Key result
Propafenone and its metabolites 5-hydroxypropafenone and N-depropylpropafenone depressed Vmax at high concentrations and exhibited class IC antiarrhythmic properties in guinea pig ventricular fibers.
Why the study?
Do the propafenone metabolites 5-hydroxypropafenone and N-depropylpropafenone possess similar electrophysiological properties to the parent drug in guinea pig ventricular muscle fibers?
Population
Papillary muscle fibers from guinea pig ventricular myocardium
Comparison
Superfusion with propafenone… vs Baseline measurements before superfusion
Design
Preclinical
Authors
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Metabolite class IC effects in guinea pig fibers warrant human pharmacokinetic studies; leaves open any change to propafenone use.
Do the propafenone metabolites 5-hydroxypropafenone and N-depropylpropafenone possess similar electrophysiological properties to the parent drug in guinea pig ventricular muscle fibers?
The propafenone metabolites 5-OH-Pf and N-DP-Pf exhibit class IC antiarrhythmic properties similar to the parent drug, which may have cumulative clinical implications in extensive metabolizers.
Rouet et al. (1989) studied this question. Propafenone, 5-hydroxypropafenone, and N-depropylpropafenone vs. baseline was evaluated on Electrophysiological characteristics including maximal rate of depolarization (Vmax) and refractory periods. Propafenone and its metabolites 5-hydroxypropafenone and N-depropylpropafenone depressed Vmax at high concentrations and exhibited class IC antiarrhythmic properties in guinea pig ventricular fibers.
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