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  • Title: Dose-dependent effect of propafenone on in vivo drug metabolism in the rat.
    Author: Chong MT, Svensson CK.
    Journal: Res Commun Chem Pathol Pharmacol; 1987 Nov; 58(2):147-56. PubMed ID: 3423421.
    Abstract:
    The effect of propafenone, an investigational antiarrhythmic, on in vivo drug metabolism was examined in the rat using the model substrate antipyrine. Administration of a single oral dose of propafenone 100 mg/kg one hour prior to antipyrine administration resulted in a 23% reduction in antipyrine clearance. Similarly, administration of a dose of 200 mg/kg resulted in a 40% reduction in antipyrine clearance. These data indicate that propafenone, like other agents subject to substantial first-pass metabolism, is capable of inhibiting oxidative drug metabolism in vivo. The dose-dependency of this phenomenon suggests a competitive mechanism.
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