Role of CYP2B6 in Stereoselective Human Methadone Metabolism

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Abstract
METHADONE is an efficacious, inexpensive, cost effective, utilitarian μ-opioid agonist with clinical application in adults, children and even neonates. It is effective in the treatment of acute, chronic, neuropathic, and cancer pain and can be administered via intravenous, oral, nasal, rectal, epidural, and other routes.1,2 Methadone is used in opioid rotation strategies, is increasingly being used as a first-line analgesic, and is a mainstay in the treatment of opioid addiction. Methadone is usually administered as a racemic mixture of R - and S -enantiomers, although nearly all μ-opioid agonist activity resides in the R -enantiomer.3