Loperamide?

[kneeco]

So as any opiate users who have access to great websites like this one, we have all researched what can make our DOC stronger and as for me I have raided the medicine cabinet one too many times (completely killed my monthly supply of xanax, promethazine, carisprodol, nyquil, and ativan) so I was looking for other ways to intense my opiate experience (I just moved way far away from my 'spot' to cop so I'm making plans on getting straight... or just lowering my tolerance by taking a small vacation:D)

Anywho, today I'm starting a taper [btw I'm a black tar IV user] and only going to use when I start to get sick and only small amounts and cut it down slowly yadda-yadda..

BUT!

I want to enjoy it too so I found a whole bottle of liquid loperamide in my bathroom and was going to chug some down here now (t- 1 hr till sickness sets in) and then dose and see if I feel anything, what I'm trying to contribute to here is to hopefully bring some clarity and truth to the loperamide potentiator myth/story cause I sure as hell can't seem to find any solid information on it, if anyone objects to this plan please tell me of my mistake, everyone have an apathetic day!

[starglazer33]

Good luck, and welcome.


Sg33

[roxi*stardust]

Only thing I know that Lopermide will potentiate for sure is constipation.

[RxQueen]

heheheh, yeah... there's lots of info around this place about that particular side effect from opiates. if it's one that has ever bothered you before, using loperamide to potentiate will pretty much guarantee that you don't shit at all for a few days. i'd try benadryl or one of those types of antihistamines before loperamide. or of course, good ol' tagamet.

[kneeco]

good ol' tagamet.

what is this tagamet and where does one find it? is it otc?

and the constipation thing.. i don't mind really anyway i dont shit for days/weeks anyway cause im either too busy trying to score or being numbed up :cool:

and two hours into it, nothings different... waste of time to make shit potent.. for me at least, at least the ten bag i had was FAT [weird huh how when i plan on it being my last balloon for a while]

[paroxetina]

Loperimide (immodium) is not going to potentiate the high. It will help with diarrhea from withdrawals but that is it, as roxi*stardust said. one dose of that stuff and I dont shit for like 5 days - be careful how much you take unless you want some bad fecal impaction.

[RxQueen]

what is this tagamet and where does one find it? is it otc?

and the constipation thing.. i don't mind really anyway i dont shit for days/weeks anyway cause im either too busy trying to score or being numbed up :cool:

and two hours into it, nothings different... waste of time to make shit potent.. for me at least, at least the ten bag i had was FAT [weird huh how when i plan on it being my last balloon for a while]

tagamet is an OTC antacid/heartburn med (generic name: cimetidine). i'm not certain anymore, but i think what it does is to inhibit the enzymes in your gut that break down opiates (morphine-based ones in particular, i think), allowing more of it to be absorbed into your system. is that right, guys? it's really late in my day (stupid night schedule...).... anyone? roxi?

anyway it helps some for me, and others here swear by it. also white grapefruit juice has some enzyme-inhibiting action as well. drink a bunch about 30-40 minutes before you dose.

and i'm glad that the constipation thing isn't a bother for you. just be careful, cuz if you stay backed up for too long, no matter who you are, it WILL eventually cause a painful impaction that can seriously threaten your health. just go read jacky's "shitting out my mouth" thread for proof. you might wanna be sure to read it on an empty stomach though.... fair warning. :cool:

[Indy]

There's a lot of experience that says loperamide potentiates opiates. WHY exactly isn't known because not many people publish studies on ways to get high for cheaper. My guess would be that loperamide is metabolized by many of the same enzymes in the liver as the "real" opiates, and if there's a bunch of loperamide in your system, there will be less enzyme concentration to metabolize the "real" opiates, thus they stay in your body longer before being destroyed; thus you get higher and stay higher for longer.

[DCBA]

There's a lot of experience that says loperamide potentiates opiates. WHY exactly isn't known because not many people publish studies on ways to get high for cheaper.

Loperamide potentiates opiates because it binds to the opiate receptor in the gut and spinal chord, it is a powerful mu agonist in there.
So what will happend when your using loperamide before the opiate that you normally use?
Because the opiates you normally do ALSO bind to the opiate receptors in the gut and spinal chord, if you use loperamide before it will happen that loperamide is ALLREADY BOND to the opiate receptors in the gut and spinal chord, THAT LEAVES MORE of your opiate FREE FOR acting in the brain and not in the gut or spinal chord.

Loperamide potentiates because it causes other opiates to be free from the receptors in the gut and spinal chord and that leads to more opiate in the brain...

Easy to understand..

