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Brain levels of dextromethorphan and the intensity of opioid withdrawal in mice (2008)

Brain levels of dextromethorphan and the intensity of opioid withdrawal in mice (2008)

  1. Metomni
    Bisaga A, Kos T, Wójcikowski J, Daniel WA, Popik P. Drug & Alcohol Dependence 2008 May 1;95(1-2):147-51. Epub 2008 Mar 6.

    Consistent with their antagonistic actions at N-methyl-d-aspartate type glutamate receptors, dextromethorphan (DXM) and its metabolite, dextrorphan (DXT) decrease the intensity of opioid withdrawal syndrome. Since quinidine (QND) affects CYP2D6-mediated metabolism and P-glycoprotein governed transport, we sought to determine whether co-treatment with QND would affect brain levels of DXM and DXT as well as the effect of these compounds on opioid withdrawal syndrome in mice. We found that DXM dose dependently inhibited the intensity of opioid withdrawal syndrome and that there was a tendency for a further decrease when QND was co-administered with DXM. Administration of 30mg/kg of DXM resulted in higher brain levels of DXM and DXT than administration of 10mg/kg of DXM, but much lower DXT levels than that produced by 30mg/kg of DXT. Co-treatment with QND resulted in higher brain levels of DXM (but not DXT) suggesting that QND produces an increase in the brain availability of DXM. In summary, brain levels of DXM were inversely correlated with the intensity of opioid withdrawal syndrome. QND induced increased brain levels of DXM tend to attenuate the intensity of opioid withdrawal syndrome. We suggest that it is DXM, rather than DXT, that is responsible for the attenuating effect on the intensity of opioid withdrawal syndrome, and that the beneficial action of QND on the effect of DXM should be more pronounced in humans.

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  1. Mindless
    Mindless
    5/5,
    Version: 2008-04-01
    The effects of quinidine, which acts on p-glycoprotein transport, as well as CYP2D6, which mediates metabolism. Qinidine administered with dextromethorphan may increase brain availability of dextromethorphan. This study is based on data derived from mice, the action of quinidine on the effect of dextromethorphan 'should be more pronounced in humans'. This may be of benefit in detox and withdrawal, but also increases the potential for overdose.