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20-September-2008 09:55:48 - Hydralazine Hydralazine Systematic IUPAC name 1-hydrazinophthalazine Identifiers CAS number 86-54-4 ATC code C02DB02 PubChem 3637 Chemical data Formula C8H8N4 Mol. mass 160.176 g/mol Pharmacokinetic data Bioavailability ? Metabolism Hepatic Half life 2-4 hours Excretion Renal Therapeutic considerations Pregnancy cat. ? Legal status Routes Oral, intravenous Hydralazine hydrochloride 1-hydrazinophthalazine monohydrochloride; Apresoline is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles. By relaxing vascular smooth muscle, vasodilators act to decrease peripheral resistance, thereby lowering blood pressure.1 Contents 1 Mechanism 2 Clinical Use 3 Side effects 4 References Mechanism The mechanism of action of hydralazine is not well known. It interferes with the action the second messenger inositol triphosphate, limiting calcium release from the sarcoplasmic reticulum of smooth muscle. This results in an arterial and arteriolar relaxation.2 An exam revision source declares that hydralazine works through a cGMP-mediated mechanism, resulting in smooth muscle relaxation.3 Clinical Use Hydralazine is not used as a primary drug for treating hypertension because it elicits a reflex sympathetic stimulation of the heart the baroreceptor reflex. The sympathetic stimulation may increase heart rate and cardiac output, and may cause angina pectoris or myocardial infarction.1 Hydralazine may also increase plasma renin concentration, resulting in fluid retention. In order to prevent these undesirable side effects, hydralazine is generally prescribed in combination with a beta-blocker e.g., propranolol and a diuretic.1 Hydralazine is used to treat severe hypertension, but again, it is not a first line therapy for essential hypertension. However, hydralazine is the first line therapy for hypertension in pregnancy, with methyldopa.3 Side effects Common side effects include: Diarrhea Compensatory tachycardia due to baroreceptor reflex Headache Loss of appetite Nausea or vomiting Pounding heartbeat Drug-Induced Lupus Erythematosus Patients given hydralazine over a peroid of six months may develop a lupus-like syndrome or other immune related diseases that generally are reversible with withdrawal.1 Hydralazine is differentially acetylated by fast and slow acetylator phenotypes thus incidence of lupus-like disease in slow acetylators. References ^ a b c d Harvey, Richard A., Pamela A. Harvey, and Mark J. Mycek. Lippincott's Illustrated Reviews: Pharmacology. 2nd ed. Philadelphia: Lipincott, Williams Wilkins, 2000. 190. ^ Rang, Dale, Ritter and Flower. Pharmacology. 6th Ed, 2007. ^ a b Bhushan, Vikas, Tao T. Lee, and Ali Ozturk. First Aid for the USMLE Step 1. New York: McGraw-Hill Medical, 2007. 251. v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Hydralazine Categories: Antihypertensive agents | Hydrazines | Pyridazines Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Hrvatski Italiano 日本語 Polski This page was last modified on 15 August 2008, at 19:41
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