[havok]

I don't think loperamide poteniates other opiates. The only reason to take loperamide is if you are in withdrawals. It helps alot for that. The worst part of withdrawals for me is the stomach pain and constant diarrhea. Loperamide gets rid of all my stomach pain. It is the best over the counter medication you can take when you are in withdrawals.

Loperamide is a full opiate agonist, but it can not cross the blood-brain barrier and therefore it doesnt effect the central nervous system (you don't get high). It does however bind to all the other mu-opioid receptors in the body (like the ones in your stomach). In very high doses it gives somewhat of a body high, and I have heard that small amounts of it cross over into your brain.

[HistoryofMadness]

forget about it.

[reddragon3668]

Loperamide works pretty good to help counter withdrawals, but I have never heard of it being used to potentiate. Both Indy's and DCBA's explanation makes sense to me. I may actually give it a try. Its a fairly safe substance...I do not think its possible to OD on it. When fighting withdrawals, I've taken 20-30mg of the shit and its never bothered me.

As for it stopping you up, I have often wondered if it would do that to a opiate tolerant person. I mean, I take opiates that are many many times more powerful than loperamide. If they don't stop me up, then why would loperamide? I know that it targets the receptors in the body and not the brain, but still, doesn't tar or Opana or Morphine bind to those same receptors? I've been battling diarrhea now since the 23rd of February, but even when I take 30mg in a day, it only slows down my bowels a little bit, but definitely doesn't constipate me.

To the OP, thanks for bringing this up. I've not tried loperamide to potentiate but I am going to give it a try. One thing that I know for sure that works, however, is DXM. It not only potentiates at lower dosages... around 30-60mg, but it also helps lower tolerance. I've been using it now for a couple of weeks to taper, in preparation for a kick that I knew was coming. The DXM made the taper more manageable and I was able to kick with less discomfort than expected. So, I highly recommend using it while you taper. There are a good number of products out there with DXM as an ingredient, but not that many that have it as the sole ingredient (at least, that I can find), which is what you want. Of the available products that meet that criteria, I found Robitussin Cough Gels to be the cheapest. You can get them at Walmart for a little over 3 bucks. Each gel cap contains 15mg of DXM.

Good luck on your taper. I hope that you are able to find something that will help ease the discomfort. Also, I started writing this reply 5-6 hours ago, so I apologize if any of this is redundant. I got distracted and just got back to it.

[resorcinol]

Loperamide potentiates opiates because it binds to the opiate receptor in the gut and spinal chord, it is a powerful mu agonist in there.
So what will happend when your using loperamide before the opiate that you normally use?
Because the opiates you normally do ALSO bind to the opiate receptors in the gut and spinal chord, if you use loperamide before it will happen that loperamide is ALLREADY BOND to the opiate receptors in the gut and spinal chord, THAT LEAVES MORE of your opiate FREE FOR acting in the brain and not in the gut or spinal chord.

Loperamide potentiates because it causes other opiates to be free from the receptors in the gut and spinal chord and that leads to more opiate in the brain...

Easy to understand..

Man I wish it worked that way, but it just doesn't.

How many u-opioid receptors are bound is dependent on the concentration of the active opioid in your serum and the equilibrium constant for the coordination chemical reaction that binds (or unbinds) the opiate to the u receptor. Since taking loperamide doesn't change the concentration of the drug you want to potentiate, including in the brain where no loperamide can enter to create any DIRECT additive effect, (at least not to any appreciable degree), it won't get you any higher. If loperamide was a strong inhibitor of cytochrome enzymes it would potentiate, but that has nothing to do with the mechanism you proposed AND i don't think loperamide has much effect on cytochrome enzymes.

Sucks, I know.

It will help w/d to some degree though... not the mental symptoms though, which are the worst, so don't expect a miracle.

[Papa Verine]

Man I wish it worked that way, but it just doesn't.

How many u-opioid receptors are bound is dependent on the concentration of the active opioid in your serum and the equilibrium constant for the coordination chemical reaction that binds (or unbinds) the opiate to the u receptor. Since taking loperamide doesn't change the concentration of the drug you want to potentiate, including in the brain where no loperamide can enter to create any DIRECT additive effect, (at least not to any appreciable degree), it won't get you any higher. If loperamide was a strong inhibitor of cytochrome enzymes it would potentiate, but that has nothing to do with the mechanism you proposed AND i don't think loperamide has much effect on cytochrome enzymes.

Sucks, I know.

It will help w/d to some degree though... not the mental symptoms though, which are the worst, so don't expect a miracle.

It didn't sound right to me either. Thanks for clearing that up Resorcinol, you're one smart mother-fucker. I always look forward to reading your posts.

