Effects of silodosin (KMD-3213) on phenylephrine-induced increase in intraurethral pressure and blood pressure in rats--study of the selectivity for lower urinary tract

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
Satoshi TatemichiNobuo Shibata

Abstract

The effects of silodosin, an alpha(1A)-adrenoceptor (AR) antagonist, and of other alpha(1)-AR antagonists on the phenylephrine (PE)-induced increase in intraurethral pressure (IUP) and on blood pressure (BP) were studied in anesthetized rats. The drugs were administered intravenously (i.v. study) or intraduodenally (i.d. study). IUP and BP were measured via catheters inserted into the prostatic urethra and common carotid artery, respectively. In the i.v. study, drugs were administered every 30 min for effects on BP, and 5 min before each PE-injection (30 microg/kg, every 60 min) with stepwise increases in dose for effects on IUP. In the i.d. study, one dose of drug was administered per rat, then IUP and BP were observed for 4 h [IUP being measured time-dependently following PE-injection (30 microg/kg)], and IUP and BP were expressed as a percentage of the values without any drugs. ID(50) for IUP and ED(15) for BP were calculated, and uroselectivity was determined as ED(15)/ID(50) for each drug. All drugs both inhibited the IUP increase and lowered BP, each effect being dose-dependent. The order of uroselectivities was silodosin (11.7)>tamuslosin (2.24)>naftopidil (0.133) in the i.v. study, and silodosin (26.0)>tamuslosin (3.82)...Continue Reading

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Mar 7, 2006·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Satoshi TatemichiNobuo Shibata

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Citations

Jul 15, 2011·Clinical Interventions in Aging·Masaki YoshidaKazuki Kawabe
Nov 29, 2007·Expert Opinion on Investigational Drugs·Masaki YoshidaKazuki Kawabe
Mar 7, 2006·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Yoshitaka TomiyamaNobuo Shibata
Jan 10, 2012·International Journal of Urology : Official Journal of the Japanese Urological Association·Kimio SugayaHideyuki Yamamoto
Oct 3, 2018·Indian Journal of Psychological Medicine·Sujita Kumar Kar
Mar 7, 2006·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Mamoru KobayashiNobuo Shibata

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