USMLE drugs Flashcards

Dopamine receptor
Terms Definitions
Antineoplastic, immunosuppressant: cell cycle-specific drug that inhibits dihydrofolate reductase. Major dose reduction required in renal impairment. Tox: GI distress, myelosuppression, crystalluria. Leucovorin rescue used to reduce toxicity.
Antihypertensive: arteriolar vasodilator, orally active; used in severe HTN, CHF. Minoxidil, a similar but more powerful antihypertensive, is also used topically in baldness. Tox: tachycardia, salt and water retention, lupus-like syndrome (hydralazine).
Acetylcholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma, atropine poisoning. Tox: convulsions, excess cholinomimetic effects. Others: neostigmine and pyridostigmine; DFP and echothiophate are organophosphates used rarely.
Platinum-containing alkylating anticancer drug. Used for solid tumors (eg, testes, lung). Tox: Neurotoxic and nephrotoxic. Carboplatin is similar.
Penicillinase-resistant penicillin: used for suspected or known staphylococcal infections; not active against MRSA. Tox: penicillin allergy. Others in group include methicillin (the prototype, rarely used), oxacillin, cloxacillin, and dicloxacillin.
K+ Sparing Diuretics
inhibits VLDL synthesis
erythropoietin side effect
essentially an NSAID
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 (postantibiotic effect) and less toxic. Amikacin and tobramycin are similar.
Prototype carbapenem antibiotic: active against many aerobic and anaerobic bacteria; bactericidal inhibitor of cell wall synthesis. Used with cilastatin. Tox: allergy (partial cross- reactivity with penicillins), seizures. Meropenem and ertapenem are similar but do not require cilastatin and are less likely to cause seizures.
Tetracycline antibiotic: protein synthesis inhibitor (30S), more effective than other tetracyclines against chlamydia and in Lyme disease. Unlike other tetracyclines, it is eliminated mainly in the feces. Tox: see tetracycline.
Antibiotic: broad-spectrum agent; inhibits protein synthesis (50S); uses restricted to backup drug for bacterial meningitis, infections due to anaerobes, Salmonella. Tox: reversible myelosuppression, aplastic anemia, gray baby syndrome.
Bisphosphonate; stabilizes bone structure and increases bone mineral density. Used in postmenopausal and steroid-induced osteoporosis. Tox: esophageal ulceration. Other bisphosphonates (eg, etidronate, pamidronate) are used in Paget's disease.
Centrally acting antimuscarinic prototype for parkinsonism. Tox: excess antimuscarinic effects.
Adrenoceptor agonist prototype: product of adrenal medulla, some CNS neurons. Affinity for all a and all b receptors. Used in asthma; as hemostatic and as adjunct with local anesthetics; drug of choice in anaphylaxis. Tox: tachycardia, hypertension, MI, pulmonary edema and hemorrhage.
Macrolide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); activity includes gram-positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis. Tox: cholestatic jaundice (avoid estolate in pregnancy), inhibits liver drug-metabolizing enzymes. Other macrolide antibiotics include azithromycin and clarithromycin.
Antineoplastic: anthracycline drug (cell cycle-nonspecific); intercalates between base pairs to disrupt DNA functions, inhibits topoisomerases, and forms cytotoxic free radicals. Tox: cardiotoxicity, myelosuppression. Daunorubicin is similar.
Antihypertensive: prodrug of methylnorepinephrine, a CNS- active a2 agonist. Reduces SANS outflow from vasomotor center. Tox: sedation, positive Coombs test, hemolysis.
Nondepolarizing neuromuscular blocking agent prototype: competitive nicotinic blocker. Releases histamine and may cause hypotension. Analogs: pancuronium, atracurium, vecuronium, and other "-curiums" and "-oniums." Tox: respiratory paralysis. Antidote: cholinesterase inhibitor, eg, neostigmine.
Aldosterone receptor antagonist: K+-sparing diuretic action in the collecting tubules; used in aldosteronism, HTN, and female hirsutism (androgen receptor blocking action). Tox: hyperkalemia, gynecomastia. Eplerenone, used in HTN and HF, is a more selective aldo¬sterone antagonist.
Cholinesterase inhibitor: prototype synthetic quaternary nitrogen carbamate with little CNS effect. Tox: excess cholinomimetic effects. Pyridostigmine is similar.
what's prazosin?
alpha 1 antagonist.
antitumor antibotics, inhibits topoisomerase II
Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors; fewer EPS adverse effects than other antipsychotic drugs. Tox: ANS effects, agranulocytosis (infrequent but significant).
