Alfuzosin: profile and news

Recovery Of Abnormal Ejaculation By Intermittent Tamsulosin ... Feb 28, 2006
Tamsulosin is the first selective alpha-1A adrenoreceptor antagonist in contrast to the non-selective blockers alfuzosin, terazosin and doxazosin. ... - Medical News Today (press release),

Other information

Indication
For the treatment of the signs and symptoms of benign prostatic hyperplasia

Pharmacology
Alfuzosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Alfuzosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Alfuzosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Alfuzosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Alfuzosin results from a decrease in systemic vascular resistance and the parent compound Alfuzosin is primarily responsible for the antihypertensive activity.

Mechanism Of Action
Alfuzosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.

Drug Category
Antihypertensive Agents; Unclassified Therapeutic Agents (92:00.00); ATC:G04CA01

Brand Names/Synonyms
Uroxatral; Xatral

Dosage Forms
TABLET (EXTENDED-RELEASE)

Absorption
Absorption is 50% lower under fasting conditions

Interactions
Interactions for Alfuzosin: Drug-Drug Interactions: The pharmacokinetic and pharmacodynamic interactions between Alfuzosin and other alpha-blockers have not been determined. However, interactions may be expected, and Alfuzosin should NOT be used in combination with other alpha-blockers.

Chemical IUPAC Name
N-[3-[(4-amino-6,7-dimethoxy-quinazolin-2-yl)-methyl-amino]propyl]tetrahydrofuran-2-carboxamide

Chemical Formula
C19H27N5O4

Half Life
10 hours

Drug Type
Approved Drug

# Accession No
APRD00490

CAS Registry Number
81403-80-7