSAIDs: ibuprofen, indomethacin, ketorolac, and naproxen. (34, 36)

Question 18

Atenolol

Answer 18

Beta1-selective blocker: low lipid solubility, less CNS effect; used for HTN, angina. (Mnemonic: Generic names of β1-selective blockers start with A through M except for carteolol, carvedilol, and labetalol.) Tox: asthma, bradycardia, AV block, heart failure. (10)

Question 19

Atropine

Answer 19

Muscarinic cholinoceptor blocker prototype: lipid-soluble, CNS effects; antidote for cholinesterase poisoning. Tox: “red as a beet, dry as a bone, blind as a bat, mad as a hatter,” urinary retention, mydriasis. Cyclopentolate, tropicamide: antimuscarinics for ophthalmology; cause cycloplegia and mydriasis. Glycopyrrolate: antimuscarinic with decreased CNS effects. (8, 58)

Question 20

Azithromycin

Answer 20

Macrolide antibiotic: similar to erythromycin but greater activity against H influenzae, chlamydiae, and streptococci; long half-life with renal elimination. Tox: GI distress but no inhibition of drug metabolism. Clarithromycin is similar but has a shorter half-life, and inhibits drug metabolism. (44)

Question 21

Baclofen

Answer 21

GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord. (27)

Question 22

Benztropine

Answer 22

Muscarinic cholinoceptor blocker: centrally acting antimuscarinic prototype for parkinsonism. Tox: excess antimuscarinic effects. (8, 28)

Question 23

Botulinum

Answer 23

Toxins produced by Clostridium botulinum: enzymes that cleave proteins (synaptobrevin, others) and block transmitter release from acetylcholine vesicles. Injected to treat muscle spasm, smooth wrinkles, and reduce excessive sweating. Tox: paralysis. (6, 27)

Question 24

Bromocriptine

Answer 24

Ergot derivative: prototype dopamine agonist in CNS; inhibits prolactin release. Used in hyperprolactinemia and a rarely used alternative drug in parkinsonism. Tox: Various CNS disturbances, dyskinesias, hypotension. (16, 28, 37)

Question 25

Bupivacaine

Answer 25

Long-acting amide local anesthetic prototype. Tox: greater cardiovascular toxicity than most local anesthetics. (26)

Question 26

Buprenorphine

Answer 26

Opioid: long-acting partial agonist of μ receptors. Analgesic (not equivalent to morphine) and effective for detoxification and maintenance in opioid dependence. Other mixed agonist-antagonists: nalbuphine activates κ and weakly blocks μ receptors; pentazocine, κ agonist and weak μ antagonist or partial agonist. (31)

Question 27

Bupropion

Answer 27

Antidepressant and used in smoking cessation: mechanism uncertain, but no direct actions on CNS amines. Tox: agitation, anxiety, aggravation of psychosis and, at high doses, seizures. (30)

Question 28

Calcitonin

Answer 28

Peptide hormone secreted by thyroid gland. Decreases serum calcium and phosphate by decreasing bone resorption. Delivered as a nasal spray and subcutaneous injection. Side effects: rhinitis with nasal spray. (42)

Question 29

Captopril

Answer 29

ACE inhibitor prototype: used in HTN, diabetic nephropathy, and HF. Tox: hyperkalemia, fetal renal damage, cough (“sore throat”). Other “prils” include benazepril, enalapril, lisinopril, quinapril. (11, 13, 17)

Question 30

Carbamazepine

Answer 30

Antiseizure drug: used for tonic-clonic and partial seizures; blocks Na+ channels in neuronal membranes. Drug of choice for trigeminal neuralgia; backup drug in bipolar disorder. Tox: CNS depression, myelotoxic, induces liver drug-metabolizing enzymes, teratogenicity. (24, 29)

Question 31

Carvedilol

Answer 31

Adrenoceptor blocker: racemic mixture, one isomer is a nonselective β blocker and the other is an α1 blocker. Used in HTN, prolongs survival in HF. Tox: cardiovascular depression, asthma. Labetalol is similar. (10, 11, 13)

Question 32

Caspofungin

Answer 32

Antifungal: echinocandin prototype, inhibitor of β (1-3)-glucan synthesis, a cell wall component. Used IV for disseminated Candida and Aspergillus infections. Tox: GI effects, flushing. Increases cyclosporine levels (avoid combination). (48)