Questions regarding Loperamide

[lespaulpower]

I need some info regarding loperamide. For anyone who doesn't know, it's the active ingredient in OTC diarrhea meds such as 'Immodium AD'.

It's a synthetic opioid agonist but only works on receptors in the Large intestines. It does not cross the blood brain barrier and has no psychoactive properties.

I've read however, that when loperamide particles are coated with 'polysorbate 80' and injected, the drug DOES cross the barrier.

Does anyone know about this process? If one were to do this, would it be a practical process? Any info is appreciated.

Also, I hear alot of talk here about the value of loperamide for helping withrawals. Obviously, It would be effective at alleviating the diarrhea and GI problems, but how about any others? In LARGE doses, could it be effective at easing other symptoms (Restless limbs, aches/pains, emotional distress, chills)???

Thanks.

LP

[StinkyPickle]

Someone on this board was convinced you could get fucked up from Immodium if you ate like 2 grams of the shit. Would be more expensive than scoring a bag. UTSE, it shouldn't be too hard to find it.

[Indy]

Man does THIS take me back....way before i even JOINED, there were discussions about this, and also acetylating loperamide to make it cross the BBB more effectively.

IMO, if you take a shitload of loperamide (like 10-20 pills at once) in withdrawal, you'll get relief from some of the physical symptoms. I'm not sure exactly how it works, but it's definitely MORE than just relieving the GI symptoms. I'm guessing if you just bombard your blood with it, SOME of it has to make it through? Not sure.

There was a guy on bluelight who claimed to take a couple hundred mgs of loperamide and stay slightly more than just well, nobody bought his story on BL, but i dunno, in theory it MIGHT work.

As for the polysorbate nanoparticles, I never did figure out what the process was, but i'm pretty sure you need a lab and some chem experience. Hm, this was before Mayo joined, i should ask him his opinion.

[lespaulpower]

Yeah, thank you guys for the replies thus far. Just for the record, and to avoid getting flamed, I am NOT trying to get high from Immodium. I could just score some dones for that (plus Im on suboxone already). But I came across some info on Wikipedia and It really made me curious. Maybe back in my desperate/sick days this could've been something to try.

[hovadagod]

You WILL NOT be flamed for trying to get high from immodium. That is a common past-time around here.

[Indy]

Imagine if it were as easy as boiling loperamide with vinegar to get it to cross the blood-brain barrier. I have to confess, i fantasize about this at times.....basically it'd be like, whatever dose constipated you, would be like any other opioid dose that constipated you the same amount, actually going into your brain. Unfortunately it's not that simple, though i don't remember if paregoric kid ever did do his experiment with acetic anhydride to acetylate loperamide. IIRC the molecule lends itself to acetylation, and acetylation tends to make things cross the BBB better (i'm not a chem buff, so correct me if i'm wrong), so maybe it COULD work.

the only caveat, was that i think the structure of loperamide was similar to that MPTP stuff or whatever it was called, so possibly doing a bad acetylation could have really nasty permanent effects....not worth it until more is known IMO.

[pinn3d]

If I recall correctly, loperamide DOES cross the blood-brain barrier, but it just does so very poorly, so to get an effect you have to take A LOT... and so of course with that will most likely be severe constipation....

I dunno about you, but i HATE constipation... nothin worse than feelin like you need to take a huge crap, and nothin comes out..... can't stand it.... so if you are gonna try takin loads of loperamide, maybe eat a pound of prunes along with it..... and you'll probably wanna order generic loperamide off the internet in bulk to save cash.....

And apparently loperamide coated w/ polysorbate 80 will act like a regular opioid when injected... and you CAN apparently buy polysorbate 80 online...

**If your gonna inject that mixture BE CAREFUL, and research first to find the right dose**


Check out these links...


http://www.bluelight.ru/vb/showthread.php?t=376600

http://www.bluelight.ru/vb/archive/index.php/t-299226.html


PS-- I hope informational links to other forums are OK--- I read the rules here and didn't find anything about them...

[scikid]

All I know is it works great for GI related opiate withdrawl. Maybe makes the cravings a little milder but I haven't ever taken more then 8 milligrams.

[Indy]

If I recall correctly, loperamide DOES cross the blood-brain barrier, but it just does so very poorly, so to get an effect you have to take A LOT... and so of course with that will most likely be severe constipation....

I dunno about you, but i HATE constipation... nothin worse than feelin like you need to take a huge crap, and nothin comes out..... can't stand it.... so if you are gonna try takin loads of loperamide, maybe eat a pound of prunes along with it..... and you'll probably wanna order generic loperamide off the internet in bulk to save cash.....

And apparently loperamide coated w/ polysorbate 80 will act like a regular opioid when injected... and you CAN apparently buy polysorbate 80 online...

**If your gonna inject that mixture BE CAREFUL, and research first to find the right dose**


Check out these links...


http://www.bluelight.ru/vb/showthread.php?t=376600

http://www.bluelight.ru/vb/archive/index.php/t-299226.html


PS-- I hope informational links to other forums are OK--- I read the rules here and didn't find anything about them...


The problem is that you don't just mix the polysorbate 80 and the loperamide, you have to create nanoparticles of the loperamide, where each individual particle is coated by the polysorbate 80, and i'm not sure how to do that, but it sure as hell doesn't sound easy.

[upstate_007]

and i'm not sure how to do that, but it sure as hell doesn't sound easy.

Lasers and styrofoam.


I have no idea. I just like lasers.

[Mayo]

All I can say is there are a few ways to get loperamide and acetyl derivatives across the BBB, but boiling with vinegar is not one of them.
Yes loperamide can be acetylated, and taken with a protein pump inhibitor to increase duration, but I wouldn't do it.

