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Opioids The Ultimate Opiate Potentiation Thread

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Methadone is metabolised by several different P450 enzymes. SSRI's inhibit various of these enzymes, each to a different extent, and each with a slightly different profile as to which enzymes it inhibits. Fluvoxamine probably is the most effective in blocking methadone metabolism, although fluoxetine is probably also very effective. Paroxetine is lest less.

Grapefruit juice inhibits the metabolism of methadone in the gut, thus it only has an effect on how much methadone makes it into your body. SSRI's, cimetidine, and cat's claww inhibit hepatic (liver) enzymes, and thus allow more drug into the blood stream, and it stays in the body longer before being metabolised. You can take several enzyme inhibitors at once, and thus increase the enzyme inhibition by several enzymatic pathways.

I myself only take grapefruit juice with my methadone. I want to be on as few drugs as possible, and don't want to feel like I need to take other substances just to get higher. I have lost the ability to get high from methadone, and that is supposed to happen, it is why methadone is prescribed. To decrease cravings, and to also block an opiate high. If you take any opiates long enough, eventually you get to a point where more opiates just don't make you any higher anymore. This is called tolerance, and it is mostly due to a down regulation of opiate receptors.

If you really want to get back that opiate buzz, the best thing to do is to stop altogether, or to dramatically cut your dose back for awhile, and then go back up. That is a step I am unwilling to take as I started methadone to avoid having to constantly go through the withdrawal cycle whenever I ran out of dope. Opiates won't make you feel great for the rest of your life, and methadone maintenance wont' do it either, that is just the way the brain works.

Sorry to pop the bubble, I used to believe that by going on methadone I could just be high all the time. It took me two years to realize why I don't want to do that.
 
Last, I know antidepressants don't make everything rosy and happy. I have been on them for 13 years. But I do enjoy life more than I did when all I could think about was suicide. So for me, yes, they did make life more enjoyable. No, they don't make everybody (or anybody) super happy, it all depends on where you start from before you take them.
 
Okay, one last thing. I used to pop benzo's like they were candy. I found that they were great to take with opiates. Each person seems to have their own particular favorite benzo, for me, there was nothing quite like chlordiazepoxide, diazpepam, or alprazolam, these were my favorites. The main thing these had in common was their high lipophilicity, making them fast acting. Other benzo's also work, mostly to the same degree, some are just less potent, but that just means you take more mg's of them, no big deal. I used to snort them, they tasted great and made me feel just fine. Clonazepam was another favorite of mine.

Most any sedative, hypnotic, or relaxant will probably feel pretty good mixed with opiates. I never got anything from kava capsules, nor from valerian, but that may have just been me, or maybe it was because the capsules I took were just not strong enough, I don't know.

As far as NMDA antagonists go, the easiest and most interesting one for me always was dextromethorphan. I used to take Coricidin HPB II, they also had an antihistamine, but I have always had a huge antihistamine tolerance. I don't know if the DXM potentiated the opiates or not, I would usually take them when I was without, and they worked great for quelling withdrawal symptoms. One thing about DXM, it is all about dose. At low doses (160 to 240mg) I had a nice little stimulant buzz with little dissociative effect. At doses of 900 to 2000 mg, it was a strongly dissociate, no stimulation, and strongly psychedelic. In between doses were a combination of the two effects. That was for me, everybody is different..
 
Thanks very much Kebil, for attempting to answer my questions. I'm still a bit confused about Cat's Claw however. Is it an NMDA antagonist or not? I'm sure that i've read this before, even if CC has none of the dissociative effects of DXM for example. Maybe it is an enzyme inhibitor AND an NMDA antagonist, though pharmacology is not a strong point of mine.
As far as GFJ goes Kebil, do you find fresher stuff more effective or the cheap long-life stuff? I have read differing reports, some recommending the former, some the latter. Also, when do you take yours in relation to your methadone?
I guess i'll have to accept sometime that methadone is NOT a ticket to being high all the time, and tolerance will build much the same as any other opioid.
 
^ I'd recommend fresh GFJ about 45 minutes prior to ingestion of your opioid. But above that I'd recommend Tagamet instead.

I couldn't find anything definitive about Cat's Claw and NMDA antagonism, just a few forum threads similar to this one. I could find a few results, however, about it inhibiting CYP3A4.

ETA:

Kebil said:
Last, I know antidepressants don't make everything rosy and happy. I have been on them for 13 years. But I do enjoy life more than I did when all I could think about was suicide. So for me, yes, they did make life more enjoyable. No, they don't make everybody (or anybody) super happy, it all depends on where you start from before you take them.
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Good point. I can't say I ever experienced quite the same effect whilst using opioids and being treated for depression, but I see what you are getting at. Please, no more multiple posting in a row though.
 
Thanks Mr Blonde. Just that i'd heard that the cheap stuff contains more of the good stuff because they use GF rind as well, and it generally tastes more bitter. I'd imagine the difference is pretty minute anyway.
Any harm in taking GFJ AND Tagamet? They won't cancel one another out or anything?
 
Does anyone have any information about the metabolism of diphenoxylate hydrochloride? Is there anyway to boost absorption and increase the already long duration
?
 
Diphenoxylate does not readily cross the blood brain barrier, I have never heard of anybody using it to get high as you would mostly just get constipated (which is what it is for), but there may be some people with an unusual sensitivity to it.

