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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 |