The other safe methods are completely impractical without lots of equipment and knowledge,
like incorporation into polyacrylate nanoparticals then coating with a polysorbate.
Tedious, time consuming, and lots of equipment. Who's gonna do all that?

Mixing loperamide and Tween 80 and injecting it would be crazy IMO, and I can't be any part of that.
I'd suggest shooting 'done syrup first (don't do that).

I think robo is probably busy, maybe resorcinol would like to discuss this, as it is a purely theoretical and completely impractical topic.
But I think he likes to talk about all things chem/pharma - related..idk?

sorry, just not my thing anymore. (I'm lazy without my DOC ;))

[erica]

Yes, I did some research on this a while back, and if done correctly (and IV'd), it will cross the blood barrier. However, you need to order the polysorbate-80 online from a chemical supply place, in large quantities, and that is quite expensive. You also need to do it correctly, and for this, you will need an extensive knowledge of chemistry. Spend some time on Google, and you'll find it. But like I said, you'll basically need the equivalent of a degree in chem to be able to do it correctly.

As for loperamide alone, when I have REALLY bad WDs, I take about 25 of them at a time, and it helps immensely. Fuck the constipation, when you're that sick, you don't care. It helps with the RLS, cold sweats, chills, all that stuff.

[Synack]

avoid the pills if you take alot (30mg in my experiment), the coating gives you wicked stomach aches & cramps.... try to find a syrup.

[roxi*stardust]

Use the search engine, there are a ton of threads on making Lopermide more efficient. Back in the day when I would run out of pills early I would take 8-10 Lopermide tabs and get some pretty good releif from w/d.

[pinn3d]

The problem is that you don't just mix the polysorbate 80 and the loperamide, you have to create nanoparticles of the loperamide, where each individual particle is coated by the polysorbate 80, and i'm not sure how to do that, but it sure as hell doesn't sound easy.
Yeah---- I have NO IDEA how anyone would go about making the correct mixture of polysorbate 80 and loperamide actually injectable--- so please do not try this unless you find the right info, and are SURE you know what you are doing.....

[Mayo]

Right. You cant just mix a polysorbate and crushed up tabs or syrup, it must be a pure form of loperamide.
It doesn't need to be in nanopartical form, but if not it would be immediately pumped out of the brain giving a likely half-life of minutes,
requiring the use of some type of efflux pump inhibitor.
Overall, it is not a difficult thing to do, simply the formation of a normal phase micelle.
I just don't know how safe it would be, so can't provide some how-to guide
(which I wouldn't do anyway as this is not a harm reduction issue IMO).

Incorporation of loperamide into a poly(alkyl cyanoacrylate) nanopartical structure is not exceedingly difficult either,
but requires very specific knowledge of the process. But that would be the easy part anyway.
The product must then be purified, sterilized, and coated with a polysorbate 80 of the highest purity.
That is where this idea becomes completely impractical.
I have a chem degree and would not even remotely consider this as a viable option to deal with opiate withdrawal,
or for recreational use. (Pod tea anyone?)


The problem is that you don't just mix the polysorbate 80 and the loperamide, you have to create nanoparticles of the loperamide, where each individual particle is coated by the polysorbate 80, and i'm not sure how to do that, but it sure as hell doesn't sound easy.


Yeah---- I have NO IDEA how anyone would go about making the correct mixture of polysorbate 80 and loperamide actually injectable--- so please do not try this unless you find the right info, and are SURE you know what you are doing.....

[Synack]

I believe this article tells you a method used to coat loperamide

SpringerLinkJournal Pharmaceutical Research
Publisher Springer Netherlands
ISSN 0724-8741 (Print) 1573-904X (Online)
Issue Volume 14, Number 3 / March, 1997
DOI 10.1023/A:1012098005098
Pages 325-328
Subject Collection Biomedical and Life Sciences
SpringerLink Date Tuesday, November 30, 2004
Delivery of Loperamide Across the Blood-Brain Barrier with Polysorbate 80-Coated Polybutylcyanoacrylate Nanoparticles

[Narkotikon]

I've taken up to about 20 2mg pills of Immodium / loperamide before, but it didn't do anything other than constipate me. I can't imagine taking 2 grams of the stuff. I'd think that would scream "fecal impaction." God, can you imagine having to go to the ER for a fecal impaction and having to say "yeah, it's because I ate 2 grams of Immodium" then having to explain WHY you did that?

I think it works for some in w/d, and for others it doesn't. I guess it wouldn't hurt to give it a try, but just don't get too carried away with it.

I've heard about the Polysorbate 80 thing too, and something else about using quinidine or something like that. I have no idea how you'd go about doing it though.

[MindAsh]

just be careful, high doses of lope have been known to cause fatal paralysis that i once began to exp after injesting 2 bottles containing 48 2mg lopes. not a pleasant experience at all tho it did kill my sickness.

[I'm-Nod-Addicted]

just be careful, high doses of lope have been known to cause fatal paralysis that i once began to exp after injesting 2 bottles containing 48 2mg lopes. not a pleasant experience at all tho it did kill my sickness.


So eating 96 pills might be a dangerous thing to attempt?

[Thanat0s]

...high doses of lope have been known to cause fatal paralysis...

known to who?

source?

...and this thread is 2years old goddamnit.

[Uncle Wiggly]

"high doses of lope have been known to cause fatal paralysis."

Hey MindAsh, this would most certainly be news to many of us. I tried searching for this, although not as thorough as possible, and came up with nothing. Please start a new thread, as opposed to rezing one that is two years-old, regarding this if you can provide a link.

Thanks. Say"Goodnight."