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Bupe Suboxone/cimetidine money saving tip

garuda

Bluelighter
Joined
Feb 2, 2007
Messages
1,475
I never put much faith in opiate/opioid potentiation with cimetidine, the few times I tried it with hydrocodone and morphine with negligible effect if any.

But after trying it with suboxone I am a believer, it is an amazing potentiator of buprenorphine! It not only almost doubles the subjective feeling of a dose but also extends the effects. I took 1mg of suboxone sublingually yesterday at 6pm and its now 10:30am and I am still feeling it strongly, and last night I slept like a baby when usually I suffer from insomnia. Without using cimetidine 2mg of suboxone will barely hold me and keep me well, I certainly would not be feeling it the next day.

My dosing schedule is:

1 hour before taking the sub I dose 600mg of cimetidine, then dose the sub, and then every 6 hours afterward I dose 400mg of cimetidine until I can no longer feel the sub which is usually sometime after the 24 hour mark. I still am well at this point I just no longer conciously feel the sub.

This is a big money saver with the cost of suboxone, as you can get 50 tablets of generic 200mg cimetidine OTC for under 5 dollars. Even if you have tried cimetidine before with other opiates/opioids give it a try with sub, you might be like me and able to get double the mileage out of your sub.

It appears cimetidine does have some potential side effects:

http://www.drugs.com/mtm/cimetidine.html

FWIW I have personally never experienced any side effects from cimetidine, but do be careful.
 
this doesn't make a whole lot of sense since the action of cimetidine is its effect on certain enzymes in your stomach. since buprenorphine is not absorbed through your stomach, i don't believe cimetidine would have any effect on it. maybe somebody could care to explain. garuda, is it possible this is just placebo or what? your experience is good news, but you have no explanation of how it could work. what is your MOA?
 
Sorry I should have covered that, it has to do with inhibiting liver enzymes that metabolize the buprenorphine, in addition to reducing stomach acid cimetidine is a cytochrome CYP3 A4 enzyme inhibitor. It has nothing to do with the stomach, you're inhibiting the enzyme that breaks down bupe in your liver.

White grapefruit juice contains a chemical that has a similar effect, I just find it cheaper and more convenient to use cimetidine instead of constantly drinking vast amounts of WGFJ.

Here is the wikipedia page you can see the table where they list inhibitors and inducers, you want to avoid the inducers.

http://en.wikipedia.org/wiki/CYP3A4

Cimetidine, white grapefruit juice, and quercetin(OTC supplement) are the easiest to find of the inhibitors and also the safest.

EDIT: From wikipedia again:
http://en.wikipedia.org/wiki/Buprenorphine
Buprenorphine is metabolised by the liver, via the CYP3A4 isozyme of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation) and other metabolites. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20–73 hours (mean 37). Due to the mainly hepatic elimination there is no risk of accumulation in patients with renal impairment and in the elderly.

So inhibit the enzyme and you slow down the metabolization of buprenorphine, leaving more in your bloodstream and for longer.
 
that's what i got mixed up. i was thinking it had to do with your stomach, when in fact it's your liver that the enzymes are inhibited in.
 
But isn't norbupe a stronger mu agonist? I've thought about this before, but never done it, I always thought I would want my body to convert the bupe to norbupe.

Perhaps I'll give this a try soon. Actually, there's no point, because I'm not going to feel anything either way; I take sub for maintenance, and feel nothing from it. The only way this would do anything good for me (personally) would be if it enabled me to dose lower, because my insurance doesn't cover the pills, so if I could dose lower I could save a little money.

I'll try to find some stats on the differences between bupe and norbupe, but I'm pretty sure norbupe is a stronger mu agonist, so it seems like you would want it metabolized. Hell, you might even want to induce CYP3A4...
 
johanneschimpo said:
But isn't norbupe a stronger mu agonist? I've thought about this before, but never done it, I always thought I would want my body to convert the bupe to norbupe.

Perhaps I'll give this a try soon. Actually, there's no point, because I'm not going to feel anything either way; I take sub for maintenance, and feel nothing from it. The only way this would do anything good for me (personally) would be if it enabled me to dose lower, because my insurance doesn't cover the pills, so if I could dose lower I could save a little money.

I'll try to find some stats on the differences between bupe and norbupe, but I'm pretty sure norbupe is a stronger mu agonist, so it seems like you would want it metabolized. Hell, you might even want to induce CYP3A4...

