ECG changes and plasma concentrations of propafenone and its metabolites in a case of severe poisoning

Journal of Toxicology. Clinical Toxicology
K FonckW Buylaert

Abstract

Propafenone is a class IC antiarrhythmic agent metabolized into two major metabolites, 5-hydroxypropafenone and N-depropylpropafenone. The potency of 5-hydroxypropafenone to block fast sodium channels is comparable to that of its parent. We report the positive correlation between plasma concentrations and electrocardiographic changes in a patient with severe oral self-poisoning. Serial ECG changes were measured and plasma concentrations were determined by high-performance liquid chromatography. The initial plasma concentrations of propafenone were in the toxic range and correlated with the widening of the QRS-complex. The slow decline in concentration during this first phase might relate to saturation of the isoenzyme CYP2D6. The half-life of propafenone, calculated from the second phase, was approximately 3 hours, defining the patient as a fast metabolizer. The initial concentrations of the metabolite N-depropylpropafenone were surprisingly higher than those of 5-hydroxypropafenone which may also be due to saturation of CYP2D6.

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Citations

Apr 8, 2010·Journal of Medical Toxicology : Official Journal of the American College of Medical Toxicology·Hanna OvaskaPaul I Dargan
Jun 16, 2010·The Canadian Journal of Cardiology·Adam YeungKenneth Gin
Jul 5, 2003·The Annals of Pharmacotherapy·Aurélie C MoliaThierry C Trenque
Apr 1, 2017·Scientific Reports·Ching-Shuen WangOlga J Baker
Feb 21, 2002·World Journal of Gastroenterology : WJG·Q ZhouS Zeng

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