Doxazosin
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|---|---|
| Systematic (IUPAC) name | |
| (RS)-2-{4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine | |
| Clinical data | |
| Trade names | Cardura |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a693045 |
| Pregnancy cat. | ? |
| Legal status | ℞ Prescription only |
| Routes | oral |
| Pharmacokinetic data | |
| Bioavailability | 65% |
| Protein binding | 98% |
| Metabolism | Hepatic |
| Half-life | 22 hours |
| Identifiers | |
| CAS number | 74191-85-8 |
| ATC code | C02CA04 |
| PubChem | CID 3157 |
| DrugBank | APRD00474 |
| ChemSpider | 3045  |
| UNII | NW1291F1W8 |
| KEGG | D07874 |
| ChEBI | CHEBI:4708 |
| ChEMBL | CHEMBL707 |
| Chemical data | |
| Formula | C23H25N5O5 |
| Mol. mass | 451.475 g/mol |
| SMILES | eMolecules & PubChem |
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Doxazosin mesylate, a quinazoline compound sold by Pfizer under the brand names Cardura and Carduran, is an α1a-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
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 (released from sympathetic nerve terminals) to the alpha-1 receptors on the membrane of vascular smooth muscle cells. The primary effect of this inhibition 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, Dosin by Eipico and Doxazocine by Multi-Apex.
[edit] Efficacy
In March 2000, the ALLHAT study stopped its arm of the trial looking at alpha blockers, because doxazosin (Cardura) was less effective than a simple diuretic, and because 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 given new rise to a preference for Doxazosin as a BPH Drug, as it was found to treat erectile dysfunction (ED). The company’s own study did not yield as statistically significant results; however, Doxazosin does show promise for men with BPH and ED.[3]
[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:10.1186/1468-6708-3-10. PMC 149403. PMID 12459039. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=149403.
- ^ "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.
- ^ "Antihypertensive Drugs and Patients With Erectile Dysfunction". http://www.medscape.com/viewarticle/439675_3.
[edit] External links
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