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