The truth about opiate potentiators

[mikemikemike]

Has anyone noted a significant difference using cimetidine and/or grapefruit juice? Is this just scientific that says they use the same liver enzyme. I can't say that I've ever noticed a difference. What % of difference would you expect 400 mg of cimetidine and a cup of 100% grapefruit juice taken 30 minutes before ingestion to have? Has anyone oticed a bigger difference with higher doses and more juice. Tagament used to be prescribed in 800mg caps, so that is safe, anyone ever done that with a liter of GF juice? Is this potentiation thing just heresay? I can tell with GF juice and benzos, thats it.

 

[mulberryman]

^^I've only noticed that the physical effects (ie, constipation) last longer, cimetidine and gf juice seem to have no effect on mental effects at all, IME.

 

[burn out]

while we are on this subject, i have another question to add to this. i read in another thread that because a potentiator will cause the drug to remain in your system longer (obviously) but at the same time, this causes you to build tolerance faster. so are you just wasting money buying cimetidine when you could just buy more of your drug of choice and dose higher?

 

[mulberryman]

It would seem that way, though cimetidine causes diarreah when taken without opiates. I've seen this make some of the w/d symptoms worse. (diarreah, especially)

 

[monstanoodle]

who said anything about buying?

(a quick slip of the hand *cough*)

 

[BodhiSvaha33]

I can definitely tell a difference after 2-3 glasses of grapefruit juice (consumed 1 hour prior), 2 tablespoons of Robitussin, and 1 teaspoon of Benadryl. I have not tried the juice by itself, however. I figure it's good for me and it can't hurt.

I'd add that the above potentiation regime seems to work for kratom and blue lotus as well as opiates.

 

[TheodoreRoosevelt]

It prevents it opiates from breaking down so theoretically I'd think this means the high lasts longer, not that it is actually stronger (although this would lead Drug/blood levels to persist longer than usual).

When I've tried it I didn't notice anything different. Heroin is always different in how long it lasts (different ratios of actual opiates in it, morphine etc) so I've never really definitely determined if it lasted longer.

Doesn't hurt though.

 

[Stuck]

I take a tagamet(cimetidine) 30 min before any opiate i take. It gives me a ridiculous nod even with a low dose and lasts ~10 hours.

 

[TheodoreRoosevelt]

So is tagamet/cimetadine OTC in the US? I've always been confused on the legality and I've searched quite a bit on it over the years. Always been kinda grey to me, like how the hell does anyone get it if it's prescription you know. It's not like oxycodone where there's a big market for it...

 

[SonOF]

So is tagamet/cimetadine OTC in the US? I've always been confused on the legality and I've searched quite a bit on it over the years. Always been kinda grey to me, like how the hell does anyone get it if it's prescription you know. It's not like oxycodone where there's a big market for it...

Tagament is certainly legal and available OTC in the US. It has no abuse potential that I know of.

 

[phr]

It prevents it opiates from breaking down so theoretically I'd think this means the high lasts longer, not that it is actually stronger (although this would lead Drug/blood levels to persist longer than usual).

Potentiation increases duration and strength. The duration is increased because it may take longer for the drug to metabolize. The strength is increased by more of the drug being available(ie prodrug enzyme inducing) and by the fact that there is more of the active drug.

 

[sonic]

It's hard to put an exact percentage on it. I haven't taken a potentiator and then taken blood samples and analyzed them because I don't work in a lab, hehe. I'm sure this has been done before with at least a few drugs. That is why things like grapefruit juice have been PROVEN to interact with drugs because they block enzymes. I'd say that a 4-600mg dose of tagament taken 45 minutes before an opiate might extend the high by 1-2 hours. I agree that it affects the physical effects of the drug. If you have a tolerance it means you can go longer without worrying about physical withdrawal, but you might not be high that much longer..

 

[mikemikemike]

It's hard to put an exact percentage on it. I haven't taken a potentiator and then taken blood samples and analyzed them because I don't work in a lab, hehe. I'm sure this has been done before with at least a few drugs. That is why things like grapefruit juice have been PROVEN to interact with drugs because they block enzymes. I'd say that a 4-600mg dose of tagament taken 45 minutes before an opiate might extend the high by 1-2 hours. I agree that it affects the physical effects of the drug. If you have a tolerance it means you can go longer without worrying about physical withdrawal, but you might not be high that much longer..

