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Tissue distribution of propafenone in the rat after intravenous administration

European Journal of Drug Metabolism and Pharmacokinetics volume 16, pages 23–27 (1991)Cite this article

Summary

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.

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Affiliations

  1. Departement de Farmacologia, Facultat de Veterinària, Universität Autònoma de Barcelona, 08193, Bellaterra, Spain

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

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  1. J. Fernández
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  2. L. Lligoña
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  3. A. Puigdemont
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  4. R. Guitart
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  5. J. L. Riu
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  6. M. Arboix
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Fernández, J., Lligoña, L., Puigdemont, A. et al. Tissue distribution of propafenone in the rat after intravenous administration. European Journal of Drug Metabolism and Pharmacokinetics 16, 23–27 (1991). https://doi.org/10.1007/BF03189870

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  • DOI: https://doi.org/10.1007/BF03189870

Keywords

  • Antiarrhythmic drugs
  • propafenone
  • tissue distribution
  • plasma kinetics