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Opioids Why do people say that codeine inhibits itself?

opiateaddict123

Greenlighter
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Apr 14, 2015
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If I am not mistaken a small amount of codeine is converted into morphine by the enzyme cyp2d6 and is converted to codeine-6-glucuronide and norcodeine by the liver enzyme cyp3a4. As far as I am aware it is well known that codeine-6-glucuronide is the main compound responsible for the analgesic/recreational effects of codeine. Now let's take hydrocodone, which is effectively a parallel of codeine as codone=codeine. A small amount of Hydrocodone is converted by the same enzyme cyp2d6 to hydromorphone. Same with oxycodone to oxymorphone. If this is true, why do people say codeine is a special opioid in that it needs an enzyme to be converted. AFAIK all members of the codone family work in this way, ie some of the drug is converted into a form of morphine and some of the drug is converted into other active metabolites. So why do people say codeine is any different to dihydrocodeine, hydrocodone or oxycodone? How is dihydrocodeine and hydrocodone different in the way they work compared to codeine?

Thanks
 

Runtoparadise

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I won't go into too much detail, but only some ppls individual body chemistry can convert codiene into morphine. In to as how the codones & morphine/morphones work, it's that codiene has a ceiling effect when the aforementioned don't.

Rtp
 

pinpoint

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Codeine inhibits CYP2D6 which is the metabolic pathway by which O-demethylation to morphine takes place. However there have been some studies that have stated that it's the codeine glucuronide metabolite which is responsible for the analgesia of codeine and that does not share the 2D6 metabolic pathway.
 

sekio

Moderator: N&PD
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As far as I am aware it is well known that codeine-6-glucuronide is the main compound responsible for the analgesic/recreational effects of codeine.
It was not always "well known", it was widely assumed until recently the narcotic effect of codeine came entirely from its metabolism to morphine.

Hydrocodone and oxycodone actually show appreciable amounts of activity at opioid receptors on their own, which codeine and dihydrocodeine lack.
 
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