Codeine+CYP3A4inhibitor+CYP2D6inducer

[jasoncrest]

Codeine is metabolized by CYP2D6 enzymes to Morphine, then Morphine is eliminated from the body by CYP3A4 enzymes.(*)
(*)(that's how I understand it, I don't know anything about chemistry)

So to get full effects from Codeine, I need a CYP2D6 inducer: Alcohol, and a CYP3A4 inhibitor: Grapefruit Juice.

My questions are:
#1 if I wanna take 250mg Codeine, how much Grapefruit Juice and Alcohol should I drink?
#2 when should I take these three substance (gfj, alcohol and codeine)?

 

[Bludda]

Codeine is metabolized by CYP2D6 enzymes to Morphine, then Morphine is eliminated from the body by CYP3A4 enzymes.(*)
(*)(that's how I understand it, I don't know anything about chemistry)

So to get full effects from Codeine, I need a CYP2D6 inducer: Alcohol, and a CYP3A4 inhibitor: Grapefruit Juice.

My questions are:
#1 if I wanna take 250mg Codeine, how much Grapefruit Juice and Alcohol should I drink?
#2 when should I take these three substance (gfj, alcohol and codeine)?

Approximately 6 or 7 glasses or commercial grapefruit juice (ie. the reconstituted crap) is needed to provide for a perceivable increase in the duration and intensity of any drug metabolised by CYP3A4.

As for the alcohol, I'm not sure...... I'd say be careful because it's a depressant, but then again I suppose it depends on your tolerance to codeine. Try to combo with a smaller dose of codeine and only a few full strength beers.

You will need to drink the grapefruit juice a few hours before you take the codeine. Then drink the alcohol in the hour before you take the codeine (depending on how much you wanna drink - I find too much alcohol with codeine gets me rat-arsed ) My thoughts with the alcohol are that it takes the body approximately one hour metabolise a standard drink. Therefore take the codeine just before you finish your last couple of drinks.

If it's any help to you, I can take around 250mg of codeine and around 7 standard drinks.... and feel pretty damn awesome.


Good luck, and god speed....



Respect and Peace


EDIT: I've reread your post a couple of times and have been thinking....

The alcohol shouldn't be necessary insofar as increasing your ability to metabolize codeine into morphine, because if you have consumed enough grapefruit juice to successfully inhibit the CYP3A4 enzyme, then you will only have one type of enzyme left (CYP2D6) that will be able to convert codeine anyway.

Any codeine not converted the first time around will just stay unmetabolized until it gets a chance to be made into morphine. (The inhibitory effects of grapefruit juice on CYP3A4 apparently last for about 5 hours).

Therefore the alcohol really is unneccessary unless you enjoy combining the two drugs - and if you haven't done so before, be careful.....you may want to try combo-ing codeine and booze at a lower dose before you throw into the grapefruit juice.

But if you're a pro, just grab a blanket and relax....


EDIT of the EDIT:

Forget the alcohol as a metabolic inducer CYP2D6....it also induces CYP3A4....Hahahahahahahahahaha. (The info is on this page somewhere - http://www.aafmed.com/comor/interactions.html)


Sorry about all the edits and stuff

 

[jasoncrest]

Thank you VERY much!

 

[Nof]

And how about potentiating codeine with carbamazapine? It's a CYP2D6 inducer I think.

 

[clip']

quinine sulphate works. combined with grapefruit juice, makes for a pretty intense codiene experience.

 

[jasoncrest]

And how about potentiating codeine with carbamazapine? It's a CYP2D6 inducer I think.

As I said, CYP2D6 converts Codeine to Morphine, and CYP3A4 eliminates Morphine from the body.
So you can potentiate Codeine with CYP2D6 inducers and with CYP3A4 inhibitors.
CYP2D6 inducers will make more Codeine converted to Morphine.
CYP3A4 inhibitors will let the Mophinr stay longer in the system.

Carbamazepine is a CYP2D6 inducer, so more Codeine will be converted to Morphine.
BUT it is also a CYP3A4 inducer, so it will make the morphine leave the body more quickly...

 

[Bludda]

he he he plus it will probably knock you out on your ass and you'll wake up 10 hours later with a headache.

The only useful benefit carbamazepine will have is that, as an antihistamine, it will prevent the itchies.

I'd say forget it as a potentiator though, it really is a very strong drug. Use a low dose of benzos eg. valium or xanax instead - they have a great synergy.

Be careful guys, we're all talking about mixing downers here....which can put you up shit creek without a paddle.

I would not recommend using both alcohol and a benzo to potentiate codeine.

 

[jasoncrest]

he he he plus it will probably knock you out on your ass and you'll wake up 10 hours later with a headache.

The only useful benefit carbamazepine will have is that, as an antihistamine, it will prevent the itchies.

I'd say forget it as a potentiator though, it really is a very strong drug. Use a low dose of benzos eg. valium or xanax instead - they have a great synergy.

