The chemistry, pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of alfuzosin hydrochloride in the treatment of benign prostatic hyperplasia (BPH) are discussed. Alfuzosin is a functionally uroselective alpha 1-adrenergic antagonist indicated for the management of moderate to severe BPH. It can improve urinary voiding symptoms and increase urinary flow rates while causing few cardiovascular adverse effects. When administered as an immediate-release (IR) formulation, alfuzosin must be administered twice or thrice daily. The extended-release (ER) formulations of alfuzosin for once- or twice-daily administration are associated with small variations in peak and trough serum drug levels, which may contribute to the lower frequency of cardiovascular adverse effects reported with ER versus IR alfuzosin. Alfuzosin has been shown to improve patients' perception of quality of life, allowing patients to increase their physical activities and improve their ability to handle day-to-day activities. Less significant improvements in patients' sense of well-being and improved sexual functioning have been reported. The usual dose of alfuzosin for patients with BPH is 2.5 mg twice or thrice daily of the IR formulation or 5 mg of ER alfuzosin twice daily or 10 mg of ER alfuzosin once daily. The Food and Drug Administration is currently reviewing the ER 10-mg formulation for once-daily administration. IR alfuzosin is similar to all other second-generation alpha 1-adrenergic antagonists in mechanism of action, clinical efficacy, and adverse effects. No dosage titration is needed for ER alfuzosin, and its onset of peak action is within days of the start of treatment.