Alfuzosin: Overview of pharmacokinetics, safety, and efficacy of a clinically uroselective α-blocker

Efficacy and safety of alfuzosin administered as 3-times-daily and 2-times-daily formulations have been previously demonstrated in placebo-controlled studies, and these formulations have been commercially available in many countries. A once-daily formulation of alfuzosin administered through a novel prolonged-release system has been recently developed to improve the convenience of dosing and to provide optimal pharmacokinetic coverage over 24 hours. The results of 2 double-blind, placebo-controlled phase 3 studies in patients with lower urinary tract symptoms associated with benign prostatic hyperplasia suggests that 10 mg of alfuzosin administered once daily without dose titration is superior to placebo in terms of symptom and urinary flow rate improvement. Orthostatic hypotension and first-dose phenomenon related to the α-blocking property were rare. The incidences of asthenia and fatigue were comparable to those seen with placebo. Ejaculatory disorders were very rare. The most frequently reported adverse event potentially related to α blockade was dizziness, which occurred in 5.0% of patients treated with 10 mg alfuzosin compared with 2.1% of patients given placebo.