Blocks platelet ADP receptors irreversibly and inhibits platelet aggregation. Used in transient ischemic attacks and to prevent strokes and restenosis after placement of coronary stents. Tox: bleeding, neutropenia. Ticlopidine similar, but higher risk of neutropenia and thrombotic thrombocytopenic purpura (TTP).
Selective estrogen receptor modulator (SERM): agonist at bone receptors (used in osteoporosis), antagonist at breast receptors (used in cancer) but does not stimulate endometrial receptors.
Macrolide antibiotic: similar to erythromycin but greater activity against H influenzaenfluenzae,, chlamydiae, and streptococci; long half-life because of tissue accumulation; renal elimination. Tox: GI distress but no inhibition of drug metabolism. Clarithromyin is similar but has a shorter half-life, inhibits drug metabolism, and is contraindicated in pregnancy.
Phenothiazine antipsychotic : blocks D2 dopamine receptors. Tox: atropine-like, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation, seizures (in OD), additive effects with other CNS depressants. Other phenothiazines: fluphenazine and trifluoperazine (antipsychotics), prochlorperazine (antiemetic), promethazine (preoperative sedation)
Anxiolytic: partial agonist that interacts with 5-HT1A receptors; slow onset (1-2 weeks). Minimal potentiation of CNS depressants, including ethanol; negligible abuse liability.
Dopamine receptor agonist: nonergot used in Parkinson's disease; more receptor selectivity and less toxicity than bromocriptine. Tox: dyskinesias, sedation. Pramipexole is similar.
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).
DMARD: decreases leukocyte chemotaxis, stabilizes lysosomes, and traps free radicals. Tox: GI distress, ototoxicity, myopathy, neuropathy. Other older DMARDs: methotrexate, prednisone, sulfasalazine, gold salts, penicillamine.
Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism). Tox: dyskinesias, hypotension, on-off phenomena, behavioral changes.
Opioid analgesic: synthetic mu agonist, equivalent to morphine in efficacy but orally bioavailable and with a longer half-life. Used as analgesic, to suppress withdrawal symptoms, and in maintenance programs. Tox: see morphine.
Adrenoceptor agonist prototype: acts at b1- and all a adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN.
Class IA antiarrhythmic drug prototype: short half-life, metabolized by N-acetyltransferase. Similar to quinidine but more cardiodepressant and may cause a lupus-like syndrome.
Fibrate antilipemic: activates PPAR-a nuclear receptors; lowers serum triglycerides via stimulation of lipoprotein lipase activity. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia. Tox: GI distress, cholelithiasis, skin rashes, increased risk of myopathy when combined with statins or niacin.
Antiviral: effective against herpes viruses (cytomegalocirus [CMV] and herpes simplex virus [HSV]); for CMV requires bioactivation via viral phosphotransferase. Tox: myelosuppression, nephrotoxicity, neurotoxicity.
Class IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff-Parkinson- White syndrome. Tox: arrhythmogenic, CNS excitation.
K+-sparing diuretic: blocks Na+ channels in cortical collecting tubules.Tox: hyperkalemia.
GI disturbances, incl ulcers/bleeding,Renal tox,Aplastic anemia
Reversibly inhibit cyclooxygenase (COX-1 and COX-2)
Vinca alkaloid, inhibit microtubule formation, causes neurotoxicity
What's pramipexole?
it stimulates dopamine receptor
Antiviral: HIV protease inhibitor (PI) used as a component of combination regimens in AIDS. Tox: anemia, nephrolithiasis, metabolic disorders, inhibits P450 drug metabolism. Other PIs: amprenavir, nelfinavir, ritonavir (major P450 inhibitor), and saquinavir.
Toxin: potent sodium channel blocker; blocks action potential propagation in nerve, heart, and skeletal muscle. From puffer fish, California newt. Tox: paresthesias, paralysis. Saxitoxin (paralytic shellfish poison) is similar.
Opioid analgesic prototype: strong mu receptor agonist. Poor oral bioavailability. Tox: constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychological and physiologic dependence. Additive effects with other CNS depressants.
Nitric oxide
Endogenous vasodilator released from vascular endothelium; neurotransmitter. Mediates vasodilating effect of acetylcholine, histamine, and hydralazine. Active metabolite of nitroprusside and of nitrates used in angina. Used as pulmonary dilator in neonatal hypoxia. Tox: excessive vasodilation, hypotension
Thiazide diuretic prototype: acts in distal convoluted tubule to block Na+/Cl_ transporter; used in HTN, CHF, nephrolithiasis. Tox: a sulfonamide; increased serum lipids, uric acid, glucose; K+ wasting.
