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PCol I - Exam 3

individual drugs

QuestionAnswer
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
Created by: Krafty