Pharm Flashcards
Abciximab
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)
Acetaminophen
Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti-inflammatory. Less GI distress than aspirin but dangerous in overdose. Tox: hepatic necrosis. Antidote: acetylcysteine. (36)
Acetazolamide
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)
Acetylcholine
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)
Acyclovir
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)
Adenosine
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)
Albuterol
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)
Alendronate
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)
Allopurinol
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)
Alteplase (t-Pa)
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)
Amiloride
K+-sparing diuretic: blocks epithelial Na+ channels in cortical collecting tubules. Tox: hyperkalemia. (15)
Amiodarone
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)
Amphetamine
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)
Amphotericin B
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)
Ampicillin
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)
Anastrozole
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)
Aspirin
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)
Atenolol
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)
Atropine
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)
Azithromycin
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)
Baclofen
GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord. (27)
Benztropine
Muscarinic cholinoceptor blocker: centrally acting antimuscarinic prototype for parkinsonism. Tox: excess antimuscarinic effects. (8, 28)
Botulinum
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)
Bromocriptine
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)
Bupivacaine
Long-acting amide local anesthetic prototype. Tox: greater cardiovascular toxicity than most local anesthetics. (26)
Buprenorphine
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)
Bupropion
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)
Calcitonin
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)
Captopril
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)
Carbamazepine
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)
Carvedilol
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)
Caspofungin
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)
