Effect of pirenzepine on the N-demethylation of D(-)ephedrine and ethylmorphine by rabbit liver microsomes

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...

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Published inBiopharmaceutics & drug disposition Vol. 14; no. 3; p. 271
Main Authors el-Obeid, H A, al-Rashood, K A, al-Khamees, H A, al-Khamis, K I, Mian, M S
Format Journal Article
LanguageEnglish
Published England 01.04.1993
Subjects
Animals
Dealkylation
Depression, Chemical
Ephedrine - pharmacokinetics
Ethylmorphine - pharmacokinetics
In Vitro Techniques
Male
Microsomes, Liver - drug effects
Microsomes, Liver - enzymology
Microsomes, Liver - metabolism
Mixed Function Oxygenases - metabolism
Phenobarbital - pharmacology
Pirenzepine - pharmacology
Rabbits
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Summary: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.
ISSN:0142-2782
DOI:10.1002/bdd.2510140310