Title : Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro.

Pub. Date : 2003 Jun

PMID : 12756206






5 Functional Relationships(s)
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1 Based on studies with isoform-selective chemical inhibitors and expressed enzymes, CYP3A4 was the predominant enzyme involved in the metabolism of (R)-methadone. Methadone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 In recombinant CYP3A4, the metabolic clearance of (R)-methadone was about 4-fold higher than that of (S)-methadone. Methadone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 In recombinant CYP3A4, the metabolic clearance of (R)-methadone was about 4-fold higher than that of (S)-methadone. Methadone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 The present in vitro findings indicated that CYP3A4, CYP2C8, and CYP2D6 are all involved in the stereoselective metabolism of methadone (R)- and (S)-enantiomers. Methadone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 These data suggest that coadministration of inhibitors of CYP3A4 and CYP2C8 may produce clinically significant drug-drug interactions with methadone. Methadone cytochrome P450 family 3 subfamily A member 4 Homo sapiens