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PCol I - Exam 3
Antihypertensives
Question | Answer |
---|---|
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 |