Alfuzosin Hydrochloride for the Treatment of Benign Prostatic Hyperplasia

Mary Lee


Am J Health Syst Pharm. 2003;60(14) 

In This Article

Abstract and Introduction


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 α1-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 α1-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.


Benign prostatic hyperplasia (BPH) is the most common benign neoplasm in American men. Autopsy findings have shown that 80% of men who live to the age of 80 years have microscopic BPH.[1] Of these men, approximately 50% will develop urinary voiding symptoms or clinical BPH, and 50% of symptomatic patients will require treatment for the disease.[2,3] Symptomatic BPH can begin in men in their fourth decade of life. Treatments available include watchful waiting, α-adrenergic antagonists, finasteride, and surgery. Watchful waiting is indicated for patients with mild symptomatic BPH, surgery is indicated for patients with severe symptomatic BPH, and α-adrenergic antagonists and finasteride are used for moderate to severe symptomatic BPH. Choosing the correct treatment depends on the severity of BPH; concurrent medical conditions of the patient; preference of the patient for or against surgical intervention; and comparative efficacy, onset of action, adverse effects, and cost of therapy. For elderly patients, the treatment must not interfere with concurrent medical therapy to minimize drug interactions.

The focus of this review is alfuzosin hydrochloride, a functionally uroselective α1-adrenergic antagonist indicated for the management of symptomatic BPH. Other commercially available α-adrenergic antagonists in the United States include prazosin (Minipress, Pfizer), terazosin (Hytrin, Abbott Laboratories), doxazosin (Cardura, Pfizer), and tamsulosin (Flomax, Boehringer Ingelheim), all of which have been available for the same indication for some time. This review will compare alfuzosin with other α-adrenergic antagonists for BPH.


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