As for which grapefruit juice to drink, I just drink like a bottle of tropicana ruby red grapefruit juice, although I have read that white grapefruit is better though, I have never come across any white grapefruit juice in any of my local grocery stores. I do believe I have an effect, only it is not a huge difference from not taking the juice with my methadone and I get by either way. I get 3 and 4 days carries, and the hardest thing for seems to be to not take it all at once, but I often take a double dose and end up going a day without, which is not really fun.

The only mechanism of action of Cat's Claw that I have come across is by CYP450 inhibition. It was actually in a brochure put out my one of the Methadone Maintenance programs. The only place I have ever heard about it being an NMDA antagonist is in here. I have done a fair bit of reading about various NMDA antagonists when I was working on my neuropharmacology thesis and never heard any reference to them (although that could just be absence of evidence and not evidence of absence.
 
Kebil said:
Diphenoxylate does not readily cross the blood brain barrier, I have never heard of anybody using it to get high as you would mostly just get constipated (which is what it is for), but there may be some people with an unusual sensitivity to it.
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It definitely crosses the BBB, but it lacks "warmth" and euphoria. I'd compare it to buprenorphine.
I keep some for the proverbial rainy day, I was interested if there is anyway to stretch it out such as taking cimetidine with suboxone. I know one of the metabolites diphenoxin is supposed to be much more potent.
 
I stand corrected. All these years I always thought diphenoxylate was more like imodium. It was the one opiate I never touched those years I was storming through our hospital pharmacy.
 
i too have a soft spot for diphenoxylate i think it signifigantly helps and some must cross the BBB its not at all like loperamide
 
Since a high fat meal increases bioavailability, would omega 3 fatty oils (fish oil) work as well?

*I tried searching but didn't find anything relevant to this question. Sorry if it has indeed been addressed.
 
Cimetidine as a heroin potentiator?

hey.. i was looking at some old opiate potentiation threads and one user said that cimetidine can be used as an opiate potentiator? I was seeing if this is true as well for heroin? It theoretically should be true right since heroin is the opiate.

this is what the post said

I've very effectively been using cimetidine as a potenater. The drug, usually used for acid reflux, is safe in higher doses and is relatively easy on the GI tract and system.

Cimetidine comes in doses of 200 mg per pill; and are used once a day for its typical recommendation of acid reflux. But it has been used upwards of a couple grams for severe stomach problems in hospitals; including ulcer's. I found this on Rxlist, by the way.

Methadone peaks for me at about the t + 1.5 hr point from ingestion. And usually plateau's off at this time for another 2 hours. During this time i "load" on cimetidine. Dosing usually 800 mg at t + 1 hr every half hour or so for the next 2-3 hours.

Since Cimetidine is eliminated and metabolized by the same enzyme that metabolizes opioids, i usually wait for the methadone to realize its effect first; then take the booster to hinder my body in metabolizing it quickly.

The potenation effect of cimetidine is most certainly noticable IME. 800 mg will push the effects up, including the itch and nod, for about 30 minutes - 1 hour. And will certainly accumulate in the system to overall increase and lengthen the plasma levels of methadone in my blood; at least it seems so. i've never directly monitored by plasma levels.

Cimetidine does occupy the CYD enzymes that metabolize opioids (and other drugs) so be careful when using it. Liver toxcity is probably possible including jaundice, abdominal pain, and eventually cirrohsis of the liver; so use sparingly!

Cimetidine is readily available OTC. I recommend the generic version which clearly has "cimetidine" printed on it. It should be no more than $5 for at least 30 200 mg pills. Its also known as tagment HB but for a much higher cost.

who knew? tagment and opiates?
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ok.. so the poster is saying that he ingests the cimetidine an hour and half after he takes the methadone.. so right when the effects of the methadone start hitting him. So if i were to apply this to heroin I would just take the cimetidine right when I feel the effects of heroin.. which is right away/5 minutes after I take it.

has anyone tried this and had it work for them? 800mg sounds like a lot of cimetidine to be taking.. especially if it might cause liver toxicity
 
Well, heroin is morphine once metabolised, so yes, cimetidine will inhibit the 2D6 enzyme that metabolises morphine. You dont take it after though, you take it before. It makes no sense taking it after! :)
 
What would be a good potentiator for oxymorphone? Would grapefruit juice and cimetidine work?
 
Whats everyones thoughts on using other opiates while using suboxone and subutex containing bupe. I know having opiates in ya systems before having sub's while send u into the worst rapid withdrawals. But what if you take the other opiates after the bupe? Some users were telling me it works. I was like you use H and bupe all the time? i was confused some opiate treatment drug that is.
Well i been using small dose's of sub's to help with my benzo detox and tapering plan to manage pain. Also to avoid using massive amounts of codeine, DHC, oxys etc. and getting another opiate habit.
Tonight i going to try to use some DHC and codeine after having 8mg of bupe last night. See how i go
What do people use or know potentates bupe?
 
My question is concerning Carisoprodal (brand name Soma). When should i take it in relation to my methadone dosage and how much should i take. Would it be similar to taking a benzo with methadone i.e. take it at roughly the same time as your methadone?
Another issue i was wondering about, is Diazapam THE benzo to take with methadone or will other similar benzos, or shorter acting ones like Lorazapam or Alprazolam have a similar effect? I read that Diazapam is the benzo that has most affinity with methadone. How much of it do others in a similar position take it?
Finally, i've asked very similar questions about Cat's Claw beforehand but when and how much of it should i take to potentiate meth? Do you need to take it beforehand like Cimetidine, and if so is it worth taking some more afterwards as well? Does anyone know how long it takes to work?
 
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