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Converting more Oxycodone into Oxymorphone in the liver?

51fifty

51fifty

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Mar 20, 2007
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Is there a supplement, chemical, or medication that can increase the amount of Oxycodone metabolized into Oxymorphone by the liver? If 10% of Oxycodone gets demethylated by the liver into Oxymorphone, can an enzyme (such as CYP-450) be induced/inhibited to increase this conversion? Such as Glutethimide's effects on Codeine.

Any thoughts on this? Glutethimide seems like it would have similar effects because it causes more Codiene to be demethylated. Which is the same process for Oxycodone, but the Schedule II tag makes it hard to obtain.
 
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CYP2D6 metabolizes oxycodone in oxymorphone so you can take Gluthenimide (example used by you). You can potentiate in the same you would for codeine.
 
Slapdragonx said:
CYP2D6 metabolizes oxycodone in oxymorphone so you can take Gluthenimide (example used by you). You can potentiate in the same you would for codeine.
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How safe would that be? Mixing downers with opiates isn't safe in general, and if it also potentiates the opiate perhaps even more so?
 
fryingsquirrel said:
How safe would that be? Mixing downers with opiates isn't safe in general, and if it also potentiates the opiate perhaps even more so?
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Yeah Glutethimide seems dangerous and it's schedule II. I'm searching for CYP2D6 inducers and only found a few, might answer my own question. I think this could be useful if there's an easily obtainable, safe drug that can double or triple the potentcy of methoxy opiates.
 
fryingsquirrel said:
How safe would that be? Mixing downers with opiates isn't safe in general, and if it also potentiates the opiate perhaps even more so?
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^Then any CYP inducer. I can't think of any nice/OTC ones off hand, there are far more inhibitors than inducers (at least readily available ones). I wouldn't expect much more in terms of effects anyway; maybe you can make an 80 feel like 85 mg.
 
johanneschimpo said:
^Then any CYP inducer. I can't think of any nice/OTC ones off hand, there are far more inhibitors than inducers (at least readily available ones). I wouldn't expect much more in terms of effects anyway; maybe you can make an 80 feel like 85 mg.
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It seems to be particularly the CYP450-2D6 enzyme. If there is one with even near the potentiating(word?) power of Glutethimide, say %5-10 more of Codiene or Oxycodone getting metabolized into its parent drug, that would make 100mg of Codiene = 100mg Codiene + 10mg Morphine. Almost doubling its potency. Could be useful if applied to those desperate and/or those who live where Codiene is OTC.
 
If you are looking to potentiate oxycodone, inhibit the 2d6, luckily that will help you out since inducers will make youre high stronger, it has its double edged sword of gettin the fuck outa there faster too. Inhibitors like cimetidine, celebrex (NSAID) and ranitidine. all which you can find in youre local pharmacy. Increases the serum levels of oxycodone, oxymorphone in your system. ;)
 
I just read the prescribing info for Oxycontin. Its confirmed, CYP450-2D6 is the enzyme responsible for demethylating the methoxy group on Oxycodone turning it into Oxymorphone. Inducers of this enzyme increase the amount of OC metabolized into OM. CYP450-3A demethylated both OC and OM at the nitrogen atom turning them into inactive metabolites. CYP450-3A inhibitors prolong the serum levels by preventing this reaction.
 
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