Amiodarone pharmacokinetics

Am Heart J. 1983 Oct;106(4 Pt 2):840-7. doi: 10.1016/0002-8703(83)90006-6.

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.

MeSH terms

  • Adipose Tissue / metabolism
  • Adult
  • Aged
  • Amiodarone / analogs & derivatives
  • Amiodarone / blood
  • Amiodarone / metabolism*
  • Benzofurans / metabolism*
  • Female
  • Half-Life
  • Humans
  • Kinetics
  • Liver / metabolism
  • Lung / metabolism
  • Male
  • Metabolic Clearance Rate
  • Middle Aged

Substances

  • Benzofurans
  • desethylamiodarone
  • Amiodarone