Number №1, 2012 - page 36-40

Pharmacological profile of alpha-1 adrenergic receptors antagonist - silodosin

Martin C. Michel

Alpha-1 adrenergic receptors antagonists (alpha-blockers) are the most effective drugs for the treatment of patients with lower urinary tract symptoms (LUTS) caused by benign prostatic hyperplasia This article provides an overview of the pharmacological profile of a new alpha-1 adrenergic receptors antagonists - silodosin, especially - for the safety and portability profiles.
Silodosin, formerly known as KMD- 3213, is a novel alpha-blocker for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia. It has unprecedented selectivity for alA-adrenoceptors, as compared to both alB- and alD- adrenoceptors, exceeding selectivity of all currently used a-blockers. Such selectivity has been shown in vitro with cloned receptor subtypes as well as in a range of isolated human and animal tissues. It translates into in vivo functional uroselectiv- ity in multiple animal species with efficacy against voiding dysfunction combined with a low degree of cardiovascular effects in both animals and patients.

Among the side effects were ejaculation disorders, but the clinical importance of this phenomenon remains unknown, since patients who have ejaculation disorders during treatment, do not want to stop treatment. Silodosin have a good pharmacokinetic profile - maximal therapeutic plasma concentration is achieved after 2-6 hours, and the half-life is 13 hours.These properties make silodosin a clinically promising new agent.

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