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Heroin Addiction and Related Clinical Problems: 1999, 01, 1 (pages: 19 - 34)

Pharmacokinetics and pharmacogenetics of methadone: clinical relevance

Eap C. B., Deglon J. J., Baumann P.

Summary: Recent data on the pharmacokinetics and the pharmacogenetics of methadone, taking into account its enantiomers, have been collected. In particular, it has been demonstrated that isozymes belonging to the cytochrome P450 superfamily play a major role in the metabolism of methadone. During the past ten years, a large amount of informations has been collected on this enzymatic system. In particular it is now well known that these isozymes can be inhibited or can be induced by specific compounds. A large variability in the activities of these isozymes has been shown, a variability which is both genetically and environmentally controlled. These data allow us to explain and possibly avoid the majority of metabolic interactions involving methadone and to undestand the interindividual variability of methadone pharmacokinetics. This latter point is of major clinical relevance and stresses the importance of individualization of methadone treatment