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PCol I - Exam 3
individual drugs
| Question | Answer |
|---|---|
| clonidine | alpha 2 agonist (CAS; anti-HTN) |
| guanabenz | alpha 2 agonist (CAS; anti-HTN) |
| guanfacine | alpha 2 agonist (CAS; anti-HTN) |
| methyldopa | alpha 2 agonist (CAS; anti-HTN) - prodrug |
| reserpine | adrenergic neuron blocking agent (anti-HTN) |
| guanethidine | adrenergic neuron blocking agent (anti-HTN) |
| guanadrel | adrenergic neuron blocking agent (anti-HTN) |
| prazosin | alpha-1 receptor blockers (anti-HTN; angina - mixed venous/arteriolar dilator) |
| terazosin | alpha-1 receptor blockers (anti-HTN) |
| doxazosin | alpha-1 receptor blockers (anti-HTN) |
| phentolamine | non-selective alpha blocker; early agent (anti-HTN) |
| atenolol | beta-1 selective blocker, no ISA (anti-HTN; angina) |
| betaxolol | beta-1 selective blocker, no ISA (anti-HTN) |
| bisoprolol | beta-1 selective blocker, no ISA (anti-HTN); selectivity lost above doses of 20 mg |
| metoprolol | beta-1 selective blocker, no ISA (anti-HTN) |
| acebutolol | beta-1 selective blocker, ISA+ (anti-HTN) |
| carteolol | beta-1 selective blocker, ISA+ (anti-HTN) |
| nadolol | non-selective beta blocker (B1/B2), no ISA (anti-HTN), not readily metabolized (once daily dosing), no significant CNS penetration |
| propranolol | non-selective beta blocker (B1/B2), no ISA (anti-HTN) |
| timolol | non-selective beta blocker (B1/B2), no ISA (anti-HTN), lacks local anesthetic action |
| penbutolol | non-selective beta blocker (B1/B2), ISA+ (anti-HTN) |
| pindolol | non-selective beta blocker (B1/B2), ISA+, MSA+ (antiarrhythmic effects) (anti-HTN) |
| carvedilol | alpha-blocker/beta-blocker, no ISA (anti-HTN; angina); S-isomer = nonselective BB; R-isomer = alpha blockade; may have eNOS effects via B2 |
| labetalol | non-selective beta blocker (alpha/B1/B2), no ISA (anti-HTN); best BB for pheochromocytoma |
| nebivolol | beta-1 blocker, beta-2 agonist (B2 activity stimulates eNOS), (anti-HTN); dual MOA, most selective BB available, once daily dosing |
| amlodipine | calcium channel blocker (anti-HTN; approved for angina) |
| diltiazem (SR & ER only) | calcium channel blocker (anti-HTN; approved for angina); has significant nonspecific sympathetic antagonism |
| felodipine | calcium channel blocker (anti-HTN) |
| isradipine | calcium channel blocker (anti-HTN); HTN is only approved use |
| nicardipine, nicardipine SR and IV | calcium channel blocker (anti-HTN; approved for angina) |
| clevidipine IV | calcium channel blocker (anti-HTN) - hypertensive crisis; only reduces systemic vascular resistance (no effect on preload), onset 2-4 min, offset 5-15 min |
| nifedipine ER | calcium channel blocker (anti-HTN; approved for angina); greater selectivity for smooth muscle than cardiac calcium channels (leads to reflex tachycardia) |
| nisoldipine | calcium channel blocker (anti-HTN) |
| verapamil, SR, ER | calcium channel blocker (anti-HTN; approved for angina); has cardiac depressant effect so less reflex tachycardia |
| hyrdalazine | vasodilator, causes synthesis of NO from endogenous sources (anti-HTN; angina - arteriolar dilator) |
| nitroprusside | vasodilator, inorganic nitrate, causes direct release of NO --> disintegrates (anti-HTN); sodium nitroprusside for emergency/ST only --> creates cyanide as a by product |
| nitroglycerin | vasodilator, organic nitrate, causes direct release of NO but required cysteine (anti-HTN; angina - venous dilator); when you reach headache as side effect that's how you know the dose is working |
| minoxidil | vasodilator, potassium channel (K-channel) opener (anti-HTN; angina - arteriolar dilator); differences in acetylation; doses higher than 200 mg associated w/lupus-like syndrome |
| diazoxide | vasodilator, potassium channel (K-channel) opener (anti-HTN); parenterally admin for hypertensive emergency --> combine w/BB to prevent reflex tachycardia; mini-bolus |
| fenoldopam | vasodilator, DA agonist (D1 selective), (anti-HTN; angina) |
| captopril | ACE Inhibitor, first nonpeptide ACEI, bone marrow depression, only one with a sulfhydryl group (anti-HTN) |
| enalapril | ACE Inhibitor, prodrug,(anti-HTN) |
| lisinopril | ACE Inhibitor, lysine derivative of enalaprilat(anti-HTN) |
| benazepril | ACE Inhibitor, prodrug, excreted mainly by kidney,(anti-HTN) |
| ramipril | ACE Inhibitor, prodrug, excreted mainly by kidney,(anti-HTN) |
| fosinopril | ACE Inhibitor, prodrug, metabolized by liver or kidney --> no dose adjustment in impaired renal function(anti-HTN) |
