Amiodarone pharmacokinetics

Abstract

The single-dose pharmacokinetics of amiodarone have been studied in volunteer subjects given 400 mg doses by the intravenous and oral routes. The data show the compound to have a very large volume of distribution, a low total clearance, and a long and variable terminal elimination half-life. In patients the terminal elimination half-life was on the order of 40 days, with a more rapid phase of elimination in the first few days following the withdrawal of therapy. The terminal elimination half-life of desethylamiodarone was longer than that of the parent compound. High concentrations of amiodarone and its desethyl metabolite were found in tissue samples, with fat forming a potentially large tissue reservoir of the drug.

Anaesthesia and amiodarone

“…Both amiodarone and its major metabolite desmethylamiodarone are measurable in plasma for at least nine months after cessation of amiodarone therapy. 24 We are unable to prove a definite cause and effect relationship between amiodarone therapy and the complications which we found; however, complications and mortality were significantly more frequent in patients taking amiodarone than in our control group of patients in whom one would expect a high incidence of complications and death.…”

Effects of amiodarone and thyroid dysfunction on myocardial calcium, serum calcium and thyroid hormones in the rat

“…These concentrations are within the therapeutic range defined in man (approximately 1.5-3.5mg litre-') (Holt et al, 1983).…”

Efficacy, Safety, and Determinants of Conversion of Atrial Fibrillation and Flutter With Oral Amiodarone

“…[16][17][18][19][20] Others found a clear concentration-related effect of amiodarone on QT-interval prolongation, slowing of heart rate, and suppression of ventricular arrhythmias. [21][22][23] The present study showed that for conversion of atrial fibrillation, plasma concentrations of desethylamiodarone were more important than those of the parent compound. This is in agreement with previous studies 24 and is possibly related to a high myocardium/plasma concentration ratio in the case of desethylamiodarone.…”