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 language | English |
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Pages (from-to) | 270-275 |
Number of pages | 6 |
Journal | Journal of Cardiovascular Pharmacology |
Volume | 4 |
Issue number | 2 |
Publication status | Published - 1982 |
Keywords
- Amiodarone
- Kinetics
- Perfused liver
- Rat
ASJC Scopus subject areas
- Cardiology and Cardiovascular Medicine
- Pharmacology