According to wikipedia:

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

The main active metabolite, norbuprenorphine, is a δ-opioid receptor and ORL1 receptor agonist, μ- and κ-opioid receptor partial agonist, but buprenorphine antagonizes its effects.[6]

Personally I might have some reservations about taking that much cimetidine day in and day out for maintenance, you could also look into quercetin and bergamottin but they might be more expensive then cimetidine.

I know its subjective experience, but it really works for me. The first time I took 2mg with cimetidine I nodded for the first time off of suboxone. After that I reduced the dose to 1mg.

And like I said with hydrocodone and morphine I really noticed no significant potentiation so I was surprised.
 
Ah I see. So even if norbupe is a stronger, or full, mu agonist (which I'm 99% sure it is), it doesn't matter because bupe is going to compete for the receptors (and win).
Interesting... makes me want to dealkylate it in some way and see what its like on its own. Anyone got a liver I can borrow?
 
make that two livers?

Benadryl and Benzos are good too. (I know, groundbreaking information, thank me later)
 
wow, this is good news. i stopped shooting subutex a long time ago, but i do snort it occasionally for pain.
IME, cimetadine HAS helped with my oxy use- always made the high more intense and last longer.
but thanks garuda, i'll give this a try next time i decide to use sub.
 
This is something i will definately try SOON. In the past month I went from 6-2 mg a day depening, but if this works I will report back because i know the penny pinching of suboxone maitinence therapy. I wish there is a generic, when is the patent up? If this works I will report back.

Good to see you sent me a message Inherownwrite, I hope everything is doing well (for you) and I will see you sometime in the near future hopefully. Muah
 
How do you dose your sub, garuda? Sublingually?

This is very interesting, I would have thought the cimetidine would just extend the half life rather then potentiate.

Any ideas on the reason for this? Something to do with the metabolites of the drug itself maybe?
 
someone who takes suboxone every day for maintenance please try this and see if you catch a buzz off your regular dose...i gotta know if it works8)
 
I take 4mg a day for maintenance. If I decide to go crazy and take a big dose, like 24mg, it doesn't do a damn thing to me. So I can say that for me, this wouldn't do anything. It might make it better therapeutically though - either by letting me take a lower dose (say 3mg), or by extending how long it lasts having to dose less often. I don't expect it to make any noticeable difference for me (I'm only talking about for me, I don't know about others).

I'm on sub maintenance, and it won't get me high no matter how much I take.
 
^i started on 12mg and have been on 8mg for almost a year. I take cimetidine every now and then (it's VERY COSTLY where I live...at least the stores I've seen it in...only tagamet)...but it definately boosts the high and the duration of sublingual bupe.. I def dont get high either as i'm on BMT...but every now and then i get a random decent nod from bupe...and the cimetidine has USUALLLY seemed to be the factor. Definately not worth paying almost $15 for 30 200mg pills of cimetidine though. (yeah it sucks in my area...maybe i'm just not looking hard enough...then again I could care less as I'm getting off bupe on my own soon enough...already started to titrate)
 
bupe is weird i have been on suboxone for 16months and even when u do get high from it its speedy like no opiate ever i cant sit still i look like a crack head lol but in my area its xpensive to man i dont know why there no generic form of it
 
bupe is weird i have been on suboxone for 16months and even when u do get high from it its speedy like no opiate ever i cant sit still i look like a crack head lol but in my area its xpensive to man i dont know why there no generic form of it

There's no generic form of it because the patent hasn't expired yet (I think). Or maybe the patent recently expired or will this year; either way, once that happens, unless the patent is renewed, there will be a generic form. May I suggest the journal for posts like this in the future though? Welcome to BL man! (or woman!)
 
back from the dead

Sorry to bring the post back from the dead, but I am interested in minimizing the amount of costly subutex I use so:

Whats general consensus about bupe + cimetidine?

Does it work as a potentiator or not?


stay safe
 
White grapefruit juice contains a chemical that has a similar effect, I just find it cheaper and more convenient to use cimetidine instead of constantly drinking vast amounts of WGFJ.

I find it does help with lengthening buprenorphine, but I get a better potentiation out of benzos such as valium or xanax when it comes to WGFJ. I love a glass of WGFJ, I need to buy some more.

I can completely understand how you see it more convenient and feasible than drinking a lot of grapefruit juice.

^ Not everything on the above webpage is incorrect, but some of it most certainly is. I wouldn't trust wiki as a source TBH ^

But, I do admit that wiki is right about the cytochrome P450 enzyme CYP3A4. That part isn't wrong, just other parts of wiki's page on buprenorphine.
 
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