| losartan | angiotensin II receptor (AT1) blocker, metabolized to active metabolite that is 10-40x more active, 1000x greater affinity for AT1, fairly clean drug,(anti-HTN) |
| valsartan | angiotensin II receptor (AT1) blocker, orally effective, 20,000x more selective for AT1, primary metabolite is inactive, (anti-HTN) |
| telmisartan | angiotensin II receptor (AT1) blocker, (anti-HTN) |
| eprosartan | angiotensin II receptor (AT1) blocker, (anti-HTN) |
| candesartan | angiotensin II receptor (AT1) blocker, (anti-HTN) |
| olmesartan | angiotensin II receptor (AT1) blocker, (anti-HTN) |
| irbesartan | angiotensin II receptor (AT1) blocker, (anti-HTN) |
| aliskiren | renin inhibitor (anti-HTN), fits binding pocket for angiotensinogen on renin; reduces plasma renin activity even though plasma renin concentration is increased; especially good when combined with HCT > ramipril > irbesartan |
| renalase | endogenous enzyme that metabolizes circulating monoamines (DA, Epi, NE), not inhibited by MAOIs, short-acting experimental injection (anti-HTN) |
| chlorothiazide | diuril; thiazide diuretic (HTN, HF, edema, hypercalciuria, NDI) |
| hydrochlorothiazide | hydrodiuril; thiazide diuretic (HTN, HF, edema, hypercalciuria, NDI); 10x more potent than chlorothiazide |
| chlorothalidone | hygroton; thiazide-like diuretic (HTN, HF, edema, hypercalciuria, NDI) |
| indapamide | lozol; thiazide diuretic (HTN, HF, edema, hypercalciuria, NDI) |
| metolazone | thiazide-like diuretic (HTN, HF, edema, hypercalciuria, NDI); combine w/loop diuretic to treat severe resistant oedema |
| furosemide | lasix; loop diuretic (HTN, hypercalcemia, edema); sulfa cross-rxn |
| bumetanide | bumex; loop diuretic (HTN, hypercalcemia, edema); sulfa cross-rxn |
| torsemide | demadex; loop diuretic (HTN, hypercalcemia, edema); sulfa cross-rxn |
| ethacrynic acid | edecrin; loop diuretic (HTN, hypercalcemia, edema); only one w/o sulfa cross-rxn (phenoxyacetic acid derivative) |
| spironolactone | aldactone; potassium-sparring diuretic; steroid-like/aldosterone receptor blocker; (prevent K loss in ptns on loop/thiazide, HF, hyperaldosteronism, refractory edema); combine w/HCTZ = aldactazide |
| eplerenone | inspra; potassium-sparring diuretic; steroid-like/aldosterone receptor blocker; (prevent K loss in ptns on loop/thiazide, HF, hyperaldosteronism, refractory edema) |
| triamterene | dyrenium; combine w/HCTZ for dyazide/maxide; sodium channel blocker; potassium-sparring diuretic; (prevent K loss in ptns on loop/thiazide, HF, hyperaldosteronism, refractory edema); |
| amiloride | midamor, combine w/HCTZ = moduretic; sodium channel blocker; potassium-sparring diuretic; (prevent K loss in ptns on loop/thiazide, HF, hyperaldosteronism, refractory edema) |
| mannitol USP | osmitrol; osmotic diuretic (trauma, CV operations, hemolytic rxn, toxic poisoning, acute cerebral edema, ophthalmic surgery) |
| urea | ureaphil; osmotic diuretic (trauma, CV operations, hemolytic rxn, toxic poisoning, acute cerebral edema, ophthalmic surgery) |
| sucrose | osmotic diuretic (trauma, CV operations, hemolytic rxn, toxic poisoning, acute cerebral edema, ophthalmic surgery) |
| glycerol | osmotic diuretic (trauma, CV operations, hemolytic rxn, toxic poisoning, acute cerebral edema, ophthalmic surgery) |
| acetazolamide | diamox; carbonic anhydrase inhibitor; (alkalinize urine, glaucoma, epilepsy) |
| dichlorophenamide | daranide; carbonic anhydrase inhibitor; (alkalinize urine, glaucoma, epilepsy) |
| digoxin | cardiac glycoside (angina), high Vd (less bound to plasma proteins), serum conc 0.5 - 2.0ng/ml; half-life is 36 hours; elimination is renal |
| digitoxin | cardiac glycoside (angina), highly protein bound, serum conc 10 - 35 ng/ml, half-life = 7 days; elimination = hepatic |
| isosorbide dinitrate | venous dilator (angina); reduces preload |
| amrinone | inodilator (angina); positive inotrope plus vasodilator |
| milrinone | inodilator (angina); positive inotrope plus vasodilator |
| natrecor | inotropic (angina); recombinant human b-type naturetic peptide |
| bidil | isosorbide dinitrate and hydralazine; inotropic (angina) |
| pimobendan | calcium-sensitizer and PDE3 inhibitor (angina) |
| levosimendan | calcium-sensitizer and ATP-dependent K channels (angina) |
| mibefradil | calcium-channel blocker (angina); removed from market due to prolonged QT intervals and arrhythmias (inhibits CYP3A and 2D6) |
| bepridil | calcium-channel blocker for angina; similar to diltizem but contraindicated in patients with cardiac arrhythmias (blocks Na/K channels, proarrhythmic) |
| ranolazine | angina; MOA unclear; inhibits CYP3A and 2D6; can prolong QT interval, lots of interactions |