uroselective

Uroselective refers to pharmacologic agents that preferentially affect tissues of the urinary tract, such as the bladder neck and prostate, with comparatively reduced impact on systemic vascular tissues. In clinical practice, the term is most often used to describe certain alpha-1 adrenergic receptor antagonists that relieve lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH).

The concept rests on both receptor distribution and pharmacokinetics. In the lower urinary tract, alpha-1A receptors are more densely expressed than in most vascular tissues, while other subtypes (such as alpha-1B) are more common in blood vessels. Drugs with high alpha-1A selectivity, or those that concentrate in urinary tract tissues, tend to relax smooth muscle in the bladder neck and prostate with less orthostatic hypotension or vascular side effects. Some agents achieve uroselectivity primarily through receptor subtype preference; others rely on tissue distribution and pharmacokinetics.

Common uroselective drugs include tamsulosin, silodosin, and alfuzosin. Tamsulosin and silodosin have pronounced activity on alpha-1A receptors, producing relief of obstruction with a lower incidence of blood pressure lowering. Alfuzosin is considered uroselective in function, with a clinically favorable effect on urinary symptoms and a comparatively modest vascular impact. These agents are primarily used to treat LUTS due to BPH, improving urinary flow and reducing symptoms such as nocturia.

Limitations of uroselectivity include that no drug is perfectly selective; all can cause some vascular effects, especially at higher doses or with interacting medications. Side effects may include dizziness, orthostatic effects, or ejaculation disturbances. The term describes relative tissue selectivity rather than absolute specificity.