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1 : 1 mixture (racemate)
Systematic (IUPAC) name
(RS)-2-{4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine
Identifiers
CAS number 74191-85-8
ATC code C02CA04
PubChem 3157
DrugBank APRD00474
ChemSpider 3045
Chemical data
Formula C23H25N5O5 
Mol. mass 451.475 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 65%
Protein binding 98%
Metabolism Hepatic
Half life 22 hours
Therapeutic considerations
Pregnancy cat.  ?
Legal status Prescription only
Routes oral
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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 that 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.

In Egypt, tablet formulation sold as Duracin produced by Biopharm group for research and the drug industry.

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 diuretics[1]. 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 study[2].

Recent Studies have also showed efficacy in using Doxazosin as a preferred BPH Drug because it has been shown to increase erectile function, although the statistical significance has not been replicated in a study of its own. Doxazosin does show promise for men with BPH and ED. See article link below: http://www.medscape.com/viewarticle/439675_3

External links

References

  1. ^ 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. 
  2. ^ "Marketing: Spin doctors soft pedal data on antihypertensives". BMJ. 2003-01-18. http://www.bmj.com/cgi/content/full/326/7381/170/DC1. Retrieved 2008-05-26. 







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