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Active ingredient: Alfuzosin - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antihypertensive Agents

Dosage Forms

  • Tablet (extended-release)

Brands / Synonyms

Uroxatral; Xatral

Indications

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.

Absorption

Absorption is 50% lower under fasting conditions

Toxicity

side effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, and fatigue.

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Alfuzosin should not be used in patients with moderate or severe hepatic insufficiency, (Childs-Pugh categories B and C) since alfuzosin blood levels are increased in these patients. Alfuzosin should not be co-administered with potent CYP3A4 inhibitors such as ketoconazole, itraconazole, and ritonavir, since alfuzosin blood levels are increased. Alfuzosin is contraindicated in patients known to be hypersensitive to alfuzosin hydrochloride or any component of Alfuzosin tablets.

Drug Interactions

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.

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