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PCol I - Exam 3

Antihypertensives

QuestionAnswer
1st line therapy for Stage 1 HTN if no compelling indications thiazide-type diuretic, OR ACEI, ARB, BB, CCB or combination
1st line therapy for Stage 2 HTN if no compelling indications thiazide-type diuretic AND ACEI, ARB, BB or CCB
1st line therapy for HTN with compelling indications diuretic, ACEI, ARB, BB, or CCB
two major types of centrally acting sympatholytics (sympatho-inhibitory) Alpha2 receptor agonists; I1 (imidazoline) receptor agonists
eight types of peripherally acting sympatholytics (Vasodilators and RAAS Inhibitors) Adrenergic Neuron Blockers, Alpha1 Receptor Blocker, Beta Receptor Blockers, Calcium Channel Blockers, Vasodilators, Angiotensin Converting Enzyme Inhibitors, Angiotensin Receptor Blockers, Renin Inhibitors
alpha-2 blockers (4) - centrally acting sympatholytics Clonidine, Guanabenz, Guanfacine,Methyldopa
imidazoline receptor agonists (2) Moxonidine, Relminidine
only one of the four alpha-2 blockers that is a prodrug methyldopa - it must first be metabolized to alpha-methylnorepinephrine as shown below
Adrenergic Neuron Blocking Drugs (3) - peripherally acting sympatholytics Reserpine, Guanethidine, Guanadrel
this adrenergic neuron blocking agent is long-acting and irreversible reserpine
usually daily dose of reserpine 0.25 mg PO
this adrenergic neuron blocking agent causes receptor supersensitivity Guanethidine
alpha-1 receptor blockers (3) - peripherally acting sympatholytics Prazosin, Terazosin, Doxazosin
these alpha-1 receptor blockers may cause "first-dose effect" consisting of hypotension and possibly syncope Prazosin, Terazosin
selective B1 blockers without intrinsic activity Atenolol, Betaxolol, Bisoprolol, Metoprolol
selective B1 blockers with intrinsic activity (ISA) Acebutolol, Carteolol
non-selective beta-blockers without intrinsic activity Nadolol, Propranolol, Timolol
non-selective beta-blockers with intrinsic activity Penbutolol
alpha-1/beta-1 blocker Carvedilol
alpha-1/beta-1/beta-2 blocker Labetalol
beta-1 blocker/beta-2 agonist (not approved in US) Nebivolol
beta-1 selective agonists dobutamine, prenalterol
beta-2 selective agonists ritodrine, terbutaline
calcium channel blockers approved for HTN Amlodipine, Diltiazem (SR & ER only), Felodipine, Isradipine, Nicardipine, Nicardipine SR, Nicardipine IV (short term, Nifedipine ER, Nisoldipine, Verapamil, Verapamil SR & ER, Clevidipine IV infusion (approved for hypertensive emergency)
Vasodilators Hydralazine, Nitroprusside, Organonitrates, Minoxidil, Diazoxide, Fenoldopam
Angiotensin Converting Enzyme Inhibitors Captopril, Fosinopril, Enalapril, Quinapril, Ramipril, Lisinopril, Moexipril, Trandolapril, Benazepril, Perindopril
Angiotensin II (AT1) Receptor Antagonists Losartan, Valsartan, Candesartan, Irbesartan, Telmisartan, Eprosartan, Olmesartan
daily dosing for prazosin multiple daily dosing required (half-life of 3-4 hours due to first pass metabolism)
daily dosing for terazosin 5 to 20 mg once daily
daily dosing for doxazosin 1 mg once daily (lowest dose with once daily dosing duration of action)
nebivolol's additional mechanism of actin beta-2 agonism in renal artery and glomerulus results in NO formation and dilation
IV infusion approved for hypertensive emergencies (CCB) Clevidipine
Created by: Krafty
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