Metabolism of ketotifen by human liver microsomes. In vitro characterization of a tertiary amine glucuronidation
Le Bigot, J.F.; Cresteil, T.; Kiechel, J.R.; Beaune, P.
Drug Metabolism and Disposition the Biological Fate of Chemicals 11(6): 585-589
1983
ISSN/ISBN: 0090-9556 PMID: 6140144 Document Number: 217273
Biotransformation of ketotifen ) were determined with native and detergent-treated microsomes. Treatment by Triton X-100 increased by about 3-fold the conjugation reaction. No sex difference was observed and N-glucuronidation did not seem to be inhibited either by bilirubin or by 4-nitrophenol. Human liver microsomes are a useful and suitable in vitro model for studying metabolic routes, specific for man, as in the case of ketotifen. Obviously, the results obtained can only reflect partially the multiplicity of in vivo events and interpretation has to be complemented by investigations with other models.