Monoclonal antibody to the platelet glycoprotein IIb/IIIa receptor that binds fibrin. Used to prevent clotting after coronary angioplasty and in acute coronary syndrome. Eptifibatide and tirofiban act similarly
Cytokines, recombinant
DNA technology products: aldesleukin (IL-2, used in renal cancer); erythropoietin (epoetin alfa, used in anemias); filgrastim (G-CSF, used in neutropenia); interferon-a (used in hepatitis B and C and in cancer), interferon-b (used in multiple sclerosis); oprelvekin (IL-11, used in thrombocytopenia); and sargramostim (GM-CSF, used in neutropenia).
Prototype aromatase inhibitor used in estrogen-dependent cancers (eg, breast cancer). Letrozole is similar.
Adverse SE's of Spironolactone
hyperkalemia, hyponatremia, gynecomastia
Chelates copper and other heavy metals, removing excess; combines with cystine, resulting in more soluable compound for excretio, preventing cystine calculi.Also has anti-rheumatic mech of unknown action
diabetes druginitially incr beta cell insulin secretionalso decr reate of hepatic glucose production, incr insulin receptor sensitivity, and incr # of insulin receptors
what's mefloquine used for?
prophylaxis for malaria
anti-fungal, not absorbed from GI, binds to ergosterol and is the drug of choice for oropharygeal candidiasis in immuno-compromised pts
what's terazosin?
it's an alpha 1 blocker
diabetes drug that decreases insulin resistance
GnRH analog, decreases LH and FSH
Antimanic prototype: a primary drug in mania and bipolar affective disorders; blocks recycling of the phosphatidylinositol second messenger system. Tox: tremor, diabetes insipidus, goiter, seizures (in overdose), teratogenic potential (Ebstein's malformations).
5-HT1D receptor agonist: used to abort migraine attacks. Tox: coronary vasospasm, chest pain, or pressure. Other "triptans": naratriptan, rizatriptan, zolmitriptan.
Ethinyl estradiol
Synthetic estrogen: used in many hormonal contraceptives; mestranol is similar
Guanethidine MoA
Enters peripheral nerves via NE reuptake mechanism and blocks the release of NE storage vesicles
antihistamine with anti 5HT activity. used to treat serotonine syndrome
what is acetylcysteine?
breaks disulfide bonds, decreasing musus viscosity; replenishes glutathione.
atropine and side effects
muscarinic antagonistSide effects:hot as a haredry as a bonered as a beetblind as a batmad as a hatterbloated as a toad
what is pentazocine?
it's a partial opioid agonist
Amphotericin B
Antifungal: polyene drug of choice for some systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability. Tox: chills and fever, hypotension, nephrotoxicity (dose limiting; less with liposomal forms).
used to relieve the pain of peripheral neuropathy. Binds to neuronal transient potential vanilloid receptor 1, depletes substance P, decreases substance P
What's special about fenoldopam?
Used for treating malignant hypertension. Dopamine D1 receptor agonist-relaxes renal vascular smooth muscle.
How dose LSD work?
partial agonist at serotonin receptor
what's the mech of colchicine?
blocking tubulin polymerization and thus disrupt chemotaxis and phagocytosis
what do you need to watch out for when prescribing TNF-alpha inhibitor
what drug do you give to pt who has peptic ulcer who wants to cont to take NSAID?
What is ursodeoxycholic acid?
its used for decrease concentration of bile acids
What is cilostazol?
a PDE inhibitor used in Pt w/ intermittent claudication. In addition to inhibition of platelet aggregation, cilostazol is also a direct arterial vasodilator.
what the life threatening side effect of clozapine?
agranulocytosis, decr WBC, requires weekly WBC monitoring
what do you need to monitor if you are treating your DM pt with thiazolidinediones?
liver funtions
what drug do you use to control carcinoid syndromes?
octreotide (synthetic somatostatin analog)
Does raloxifene cause endometrial carcinoma?
no, because it is an endometrial antagonist
Can we use non-selective beta blockers for DM? will mask the adrenergic symptoms. Use beta 1 blocker if you have to
what do adenosine and Ach do to the heart?
redce the rate of spontaneous depolarization in cardiac pacemaker cells
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