Prostate Selectivity of Alpha-Blockers: From Receptor Biology to Clinical Medicine

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Abstract
α-Adrenoceptor antagonists increase urinary flow and improve urinary symptoms in patients with benign prostatic hyperplasia (BPH). The rationale for the use of these agents in this indication is based on evidence that the contraction of prostatic smooth muscle is mediated via α(1)-adrenoceptors. The α(1)-adrenoceptor can be subdivided into at least three distinct subtypes - 1A, 1B, and 1D. Current opinion that the α-1A subtype mediates contraction of the prostatic smooth muscle has led to increased speculation that α-blockers selective for the α-1A subtype may offer the advantage of prostate selectivity in the clinic. This paper outlines the rationale for α-blockade in the treatment of BPH, focusing on the evidence for antagonist subtype selectivity and its potential clinical relevance.

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