Be careful guys, we're all talking about mixing downers here....which can put you up shit creek without a paddle.

I would not recommend using both alcohol and a benzo to potentiate codeine.

I already know everything I can take with Codeine to make the high better (benzos, muscle-relaxants, clonidine, etc...).
And I know the risk associated with mixing downers together.

I'm only interested in drugs affecting the metabolism of Codeine. (as I said CYP2D6 inducer + CYP3A4 inhibitor)

 

[BilZ0r]

CYP2D6 inducers are as rare as hens teeth. I think the availabile evidence is that ethanol inhibits CYP2D6, not induces it. (though I know there is evidence that alcoholics have high brain cyp2d6, though not hepatic).. Unless you've got some evidence that I don't know about...?

 

[jasoncrest]

CYP2D6 inducers are as rare as hens teeth. I think the availabile evidence is that ethanol inhibits CYP2D6, not induces it. (though I know there is evidence that alcoholics have high brain cyp2d6, though not hepatic).. Unless you've got some evidence that I don't know about...?

On another post (or is it this one?) someone said he read Ethanol was a CYP2D6 inducer.
I then made a search on google, and I remember I read on a site or two, that ethanol induce CYP2D6.

Now I made a more deep search on google. You an read many things on ethanol's action on CYP enzymes, but I didn't find anything saying it induce CYP2D6.
I even read on a site that there are no drugs that can induce CYP2D6...

Bilzor, if one day you find a drug that induce CYP2D6 without nasty side effects, promise you will tell us, ok?

 

[Nof]

I've experienced with carbamazapine as a recreational drug in my 'streetfreak' ("just eating whatever came by") days long time ago. I know how strong carbamezapine can be.
I know that CYP2D6 inducers are really hard to find, and that they can be very good with codeine. I've read that codeine with drug called gluthethymid (Sleep aid. Now it's impossible to get hands on it) was much better than codeine alone. So my question is - How effective can be carbamazapine as CYP2D6 inducer/How many codeine will metabolize into morphine by CYP2D6 after inducing it with carbamazapine?

 

[jasoncrest]

I've experienced with carbamazapine as a recreational drug in my 'streetfreak' ("just eating whatever came by") days long time ago. I know how strong carbamezapine can be.
I know that CYP2D6 inducers are really hard to find, and that they can be very good with codeine. I've read that codeine with drug called gluthethymid (Sleep aid. Now it's impossible to get hands on it) was much better than codeine alone. So my question is - How effective can be carbamazapine as CYP2D6 inducer/How many codeine will metabolize into morphine by CYP2D6 after inducing it with carbamazapine?

Carbamazepine is a CYP2D6 inducer, so more Codeine is converted to Morphine
BUT is is also a strong CYP3A4 inducer, so it clears the Codeine/Morphine very quickly from your system...

 

[jasoncrest]

Bilzor-> I see many sites where it is said that Ethanol hinder Codeine metabolism...

 

[clip']

I've experienced with carbamazapine as a recreational drug in my 'streetfreak' ("just eating whatever came by") days long time ago. I know how strong carbamezapine can be.
I know that CYP2D6 inducers are really hard to find, and that they can be very good with codeine. I've read that codeine with drug called gluthethymid (Sleep aid. Now it's impossible to get hands on it) was much better than codeine alone. So my question is - How effective can be carbamazapine as CYP2D6 inducer/How many codeine will metabolize into morphine by CYP2D6 after inducing it with carbamazapine?

TAKEN FROM EROWID.ORG :::::::::::;

GLUTHETHIMIDE
A combination of codeine and gluthethimide (a sleeping agent) has been used in some places as a heroin substitute. Gluthethimide is an enzyme-inducer, and it allows the body to convert more than 10% of codeine into morphine

 

[Nof]

I've read about this on a different web page. Maybe author was using Erowid to prepare his article. But what's the problem?
And if someone uses codeine with gluthethimid as an heroine substitute it must be really potent (or same SOB was trying to sell it as a heroine, and it wasn't really strong).

 

[Survival0200]

EDIT: rubbish

 

[jasoncrest]

I have a question:

With Codeine, you want a CYP2D6 inducer and a CYP3A4 inhibitor.

Most CYP2D6 inducers (what you want) are also CYP3A4 inducers (what you do not want...).
These substances don't potentiate Codeine?

 

[Nof]

So. Are you now saying that GLUTHETHIMIDE is the ONLY inducer that will make your body convert more codeine to morphine?

No, I'm not saying anything like this. Gluthethimide was an example of CYP2D6 inducer, and what can that kind of medicine do with codeine. Gluthethimide is impossible to get but carbamazapine is also CYP2D6 inducer, and it's not really hard to obtain. I think that every CYP2D6 inducer will make more codeine change to morphine and I'm asking about what bluelighters think about it and if anyone have tried it.

 

[Survival0200]

EDIT: rubbish

 

[Survival0200]

EDIT: rubbish