PMID: 9173686Apr 1, 1996Paper

Pharmacokinetics and metabolism of zamifenacin in mouse, rat, dog and man

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
K BeaumontD A Smith

Abstract

1. Zamifenacin was rapidly metabolized in vitro by liver microsomes from rat, dog, and man. 2. Zamifenacin exhibited extensive plasma protein binding with human plasma showing 20 and 10-fold higher binding that that in rat and dog respectively. 3. Following oral administration to animals, metabolic clearance resulted in decreased bioavailability due to first-pass metabolism in rat and mouse. Oral clearance in man was low as a result of increased metabolic stability and increased plasma protein binding compared with animals. 4. Metabolism was the major route of clearance of zamifenacin with the primary metabolic step resulting in opening of the methylenedioxy ring to yield the catechol. In man, this metabolite was excreted as the glucuronide conjugate, whereas in the animal species it was further metabolized by mono-methylation of the catechol.

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Citations

May 20, 1998·Journal of Pharmaceutical and Biomedical Analysis·O CorcoranJ K Nicholson
Apr 15, 2008·Chemical Research in Toxicology·J Matthew HutzlerLarry C Wienkers
Sep 24, 2013·Biochemical Pharmacology·Jianghong Fan, Inés A M de Lannoy
Mar 17, 2010·Journal of Pharmaceutical Sciences·Ying ZhangCraig Giragossian
Oct 9, 1998·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·D E AmacherK Beaumont
Mar 14, 2007·Journal of Pharmacological and Toxicological Methods·James T LimberisRuth L Martin
Aug 8, 2015·Toxicological Sciences : an Official Journal of the Society of Toxicology·Barbara A WetmoreMelvin E Andersen
Mar 1, 2005·Basic & Clinical Pharmacology & Toxicology·Han van de Waterbeemd
Aug 21, 2010·Critical Reviews in Toxicology·S J Enoch, M T D Cronin
Feb 13, 1999·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·L J Smith
Jun 8, 2021·Journal of Pharmaceutical Sciences·Akinori TakemuraKousei Ito
Apr 20, 2001·Journal of Medicinal Chemistry·H van De WaterbeemdD K Walker

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