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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

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

Case report: 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.[1]

References

  1. ECG changes and plasma concentrations of propafenone and its metabolites in a case of severe poisoning. Fonck, K., Haenebalcke, C., Hemeryck, A., Belpaire, F., Jordaens, L., Calle, P., Buylaert, W. J. Toxicol. Clin. Toxicol. (1998) [Pubmed]
 
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