PMID: 8973992Nov 1, 1996Paper

Pharmacokinetics of tamsulosin hydrochloride in patients with renal impairment: effects of alpha 1-acid glycoprotein

Journal of Clinical Pharmacology
K KoisoS Higuchi

Abstract

The pharmacokinetics of tamsulosin hydrochloride in patients with renal impairment were compared with those in healthy volunteers, and the factors that influenced plasma levels of tamsulosin were elucidated. A single oral dose of 0.2 mg of tamsulosin was given and blood and urine samples were obtained for 36 hours after administration. Unbound plasma concentration of tamsulosin was measured by a combination of equilibrium dialysis and liquid chromatography tandem mass spectrometry methods to examine the effect of protein binding on the pharmacokinetics of tamsulosin. Mean values for maximum concentration (Cmax) and area under the concentration-time curve (AUC) of total drug (Cmax,t and AUC1) in patients with renal impairment were 73% and 211% greater, respectively, than those in healthy volunteers. Mean Cmax and AUC of unbound drug (Cmax,u and AUCu), however, were almost the same in the two groups. A high correlation was found between alpha 1-acid glycoprotein (alpha 1-AGP) concentration and AUCt, but no correlation was found between alpha 1-AGP concentration and AUCu,0-36) or between creatinine clearance (ClCR) and AUCu,0-36). These results show that in patients with renal impairment, the pharmacokinetics of tamsulosin are aff...Continue Reading

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Citations

Nov 20, 2003·Experimental Animals·Takashi KuribayashiShizuo Yamamoto
May 24, 2018·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Takuya EbiharaYoshihiko Tagawa
Oct 21, 2006·British Journal of Clinical Pharmacology·Kaori ItoYasufumi Sawada
Sep 30, 2016·Journal of Clinical Pharmacology·Masahiro ShimamuraYohei Miyamoto
Nov 10, 2021·Archives of Pharmacal Research·Chang-Keun ChoSeok-Yong Lee

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