INDUCTION OF DISOPYRAMIDE N-DEALKYLATION BY PHENOBARBITAL AND DISOPYRAMIDE IN RAT-LIVER

  • 1 January 1979
    • journal article
    • research article
    • Vol. 239  (1) , 16-23
Abstract
An in vitro assay for the determination of the activity of disopyramide[4-diisopropylamino-2-phenyl-2-(2-pyridyl)-butyramide]-N-dealkylation was developed. This reaction was apparently catalyzed by the liver microsomal cytochrome P-450 centered monooxygenase system. Phenobarbital enhanced the N-dealkylation of disopyramide 4-fold, and disopyramide itself 1.6-fold, but methylcholanthrene was not effective. Disopyramide increased ethoxycoumarin deethylation 1.6-fold, and had a slight increasing effect on the activity of epoxide hydratase, but did not affect the activities of glutathione S-transferase or UDPglucuronosyltransferase. Disopyramide is an antiarrhythmic drug.

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