Doxazosin
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Doxazosin
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| Systematic (IUPAC) name | |
| [4-(4-amino-6,7-dimethoxy- quinazolin-2-yl) piperazin-1-yl]- (2,5-dioxabicyclo[4.4.0] deca-6,8,10-trien-4-yl) methanone | |
| Identifiers | |
| CAS number | |
| ATC code | C02 |
| PubChem | |
| DrugBank | |
| 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.
[edit] 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].
[edit] External links
- Information about Cardura from rxlist.com
- [1] BMJ article about Cardura.
- Article about Cardura
- Cardura XL product website, run by Pfizer
[edit] 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:. PMID 12459039.
- ^ Marketing: Spin doctors soft pedal data on antihypertensives. BMJ (2003-01-18). Retrieved on 2008-05-26.
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