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Old 17-02-2008, 03:05
ironmics ironmics is offline
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Hydrocodone Pharmacokinetics

I was wondering if anyone knew of a good resource for the pharmacokinetics of hydrocodone as a means to investigate methods of potentitation. I found one list of metabolites that was somewhat helpful, and helped me understand why grapefruit juice could aid metabolism, but a fuller report of the kinetics would be helpful.

So far I've found a few very useful statements.

Unlike codeine and dihydrocodeine, very little of hydrocodone goes directly to glucuronidation unless it is first made into hydromorphone by 2D6.27 It is unclear if some hydrocodone is metabolized by 3A4, although it likely that some 6-carbon oxidation does occur at 3A4 to create norhydrocodone. Finally, unknown enzymes reduce the 6-carbon position to minor active metabolites.

Therefore, oxycodone is not a prodrug. There is an active metabolite, however, as 2D6 activity creates oxymorphone (Numorphan®), an active opioid analgesic.1 This 3A4 activity appears to create inactive noroxycodone.

Should mean that grapefruit juice will help both of these.(already known, but still interesting)

http://www.blackwell-synergy.com/doi....x?cookieSet=1

Good read if anyone is interested. It shows that inhibition of 3A4 reduces formation of norhydrocodone, but does not always boost production of hydromorphone. Inhibition also seems quite related to concentration of inhibitor(duh), but does mean swim will be doing studies one various amounts of grapefruit juice.

Last edited by ironmics; 17-02-2008 at 03:59.
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