Prostatic alpha 1-adrenoceptors and uroselectivity

alpha 1-adrenoceptor antagonists (blockers) are now commonly used in the treatment of the symptoms of lower urinary tract obstruction. Originally phenoxybenzamine, a non-selective antagonist at both alpha 1- and alpha 2-adrenoceptors, was used by Marco Caine. In an attempt to minimize side effects, selective alpha 1-antagonists, e.g. prazosin, were subsequently developed. More recently, agents such as alfuzosin, doxazosin, terazosin, and tamsulosin have been introduced and claims of "uroselectivity" and "prostate" selectivity have emerged.

This review attempts to put these claims into perspective and represents a comprehensive analysis of all pre-clinical and clinical data including several papers from the Japanese literature. An attempt is made to define what is meant by selectivity at various levels including the test tube, in the laboratory animal and, most importantly, in the clinical context of the whole patient.

The conclusions are interpreted within the context of the subdivision of the alpha 1-adrenoceptor into alpha 1A, alpha 1B, and alpha 1D subtypes.