The Metabolism of Opioid Agents and the Clinical Impact of Their Active Metabolites

The Clinical Journal of Pain, 10/12/2011

A greater appreciation of the metabolism of commonly prescribed opioid analgesics and the impact of their active metabolites on efficacy and safety may aid prescribers in tailoring care for optimal outcomes.


  • This is a narrative review of the metabolism of various opioids that will highlight the impact of their active metabolites, and the potential impact of cytochrome P450 activity on analgesic activity.


  • An understanding of “opioid metabolic machinery,” cytochrome P450 activity, and drug–drug interactions in the context of opioid selection may benefit clinicians and patients alike.

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