[scikid]

Lope does work great for WDs IMO

[DCBA]

Since taking loperamide doesn't change the concentration of the drug you want to potentiate, including in the brain where no loperamide can enter to create any DIRECT additive effect, (at least not to any appreciable degree), it won't get you any higher.


But using loperamide will make other opiates free from the receptors that loperamide does work (in the gut and spinal chord), and by freeing them they will be available to work in the brain receptors where loperamide won't enter.

Example: imagine you took OC orally and loperamide before, more OC will enter the brain because less OC will enter the gut receptors because they were beeing ocupied by loperamide. If you are a person with lot of mu opiate receptors in the gut (like some of us are..) then it will be quite a difference.

[brimanic]

Originally Posted by DCBA http://forum.opiophile.org/images/gnome/buttons/viewpost.gif (http://forum.opiophile.org/showthread.php?p=268616#post268616)
Loperamide potentiates opiates because it binds to the opiate receptor in the gut and spinal chord, it is a powerful mu agonist in there.
So what will happend when your using loperamide before the opiate that you normally use?
Because the opiates you normally do ALSO bind to the opiate receptors in the gut and spinal chord, if you use loperamide before it will happen that loperamide is ALLREADY BOND to the opiate receptors in the gut and spinal chord, THAT LEAVES MORE of your opiate FREE FOR acting in the brain and not in the gut or spinal chord.

Loperamide potentiates because it causes other opiates to be free from the receptors in the gut and spinal chord and that leads to more opiate in the brain...

Easy to understand..

Man I wish it worked that way, but it just doesn't.

How many u-opioid receptors are bound is dependent on the concentration of the active opioid in your serum and the equilibrium constant for the coordination chemical reaction that binds (or unbinds) the opiate to the u receptor. Since taking loperamide doesn't change the concentration of the drug you want to potentiate, including in the brain where no loperamide can enter to create any DIRECT additive effect, (at least not to any appreciable degree), it won't get you any higher. If loperamide was a strong inhibitor of cytochrome enzymes it would potentiate, but that has nothing to do with the mechanism you proposed AND i don't think loperamide has much effect on cytochrome enzymes.

Sucks, I know.

It will help w/d to some degree though... not the mental symptoms though, which are the worst, so don't expect a miracle.

I don't think DCBA's description and your description are really in conflict with each other (ie. they can both be true without contradiction). You theorize basically that the number of u-opioid receptors that are bound in the brain is dependent on the bio-availability of the opiate. And that loperamide wont potentiate because the presence of loperamide in the system does not increase bio-availability of the opiate in the brain. However, if loperamide is binding to the non-brain portion in the CNS this will result in an increase in bio-availability of the opiate in the entire system including the brain. So, it seems that what you say is correct: that the number of u-opioid recepters bound in the brain is dependent on the bio-availability of the opiate. But as DCBA says essentially (I hope I am not putting words in your mouth, just trying to paraphrase what you said) the presence of loperamide in the system will result in an increase of the bio-availability of the opiate. In short, the 2 theories are completely compatible. Or resorcinol's theory is a direct result of DCBA's theory. Agree?

[DCBA]

But as DCBA says essentially (I hope I am not putting words in your mouth, just trying to paraphrase what you said) the presence of loperamide in the system will result in an increase of the bio-availability of the opiate. In short, the 2 theories are completely compatible.

Agreed.

[milkybarkid]

I don't think loperamide poteniates other opiates. The only reason to take loperamide is if you are in withdrawals. It helps alot for that. The worst part of withdrawals for me is the stomach pain and constant diarrhea. Loperamide gets rid of all my stomach pain. It is the best over the counter medication you can take when you are in withdrawals.

Loperamide is a full opiate agonist, but it can not cross the blood-brain barrier and therefore it doesnt effect the central nervous system (you don't get high). It does however bind to all the other mu-opioid receptors in the body (like the ones in your stomach). In very high doses it gives somewhat of a body high, and I have heard that small amounts of it cross over into your brain.



2 points:

1. As immodium is a full agonist then why not jst take codine or something to ease the withdrawl? If i understand properrly people tink that they can take immodium and still detox at the cold urkey rate... which isn;t so

2. Having detoxed - and i know because i've done this - don;t make the mistake of taking immodium for a coup;e of weeks or more... as it will preciptate withdrawl effects aggain


mbk

[WarmCyanide]

so i'm reading two diff things. cimetidine (Tagamet) is better potentiator than Immodium (Loperamide)??
??? not in regards to wd at all just potentiator. thanks. havent used potentiators in a long time.
off to brush up on white GFJ i guess. hope you can decipher this. glad thread is still here

[Ron-Doe]

Lope never gave me any pleasant effects I actually think it made me feel my shots less. Benzos r the only thing that seems 2 help me along.