So do they only make for a longer duration, or increase potency? I took 450 mg of ciimetidine and 3 glasses of 100% GF juice and used a 25 mcg/hr mylan patch bucally tonight and I was nodding, not typical for me with a 25. I also had an empty stomach. I guess I answered my own question, but it has been a while since I've done a patch.

 

[mikemikemike]

while we are on this subject, i have another question to add to this. i read in another thread that because a potentiator will cause the drug to remain in your system longer (obviously) but at the same time, this causes you to build tolerance faster. so are you just wasting money buying cimetidine when you could just buy more of your drug of choice and dose higher?

Generic tagament is $4.99 for 50 200 mg tablets, about the cost of a xanax bar for 25 better opiate experiences.

 

[mikemikemike]

who said anything about buying?

(a quick slip of the hand *cough*)

I'm not big on theft. If I went to jail for stealing Tagament, I would probably be suicidal in my cell.

 

[theanine]

In my experience Cimetidine prolongs the hydrocodone euphoria quite significantly. Oxycodone to a lesser degree. GFJ might help, but must be deacidified by regular antacids after intake, the higher the GI's pH is the better it is for the extension of drug effects. This of course excludes Codeine and perhaps Heroin as they are prodrugs. Codones used to be thought as prodrugs but latest research shows that they in actuallity are not. Morphone into which they convert to affect the CNS minimally and extension of the effect of the parent drug via enzyme inhibition produces more of a benefit than the morphones they are converted into if that makes any sense.

 

[sonic]

So do they only make for a longer duration, or increase potency? I took 450 mg of ciimetidine and 3 glasses of 100% GF juice and used a 25 mcg/hr mylan patch bucally tonight and I was nodding, not typical for me with a 25. I also had an empty stomach. I guess I answered my own question, but it has been a while since I've done a patch.

I think that tagament mostly just increases the duration of the high for me. Phrozen's theory that the peak plasma concentration of the drug is basically increased due to enzyme blocking is interesting, and it could be true. The increase in the high doesn't seem to be a large noticeable amount for me unfortunately .

 

[phr]

Well, that's what you're trying to do when you're inducing 2D6. You're trying to increase the amount(and speed) of the prodrug that's getting converted to the active drug. With 3A4, you're essentially doing the opposite. You're trying to delay the metabolization of the active drug.

As for strength, yes it does increase strength(as well as duration). Take benzo potentiation as an example. Anyone who has potentiated benzos, knows that strength is certainly increased. Same applies to opiate potentiation.





I know I'm being vague, but it's late and I'm tired. Maybe I'll pull up some sources tomorrow.

Oh, and this has all been answered. There are quite a few great threads in OD about opiate potentiation, how it works, its limitations, etc. One really good thread was started by Lacey. It contains a lot of good discussion.

 

[TheodoreRoosevelt]

I don't know if that is actually increasing the strength though...

It prevents it from being metabolized, this just means that it persists in your blood longer. Your peak levels will still be the same with and without it, but the amount of morphine in your system after peak will be higher and last longer because it isn't being broken down as quick.

Benzos are actually interfering with what's going on in your head, cimetadine is just dealing with metabolization. Two completely different things.

Correct me if I'm wrong, of course.

Anyways you just find tagamet at the store like you'd find some tylenol? I've never noticed it in the aisles.

 

[phr]

It prevents it from being metabolized, this just means that it persists in your blood longer. Your peak levels will still be the same with and without it, but the amount of morphine in your system after peak will be higher and last longer because it isn't being broken down as quick.

It depends at what rate it's being eliminated. If plasma levels are higher, then the strength has been increased.

I bolded a part that would indicated increased strength.

Duration increase= Same amount(level) lasting longer. Similar peak plasma levels as before, but elimination/clearence rate is reduced.

Strength increase= More activity from same amount. Higher plasma level than before.