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Effect of pirenzepine on the N ‐demethylation of D(−)ephedrine and ethylmorphine by rabbit liver microsomes
Author(s) -
ElObeid H. A.,
AlRashood K. A.,
AlKhamees H. A.,
AlKhamis K. I.,
Mian M. S.
Publication year - 1993
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510140310
Subject(s) - ephedrine , ethylmorphine , microsome , pirenzepine , chemistry , demethylation , pharmacology , rabbit (cipher) , endocrinology , medicine , biochemistry , in vitro , mathematics , muscarinic acetylcholine receptor , receptor , gene expression , dna methylation , gene , statistics
The possible interaction of pirenzepine with the mixed‐function oxidases obtained from phenobarbital‐pretreated rabbit microsomes was examined in vitro . Under experimental conditions that did not lead to its own N ‐demethylation, the drug inhibited the microsomal oxidase systems responsible for the N ‐demethylation of D(‐)ephedrine and ethylmorphine. Kinetic studies showed that pirenzepine inhibited the metabolism of both drugs in a competitive manner. The results indicated that the observed pirenzepine stability to the hepatic N ‐demethylating system is not a result of low affinity of the drug to the system.