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Related Experiment Videos

Codeine analgesia is due to codeine-6-glucuronide, not morphine.

T B Vree1, R T van Dongen, P M Koopman-Kimenai

  • 1Institute for Anaesthesiology, Academic Hospital St Radboud, Nijmegen, The Netherlands.

International Journal of Clinical Practice
|November 25, 2000
PubMed
Summary

Codeine

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Pain Management

Background:

  • Codeine is a widely used analgesic.
  • Its analgesic effects are traditionally attributed to its conversion to morphine.
  • Individual differences in metabolism can affect codeine's efficacy.

Purpose of the Study:

  • To investigate the active metabolite responsible for codeine's analgesic effects.
  • To determine if morphine is essential for codeine analgesia.
  • To clarify the role of CYP450 2D6 in codeine's pain relief.

Main Methods:

  • Analysis of codeine metabolism pathways.
  • Comparison of analgesic effects in different metabolic phenotypes.
  • Assessment of codeine-6-glucuronide activity.

Main Results:

  • Eighty percent of codeine is metabolized to codeine-6-glucuronide.
  • Only 5% of codeine is converted to morphine.
  • Poor CYP450 2D6 metabolizers achieve analgesia via codeine-6-glucuronide.

Conclusions:

  • Codeine-6-glucuronide is the primary active metabolite responsible for codeine's analgesic effects.
  • Morphine formation is not required for codeine-induced analgesia.
  • Analgesia from codeine is independent of the CYP450 2D6 metabolizer phenotype.

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