UGT2B7 inhibition for opiate users

[Cartesia]

Here's the only previous BL information I could find on it.

http://www.bluelight.ru/vb/showthread.php?t=279372&highlight=UGT2B7


Has anyone attempted to use UGT2B7 inhibitors to prevent opiate metabolism? (which i presume would keep you higher, for longer.)

There's always talk about CYP3A4 but apparently UGT2B7 is the culprit for most of the breakdown so it seems strange that nobody ever seems to talk about it!

In the other thread I've linked there is some concern that one of the metabolites is actually a requirement for the opiate euphoria/high... is this true? I was under the impression that it was just the plain regular opiate that did all the work and the metabolites were inactive.

If the metabolite(s) is/are acitve... which enzyme is it then that breaks them down into inactives?

I would've thought there'd be plenty of desperate addicts come before me trying to find any info on this!

Is UGT2B7's involvement with opiates something only newly discovered? I dont remember reading anything about it a few years ago when I got into codeine.

 

[N0 W4RN1NG]

Well, codeine requires CYP2D6 to turn it into morphine, codeine by itself is pretty worthless. Codeine is basically a prodrug for morphine.

There are some people out there who claim that hydrocodone and oxycodone highs are largely due to the small amount of hydromorphone and oxymorphone that CYP2D6 cranks out from their respective precursors. However, the amount of *morphone produced in the average individual from a hydrocodone or oxycodone dose is very small, and bioassays from several people myself included have confirmed that both hydrocodone and oxycodone are not noticeably different when taken while CYP2D6 is strongly inhibited or not.

I had, on a different forum, proposed a method of opioid potentiation involving glucoronidation inhibition like you mentioned, and I was using naproxen sodium (aleve) and quinine (tonic water) as my UGT2B7 inhibitors. As far as I could tell, there aren't too many UGT2B7 inhibitors OTC.

The Aleve and tonic water, especially when coupled with cimetidine for CYP450 2D6\3A4 inhibition, worked well to extend the duration of the high.


However, I cannot help but feel that aleve and quinine are relatively weak UGT2B7 inhibitors, if anyone knows of stronger ones let me know...

 

[Cartesia]

Tonic water? hmm... they were saying in the other thread that black pepper was as well hah.. I dunno I guess its possible, but it all sounds a bit like smoking banana peels to me

Never heard of naproxen sodium, I'll look it up thanks.

Well, codeine requires CYP2D6 to turn it into morphine, codeine by itself is pretty worthless. Codeine is basically a prodrug for morphine.

Sorry should've been more specific - i meant one of the products from UGT2B7.. see the other thread I think for talk about that. I think it was the -6-glucoronide or something.. But again.. there wasnt any reference cited for that claim.

 

[seep]

Most (all?) statins are 2b7 substrates. Lipitor for instance. I have no idea if this is useful and/or safe.

Many benzos are substrates; the synergism b/w opiates and benzos may be due to more than the fact that both are CNS depressants.

How much quinine is in tonic water anyway?

 

[N0 W4RN1NG]

Most (all?) statins are 2b7 substrates. Lipitor for instance. I have no idea if this is useful and/or safe.

Many benzos are substrates; the synergism b/w opiates and benzos may be due to more than the fact that both are CNS depressants.

How much quinine is in tonic water anyway?

Interesting. I'm not sure, I would usually kill about half a bottle with 800mg naproxen and along with cimetidine it DEFINITELY lengthened the high.

Never heard of naproxen sodium, I'll look it up thanks.



Sorry should've been more specific - i meant one of the products from UGT2B7.. see the other thread I think for talk about that. I think it was the -6-glucoronide or something.. But again.. there wasnt any reference cited for that claim.

Naproxen sodium is the OTC painkiller Aleve, I'm sure you've heard of it.

Ahh, ok I understand. However, hydrocodone and oxycodone feel better IMO when I attempted to inhibit UGT2B7, and it definitely lasted longer. It felt a bit less noddy though, but definitely still high, if that makes sense.

 

[Cartesia]

Naproxen sodium is the OTC painkiller Aleve, I'm sure you've heard of it.

Nope... maybe it's not available here in australia? (or goes under a different name?)


I'll have to try the tonic water thing, just in case... would laugh if it was that simple! I'll down a 1.25L bottle of it and see if that has any effect.. any more than that wouldnt be worth it anyway.

maybe I'll mix some ground black pepper in there as well... :lol: ... sounds like something I'd try to do to get high when I as 14. . oh welll i have no dignity anymore anyway, I'll try anything.

 

[starfarer]

Black pepper will inihibit CYP2D6 unfortunately. It is also a CYP3A4 inhibitor which will contribute towards duration. Finally it is carcinogenic. Overall it probable isnt worth the gagging and nose pinching.
Piperine is a potent 3a4 inhibitor and cyp2d6 inducer so its worthwhile using that instead,

 

[Cartesia]

Hey guys I've come back to bluelight to share a few stories around the place and wanted to dig this thread up to see if anyone has any new info on it again..

I finally got around to trying tonic water right now, but I've been doing a bit of research on the net..
According to the outline of one study I just read quinine prolonged the time of effect, but actually reduced the analgesic effects of codeine.. So I am unsure now.

Anyway I took the tonic water approx 30min after taking the codeine in an attempt to allow the codeine to metabolise into morphine, just in case quinine *does* inhibit cyp2d6.. so hopefully in the worst case scenario I'll get extension but not lose any high.. and inthe best case scenario I'll get higher and itll last longer

I will try piperine, but I won't make it a regular occurrence.

 

[Cartesia]

wow.. tonic water DEFINITELY increases the length of the high.. I drank 1.25L from about 30mins -> 1.5hrs after consuming the codeine..

No loss of high, at least not that I can notice.. these days its a bit hit and miss , whether i get off well from codeine.. but I'm definitely there ^_^

In fact this has been the best codeine experience I've had in months.. More testing necessary, but I'll be trying this a few times, and varying the timing of it too.


Also I was reading online apparently there is now a supplement which is concentrated or extracted piperine called Bioperine. I'm not sure if it's available in australia but I'll be looking into it.