Tissue distribution of propafenone in the rat after intravenous administration

J. Fernández, L. Lligoña, A. Puigdemont, R. Guitart, J. L. Riu, M. Arboix

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    Abstract

    Tissue distribution of propafenone has been studied in the rat. Measurement of propafenone was made in several tissues: plasma, heart, kidney, lung, liver, muscle, fat and brain, after i.V. administration of 2 mg/kg of the drug. The plasma propafenone kinetics profile can be described by a two-compartmental model. The pharmacokinetic parameters, derived from plasma levels, showed a t1/2β of 55.4 min, the central Vd/kg of 2.4 ml/kg, the Cl of 62.8 ml/min· kg and the AUC0-∞, of 31.6 μg· min/ml. The analysis of the propafenone tissue distribution showed the highest concentration of drug in the lung, followed by the heart and kidneys. A significant concentration was found in brain, muscle and adipose tissue, with concentration ratios (tissue/plasma) above 1. The half-life values obtained for individual organs and tissues are similar to those obtained in plasma, around 1 h. In the post-distributive phase, plasma and tissue concentrations decline in parallel. © 1991 Springer-Verlag.
    Original languageEnglish
    Pages (from-to)23-27
    JournalEuropean Journal of Drug Metabolism and Pharmacokinetics
    Volume16
    DOIs
    Publication statusPublished - 1 Jan 1991

    Keywords

    • Antiarrhythmic drugs
    • plasma kinetics
    • propafenone
    • tissue distribution

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