Opioids Oxymorphone Specific Metabolism Info?

[arthunter888]

I've done some searching, and can't find a good amount of info on Oxymorphone metabolism. All I have found are the names of 2 metabolites: 6-hydroxyoxymorphone, oxymorphone-3-glucuronide.

I would like to know (assume ROA is nasal Opana-er):

What are the main active metabolites responsible for its effects?

What are the relative potencies of these metabolites?

Which enzymes are responsible for which metabolites?

If you were to use enzyme inhibition and/or induction to maximize recreational euphoria, which potentiation method would you choose and why?


Thanks for any info.

 

[Captain.Heroin]

I've done some searching, and can't find a good amount of info on Oxymorphone metabolism. All I have found are the names of 2 metabolites: 6-hydroxyoxymorphone, oxymorphone-3-glucuronide.

I would like to know (assume ROA is nasal Opana-er):

What are the main active metabolites responsible for its effects?

What are the relative potencies of these metabolites?

Which enzymes are responsible for which metabolites?

If you were to use enzyme inhibition and/or induction to maximize recreational euphoria, which potentiation method would you choose and why?


Thanks for any info.

http://en.wikipedia.org/wiki/Glucuronidation

http://en.wikipedia.org/wiki/UDP-glucuronyltransferase

UDP-glucuronyltransferase is the enzyme that converts oxymorphone into oxymorphone-3-glucuronide.

I don't think cimetidine/WGFJ will help prevent oxymorphone's metabolization. That's just my gut instinct, I have no way of verifying that.

Someone else can fill you in on the rest. I haven't had the good fortune to try oxymorphone, so consider yourself lucky.

 

[Cane2theLeft]

Hydrocodone, for example is metabolized by CYP450 3A4 so when you take 3A4 inhibitors with it (say, WGFJ), it increases the effects.

There aren't any CYP450 enzymes that metabolize oxymorphone and so common enzyme inducers and inhibitors won't potentiate oxymorphone or otherwise interact at all. Cimetidine, WGFJ, etc have no interaction with oxymorphone.

I know you want some cool little trick to increase the efficacy of and/or decrease the necessary dose but I'm not aware of any for the reasons above.

As odd as it may sound, eating a high fat meal with OM will have an appreciable effect of peak plasma levels...

Following oral administration of oxymorphone hydrochloride, bioavailability is approximately 10%. Following oral administration of oxymorphone hydrochloride conventional tablets with a high-fat meal, peak plasma concentrations and area under the concentration-time curve (AUC) were increased 38%. Following oral administration of oxymorphone hydrochloride extended-release tablets with food, peak plasma concentrations were increased 50%; AUC reportedly was unchanged in one study and increased 18% in another study. Bioavailability of oxymorphone was increased in patients with renal impairment, those with hepatic impairment, and in geriatric individuals following administration as extended release tablets.

Concomitant administration of oxymorphone hydrochloride extended-release tablets with alcohol has resulted in variable effects on peak plasma concentrations of the drug. Changes in peak plasma concentrations of oxymorphone have ranged from a 50% decrease to a 270%
increase. Concomitant administration of oxymorphone with alcohol must be avoided. source

So *in effect* white grapefruit juice is to hydrocodone what a big bacon cheeseburger is to oxymorphone