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Antihypertensives

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