Opioids Loperamide (Immodium) Megathread: We have now lost at least 2 of our own from Lope

well

well i am not really using loperamide as a potentiator more trying to get an effect solely form that. i am not trying to potentiate4 the lope per say more allowing it to cross my BBB by inhibiting the enzyms that would prevent it form pasing. or at least allowing enough of the drug to pass throught to notice effcts. i am also going to drink GF juice for any toerh possible potentiation/. when i am doen the experminet i will let you guys know how it goes.

^This topic regarding Loperamide and getting it to cross the BBB via Glycoprotein Inhibitors and Nanoparticles etc. has been dicussed quite a bit before. You might try doing a search with some of those keywords and see what comes up, and perhaps check out the thread Malfunkshun made famous;(and caught hell for!) I think it is titled something like "One Last Word About Getting High w/Immodium."

ive read all he threads regarding loperamide. and yes malfunctions several threads on it. results have been mixed. some say a large dose will get u high, others say a large dose will jsut not let u shit until lsd becomes an OTC chemical. some claim with grapefruit juice and a protein inhibitor it works. as far as nanoparticles go hey haev onyl been demostrated in a very clinical scentific setting. reserch on protein inhiition and getting high is much mre reasonable for someone in my postion to do.AS of right now i ahve taken 200mg qunine sulfate and GFJ and 16mg lope. i took the inhibiotrs an hor or so previous to the lope. dk exactly how long the lope is in my system and thier are no discernable effetcs yet. i only did this to first hand see if it works or not.

ok it didnt work. i wont doubt the validity of the OP's expiriences jsut saying for me personally it didnt do anyting. i have no opiate toelrance btw.

Blasphemous Confessions of an Other Drug's Moderator

Ok, I know the commonly accepted verdict on this whole fiasco is that loperamide does not cross the blood brain barrier (BBB) thus no central nervous system (CNS) activity thus no high.

Well, I am here to say, something doesn't sit right.

I know I'm probably putting what little respect and credibility I have on the line right now, but I don't care. If this can help anyone in who finds themselves in my current situation, then I feel I should share.

For the last week, I have been aiding my Suboxone withdrawals with Loperamide (Imodium brand). The first day, I stuck to your typical, box-suggested doses. All it did was keep me from shitting.

The next day, I upped the dose by about 50mg, for a grand total of 60mg.

An hour later, the first hints of, we will call it, "opiate like intoxication," became noticeable. By this, I mean dry, tired, scratchy eyes. Lowered blood pressure. Relaxed breathing. Reduced anxiety. And best of all, the most wonderful and beneficial aspect of high-dose Loperamide, reduced (read: completely gone) joint pain and the stopping of the "skin crawls."

It's wonderful. I went into this experiment thinking, "Ok, I'm about to waste 12 dollars, but I'm intrigued enough to try." I came out of the experiment thinking "I'm going to do this again."

Why this happens? I do not know, but there has to be some CNS activity. My theory is that Loperamide is not COMPLETELY blocked by the BBB. There has to be a small amount that can make it through, thus CNS activity in high doses. The higher the dose, the more that gets through.

I have made it a week now without Suboxone, heroin, methadone, any opiate at all, besides Loperamide. It works wonders for the reduction/elimination of withdrawal symptoms. I can't say that it's getting me high, but to someone in withdrawals, feeling normal is a high in-and-of itself.

So, if you are withdrawing and can't get any other drug for relief, or if you don't want another drug (to get fully clean), then pick up some Loperamide. I've been taking anywhere from 40 - 60mg every other day and it's great.

Nobody with half a brain should lose respect for you for that post

panacea said:

nobody with half a brain should lose respect for you for that post

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^+1 qft

^^^Perhaps now people will take this topic a bit more seriously. Malfunkshun would be proud.

Loperamide has helped me through withdrawals several times, but its effects are primarily on the opioid receptors outside of the brain. I suspect people could be misinterpreting the body high and think its an actual high...

I can't remember where I heard it, but I thought that it could cross the actual barrier but was nearly instantaneously pumped out by something. If that's the case then I could see how massive amounts could overwhelm that mechanism.

Nanoparticles will do the trick too.

^ That's what I'm thinking, is that the higher the dose, the more that gets through.

I am aware that what I feel is not a typical, old fashioned opiate high. It's far from it. But, there are a lot of familiar symptoms of an opiate high that make it a valuable drug for withdrawal relief. It completely eliminates every symptom of withdrawal.

