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Codeine metabolites





Pharmacokinetics of codeine and its metabolite morphine in - Nature

8/13/2014
01:27 | Author: Tyler James

Codeine metabolites
Pharmacokinetics of codeine and its metabolite morphine in - Nature

Pharmacokinetics was measured over 24 h after drug intake and codeine and its metabolites in plasma and urine were analyzed by liquid.

Codeine is an analgesic drug acting on -opiate receptors predominantly via its metabolite morphine, which is formed almost exclusively by the genetically polymorphic enzyme cytochrome P450 2D6 (CYP2D6). Whereas it is known that individuals lacking CYP2D6 activity (poor metabolizers, PM) suffer from poor analgesia from codeine, ultra-fast metabolizers (UM) due to the CYP2D6 gene duplication may experience exaggerated and even potentially dangerous opioidergic effects and no systematical study has been performed so far on this question.

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Metabolism of drugsLXV Studies on the urinary conjugated

6/12/2014
03:14 | Author: Emily Peterson

Codeine metabolites
Metabolism of drugsLXV Studies on the urinary conjugated

The detection and estimation of urinary metabolites of codeine in rabbits, guinea pigs, rats, and mice were carried out by thin-layer and gas chromotography. It.

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Volume 19, Issue 7, July 1970, Pages 2353–2360 No articles found.

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Metabolism of morphine and codeine by guinea-pig liver - Springer

4/11/2014
05:21 | Author: Tyler James

Codeine metabolites
Metabolism of morphine and codeine by guinea-pig liver - Springer

When tacrine was given concommitantly, there were no significant increases inN-oxide formation eitherin vitro orin vivo. Codeine was identified as a metabolite.

Incubation of morphine with guinea-pig liver microsomal preparations resulted in the formation of 0.9% of the major isomer of morphine N -oxide (I) whereas with codeine, 19.5% of the major isomer (HI) and 0.1% of the minor isomer (IV) of codeine N -oxide were formed. Morphine — and codeine N -oxides (major isomers) were isolated in low concentrations from rat urine after administration of the corresponding tertiary alkaloids. When tacrine was given concommitantly, there were no significant increases in N -oxide formation either in vitro or in vivo. Codeine was identified as a metabolite of morphine after incubation with guinea-pig liver microsomes and after injection into rats.

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Interaction of ethanol with codeine metabolism in rat hepatocytes a

2/10/2014
07:48 | Author: Alex Watson

Codeine metabolites
Interaction of ethanol with codeine metabolism in rat hepatocytes a

In the presence of ethanol, the apparent first order fractional rate of total codeine metabolism was reduced by 66% (0.0783 vs 0.0271 min -1). There was no.

A multicompartmental pharmacokinetic model is presented, which based upon data from a previous study, describes the effects of ethanol (60 m M) on the metabolism of codeine (10 μM) in isolated rat hepatocytes. According to this model, about one third of codeine metabolized was transformed to morphine (13%) and norcodeine (18%), and two-thirds to unknown metabolites in the absence of ethanol. In the presence of ethanol, the apparent first order fractional rate of total codeine metabolism was reduced by 66% (0.0783 vs 0.0271 min -1). There was no alteration in the portion of codeine metabolized to norcodeine, but there was a 44% decrease in the fraction transformed to unknown metabolites and a tripling in the portion transformed to morphine. The fractional rate of codeine O-demethylation to morphine was apparently not sensitive to ethanol. In the absence of ethanol, about two-thirds of morphine was metabolized to morphine-3-glucuronide and the other third to unidentified metabolites. Only the glucuronidation process seemed to be inhibited by ethanol. The fractional rate of further metabolism of norcodeine to normorphine was similar in the absence or presence of ethanol. In conclusion ethanol co-incubation with codeine resulted in an inhibition of codeine conversion to unknown metabolites and norcodeine, and with morphine to morphine-3-glucuronide, but no inhibition in morphine production.

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