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

T B Vree; R T van Dongen; P M Koopman-Kimenai

PubMed · 11092114

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

T B Vree·R T van Dongen·P M Koopman-Kimenai

Abstract

Eighty per cent of codeine is conjugated with glucuronic acid to codeine-6-glucuronide. Only 5% of the dose is O-demethylated to morphine, which in turn is immediately glucuronidated at the 3- and 6-position and excreted renally. Based on the structural requirement of the opiate molecule for interaction with the mu-receptor to result in analgesia, codeine-6-glucuronide in analogy to morphine-6-glucuronide must be the active constituent of codeine. Poor metabolisers of codeine, those who lack the CYP450 2D6 isoenzyme for the O-demethylation to morphine, experience analgesia from codeine-6-glucuronide. Analgesia of codeine does not depend on the formation of morphine and the metaboliser phenotype.

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Analgesics, Opioid Codeine Humans Models, Biological Morphine Pain Measurement Receptors, Opioid Journal Article Review

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T B Vree, R T van Dongen, P M Koopman-Kimenai. Codeine analgesia is due to codeine-6-glucuronide, not morphine.. https://pubmed.ncbi.nlm.nih.gov/11092114/

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