I found an old post of mine on the issue-

Loperaminde along with Cereport, which increases permeability of the BBB, has been shown to produce clear analgesic effects.

I also have heard p-glycoprotein inhibitors get it across the BBB more effectively.

The other option is delivery of loperamide with polysorbate-80 coated nanoparticles.


Edit- If someone had a natural problem with P-gp that could lead to effects.

Edit 2- Cereport is promising: http://cat.inist.fr/?aModele=afficheN&cpsidt=2341264

What is Cereport? I'm going to Google it, but if you have any info, that'd be cool too. I'm checking that link out as well.

EDIT - Just read your link. VERY interesting. I can't wait to see the onslaught of questions on how Cereport can be obtained.

well to tell the truth i think msot of the people getting something out of it is for withdrawll. im yet to hear someone who isnt withdrawling feeling anything very significant from it. like i dont think any amount will get you an opite high compared to 15mg oxycodone or equivalncy. but then again that does ot prove that it is not active. mroe people should try this and report.

Cereport is a bradykinin B2 receptor agonist, it increases permeability of the BBB and it's used as an adjunct to make chemotherapy more effective; administered intravenously, in the hospital. That kinda dashes hopes. The only way you're getting that drug is to be an oncologist or synthesize it yourself.

mr.dopeman said:

well to tell the truth i think msot of the people getting something out of it is for withdrawll. im yet to hear someone who isnt withdrawling feeling anything very significant from it. like i dont think any amount will get you an opite high compared to 15mg oxycodone or equivalncy. but then again that does ot prove that it is not active. mroe people should try this and report.

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I don't think anyone was saying anything different, so what's your point? The general consensus has always been that it's something to aid withdrawal, nothing more.

I agree it would be nice to know how it affects others not in withdrawal - specifically those who are not addicted/dependent upon any opiate - but I'm not going to ask anyone to try it. If some of it does in fact cross the BBB, someone could easily OD. Loperamide would be active in the CNS in microgram doses, so if the smallest amount cross, it could be dangerous, especially to non-tolerant/non-dependent users.

Could you please cite a source that indicates loperamide causes CNS effects at microgram doses? Because I don't see any reason why it would be thousands of times more potent at the central opioid receptors than the peripheral ones. It's more potent than, say, oxycodone, but it's active in the single milligram range, not microgram. Similar to hydromorphone's dosing.


Could someone with access to a university network please send me the paper on this;

Central analgesic actions of loperamide following transient permeation of the blood brain barrier with Cereport (RMP-7). Brain Research, 1998 Aug 10;801(1-2):259-66.

sixpartseven said:

Just give up. Its the fucking rules and they arent going to change no matter how many little loop-holes you try to find in them. If you dont like the rules here, then stop posting here, no one is forcing you to.

And the reason we can discuss this topic (getting high off loperamide) is because this website is based on gathering and sharing information for safe(er) drug use. Its better we discuss this and learn everything we possibly can about it so that if someone decides to try and get high off it they have all the information they need to stay safe as possible.

Discussing this and discussing sources are two different things and its ridiculous to try and compare the two. Were here to keep you safer, not to "hook you up."

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he does have a point though. Discussing ordering pods is not illegal only. The only reason I could see it violating the rules is if you establish your intent by saying you plan to consume then. if you intent is for flower arragment as that is what pods are sold for then there is nothing illegal about it.

^ True, but then we could allow all sorts of things on the basis that they have 'innocent' uses; GBL to clean your CDs, amyl nitrite to clean your video heads, hell what about cocaine to use as a local anesthetic?

We only allow sources for products that have a harm reduction value, e.g. needles, filters, 5-HTP supplements.

svacheme3 said:

Could you please cite a source that indicates loperamide causes CNS effects at microgram doses? Because I don't see any reason why it would be thousands of times more potent at the central opioid receptors than the peripheral ones. It's more potent than, say, oxycodone, but it's active in the single milligram range, not microgram. Similar to hydromorphone's dosing.


Could someone with access to a university network please send me the paper on this;

Central analgesic actions of loperamide following transient permeation of the blood brain barrier with Cereport (RMP-7). Brain Research, 1998 Aug 10;801(1-2):259-66.

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I'm looking for a source now, but I thought it was pretty much well established fact that it is at least as potent as Fentanyl, which we all should know, is active in microgram doses.

i'm very jealous of the people who get 'mad high' from loperamide...

i have a bottle just sitting there...its so depressing. maybe one day i will master alchemy and render immodium equal to opium.