Morphine metabolites

  title={Morphine metabolites},
  author={Lona Louring Christrup},
  journal={Acta Anaesthesiologica Scandinavica},
  • L. Christrup
  • Published 1 January 1997
  • Biology, Chemistry
  • Acta Anaesthesiologica Scandinavica
Morphine is a potent opioid analgesic widely used for the treatment of acute pain and for long‐term treatment of severe pain. Morphine is a member of the morphinan‐framed alkaloids, which are present in the poppy plant. The drug is soluble in water, but its solubility in lipids is poor. 
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Morphine-6-glucuronide is more mu-selective and potent in analgesic tests than morphine.
6-glucuronidation of morphine confers to this widely used analgesic increased potencies both in terms of receptor binding (selectivity) and of antinociceptive properties, and Na+ ions and Gpp(NH)p inhibit similarly the binding of morphine and M6G at the mu sites, suggesting that M 6G is a mu agonist.
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It is of value to distinguish inadequate pain control due to altered morphine kinetics from true opioid resistance in order to initiate appropriate changes in therapy, and knowledge of the pharmacokinetics of morphine has important clinical implications.
Pharmacological characterization of morphine-6 beta-glucuronide, a very potent morphine metabolite.
Results imply that morphine-6 beta-glucuronide elicited its analgesic actions through the same receptor mechanisms as morphine, which strongly suggests that this metabolite plays an important role in morphine's actions.
Explanation at the opioid receptor level for differing toxicity of morphine and morphine 6-glucuronide.
The radiolabelled opioid receptor binding affinities of morphine and its active metabolite morphine 6-glucuronide at the total mu, mu 1, mu 2 and delta receptors were determined and provided a possible explanation for the reduced respiratory depression and vomiting seen following morphine6-glUCuronide in man.
Renal failure does not impair the metabolism of morphine.
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