Pharmacokinetics of amiodarone in rats

E. Riva, M. Gerna, P. Neyroz, R. Urso, I. Bartosek, A. Guaitani

Research output: Contribution to journalArticlepeer-review

Abstract

We studied the kinetics of amiodarone in the rat. After an intravenous dose of 50 mg/kg, the time-course of the drug concentrations was assessed by high-pressure liquid chromatography in blood and tissues up to 16 h. The drug disappeared from the blood with an elimination half-life (t1/2β) of 514 min and distributed extensively into tissues [apparent volume of distribution (Vd) = 29.51 L/kg]. Concentrations were highest in liver, kidney, and heart, and lowest at all times in the brain. The highest concentrations were found within 5 - 30 min of administration. Amiodarone accumulated extensively in adipose tissue and reached a fat/blood concentration ratio of about 1,000 at 16 h. Single-pass rat liver perfusion experiments gave an hepatic extraction ratio of 0.49 and an intrinsic clearance of 5.48 ml/min. Amiodarone disappearance in rat liver recirculation experiments was biexponential, with a half-life of 58 min.

Original languageEnglish
Pages (from-to)270-275
Number of pages6
JournalJournal of Cardiovascular Pharmacology
Volume4
Issue number2
Publication statusPublished - 1982

Keywords

  • Amiodarone
  • Kinetics
  • Perfused liver
  • Rat

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine
  • Pharmacology

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