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Nat Clin Pract Urol. 2007 Jul;4(7):368-78.

Pharmacology of alpha1-adrenoceptor antagonists in the lower urinary tract and central nervous system.

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  • 1Wake Forest Institute for Regenerative Medicine, Wake Forest University School of Medicine, Winston Salem, NC 27157, USA.


The main use of alpha(1)-adrenoceptor (AR) antagonists in urology has been to treat lower urinary tract symptoms (LUTS) in men with benign prostatic obstruction (BPO). The beneficial effects of these agents are primarily assumed to be because of relaxation of prostatic and urethral smooth muscle. The weak correlation between LUTS and prostatic enlargement, outflow obstruction, or both, however, has refocused interest on the role of extraprostatic alpha-ARs in the pathogenesis of LUTS and their treatment. The alpha(1)-ARs present in the bladder, urethra, vas deferens, peripheral ganglia, nerve terminals, and in the central nervous system could all potentially influence LUTS and, when the receptors are blocked, contribute to both the therapeutic and adverse effects of alpha(1)-AR antagonists. The relevance of alpha(1)-AR-subtype selectivity on the clinical usefulness of existing drug therapies has not been firmly established but it seems that blockade of both alpha(1A/L)- and alpha(1D)-ARs is necessary for the optimum balance between clinical efficacy and adverse effects.

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