Summary
The pharmacokinetics of amiodarone (A) and its desethylamiodarone metabolite (DEA) were compared in the same coronary patients after a first 1000 mg dose and one-month chronic oral dosing. Terminal half-life ( t1/ 2 el) of amiodarone increased from a mean (SD) 2 4 . 1 ± 19.5 h after the first dose to 20.4 ± 4.8 days after the last dose. Desethylamiodarone slowly appeared in the plasma after the first oral dose and its apparent t el was 61.6 ± 26.6 h. After one-month dosing apparent tV2 el of desethylamiodarone increased to 29.5 + 9.7 days. Mean maximal plasma amiodarone/desethylamiodarone concentration ratio decreased from 9.2 ± 5.0 to 2.0 ± 0.6 after chronic dosing. This change was mainly related to an increase in the plasma concentration of desethylamiodarone. These data suggest that after long-term treatment with amiodarone, the complete elimination of the drug and its metabolite may need 3–4 months in some patients.
The results of this study were presented in part at the meeting of the Société Française de Thérapeutique et de Pharmacologie Clinique, Paris, December 1985.
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Poirier, J.M., EscoubET, B., Jaillon, P. et al. Amiodarone pharmacokinetics in coronary patients: Differences between acute and one-month chronic dosing. European Journal of Drug Metabolism and Pharmacokinetics 13, 67–72 (1988). https://doi.org/10.1007/BF03189931
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DOI: https://doi.org/10.1007/BF03189931