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Dihydrocodeine: Difference between revisions
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Dihydrocodeine is metabolized via CYP2D6 to the active metabolite dihydromorphine, which has a potency similar to morphine. Other weakly active metabolites include nordihydrocodeine (which is formed via CYP3A4) and dihydrocodeine-6-glucuronide.<ref>Kirkwood LC, Nation RL, Somogyi AA. Characterization of the human cytochrome P450 enzymes involved in the metabolism of dihydrocodeine. Br J Clin Pharmacol. 1997;44:549-55.</ref> Although dihydrocodeine does have extremely active metabolites in the form of dihydromorphine and dihydromorphine-6-glucuronide, these metabolites are produced in such a small amount that they do not have clinically important effects.<ref>The role of active metabolites in dihydrocodeine effects (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/12665158</ref> | Dihydrocodeine is metabolized via CYP2D6 to the active metabolite dihydromorphine, which has a potency similar to morphine. Other weakly active metabolites include nordihydrocodeine (which is formed via CYP3A4) and dihydrocodeine-6-glucuronide.<ref>Kirkwood LC, Nation RL, Somogyi AA. Characterization of the human cytochrome P450 enzymes involved in the metabolism of dihydrocodeine. Br J Clin Pharmacol. 1997;44:549-55.</ref> Although dihydrocodeine does have extremely active metabolites in the form of dihydromorphine and dihydromorphine-6-glucuronide, these metabolites are produced in such a small amount that they do not have clinically important effects.<ref>The role of active metabolites in dihydrocodeine effects (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/12665158</ref> | ||
===Binding affinities (K<sub>i</sub>) | ===Binding affinities (K<sub>i</sub>)<ref>Affinities of Dihydrocodeine and its Metabolites to Opioid Receptors - Helmut Schmidt et al. (August 2002) | http://onlinelibrary.wiley.com/doi/10.1034/j.1600-0773.2002.910203.x/full</ref>=== | ||
* Mu opioid agonist - 325 nM | |||
* Kappa opioid agonist - 14242 nM | * Kappa opioid agonist - 14242 nM | ||
* Delta opioid agonist - 5905 nM | * Delta opioid agonist - 5905 nM | ||
Dihydrocodeine itself is a weak ligand for the opioid receptors however its main active metabolite - [[dihydromorphine]] and one of its metabolites - dihydromorphine-6-O-glucuronide show much stronger agonistic effects.<ref>Affinities of Dihydrocodeine and its Metabolites to Opioid Receptors - Helmut Schmidt et al. (August 2002) | http://onlinelibrary.wiley.com/doi/10.1034/j.1600-0773.2002.910203.x/full</ref> | Dihydrocodeine itself is a weak ligand for the opioid receptors however its main active metabolite - [[dihydromorphine]] and one of its metabolites - dihydromorphine-6-O-glucuronide show much stronger agonistic effects.<ref>Affinities of Dihydrocodeine and its Metabolites to Opioid Receptors - Helmut Schmidt et al. (August 2002) | http://onlinelibrary.wiley.com/doi/10.1034/j.1600-0773.2002.910203.x/full</ref> | ||