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20-September-2008 09:55:48 - Doxazosin Doxazosin Systematic IUPAC name 4-4-amino-6,7-dimethoxy- quinazolin-2-yl piperazin-1-yl- 2,5-dioxabicyclo4.4.0 deca-6,8,10-trien-4-yl methanone Identifiers CAS number 74191-85-8 ATC code C02CA04 PubChem 3157 DrugBank APRD00474 Chemical data Formula C23H25N5O5 Mol. mass 451.475 g/mol Pharmacokinetic data Bioavailability 65% Protein binding 98% Metabolism Hepatic Half life 22 hours Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status ℞ Prescription only Routes oral Doxazosin mesylate, a quinazoline compound sold by Pfizer under the brand names Cardura and Carduran, is an alpha blocker used to treat high blood pressure and benign prostatic hyperplasia. On February 22, 2005, the US FDA approved a sustained release form of doxazosin, to be marketed as Cardura XL. It is an alpha-1 adrenergic receptor blocker which inhibits the binding of norepinephrine to alpha receptors in the autonomic nervous system. The primary effect of this blockage is relaxed vascular smooth muscle tone vasodilation, which decreases peripheral vascular resistance, leading to decreased blood pressure. Efficacy In March 2000, the ALLHAT study stopped the arm of its trial looking at alpha blockers because doxazosin Cardura was less effective than a simple diuretic. Patients on Cardura had a 25% higher rate of cardiovascular disease and twice the rate of congestive heart failure as patients on diuretics1. Pfizer, aware of the results before publication, launched a sophisticated damage control campaign in early 2000, and sales were largely unaffected despite the dangers highlighted by the study2. External links Information about Cardura from rxlist.com Cardura XL product website, run by Pfizer References ^ Piller LB, Davis BR, Cutler JA, et al November 2002. Validation of Heart Failure Events in the Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial ALLHAT Participants Assigned to Doxazosin and Chlorthalidone. Curr Control Trials Cardiovasc Med 3 1: 10. doi:10.1186/1468-6708-3-10. PMID 12459039. ^ Marketing: Spin doctors soft pedal data on antihypertensives. BMJ 2003-01-18. Retrieved on 2008-05-26. 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 v d e Urologicals G04 Acidifiers Ammonium chloride, Calcium chloride Urinary antispasmodics primarily antimuscarinics Darifenacin, Emepronium, Fesoterodine, Flavoxate, Imidafenacin, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium For erectile dysfunction Prostaglandins E Alprostadil PDE5 inhibitors Avanafil - Sildenafil - Tadalafil - Udenafil - Vardenafil Alpha blockers Moxisylyte - Phentolamine - Yohimbine Others Apomorphine - Papaverine Other urologicals Acetohydroxamic acid, Collagen, Dimethyl sulfoxide, Magnesium hydroxide, Pentosan polysulfate, Phenazopyridine, Phenyl salicylate, Succinimide For BPH 5α-reductase inhibitors Dutasteride, Finasteride Alpha blockers α1 Alfuzosin, Doxazosin, Silodosin, Tamsulosin, Terazosin Herbals Pygeum africanum, Serenoa repens v d e Adrenergic antagonists α α1 selective Doxazosin · Prazosin · Alfuzosin · Terazosin · Indoramin · Urapidil · Trimazosin · Moxisylyte · 1A Tamsulosin, Silodosin α2 selective Atipamezole · Efaroxan · Idazoxan · Yohimbine · Benzylpiperazine · Rauwolscine · Mirtazapine Non-selective α reversible Phentolamine · irreversible Phenoxybenzamine β β1 selective cardioselective Atenolol · Acebutolol · Celiprolol · Betaxolol · Bisoprolol · Esmolol · Metoprolol · Nebivolol β2 selective Butaxamine · ICI 118551 β3 selective SR 59230A Non-selective β Alprenolol · Amosulalol · Metipranolol · Nadolol · Oxprenolol · Penbutolol · Pindolol · Propranolol · Tertatolol · Timolol · Tilisolol · Sotalol Mixed α1/β Carvedilol · Labetalol · Arotinolol Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Doxazosin Categories: Alpha blockers | Quinazolines | Pharmacology stubs 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 Deutsch Hrvatski Magyar This page was last modified on 11 August 2008, at 12:30
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