Doxazosin

Doxazosin
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 YesY
UNII NW1291F1W8 YesY
KEGG D07874 YesY
ChEBI CHEBI:4708 YesY
ChEMBL CHEMBL707 YesY
Chemical data
Formula C23H25N5O5 
Mol. mass 451.475 g/mol
SMILES eMolecules & PubChem
 YesY(what is this?)  (verify)

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.

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]

References

External links