One more word about getting high with loperamide (Immodium)

[rachamim]

Sorry if my info will be redundant because of having been offered by another poster but I cannot honestly fully read 240 posts and yet this subject needs to be discussed.

Loperamide is a great lesson ins what is and what is not an opioid. Structure is not what determines a substance's classification and indeed Loperamide is structured very nicely. The problem though, and I will not bore folks with the chemistry is the substance's inability, EVER, to cross the Blood to Brain Barrier (BBB) UNLESS directed DIRECTLY into a person's brain and noone in their right mind should ever even dream of it.

There have been trials with lower ordered primates that have had success with this direct injection, but who in the world will shove a horse needle through their brain? Not me and really, knowing how some are, I should not even have mentioned it. Never the less it is what it is.


Loperamide is useless aside as its prescribed usage, as an anti-diahhreal and perhaps in the plcebo department for Acute W/D but a thinking person will never have that option knowing the relevant info beforehand.

 

[chrlefxtrt]

I don't know anything about the chemistry behind the drugs I take, all I know is that they are effective.

This being said I must say that FOR ME loperamide worked. Everyone has a different body make up. My wife gets a decent buzz off of two darvocet. For me it takes a couple 10mg percocet when I have a low tolerance and 40mg when it has built up.

I was coming off of a mild perc binge where my tolerance at the end was 30mg or so to even feel anything. The withdrawls were extremely annoying so I tried loperamide. I will never again come off an opiate without the stuff handy. After taking 100mg I felt way better, and after about 150mg I felt "good". The effects also lasted well over 8hrs. It might not be practical, but I am going to go of a limb and say: someone wanting to get rid of the sweats and leg wiggles doesn't care about practical.

It is also cheap compared to other options. Instead of being miserable for three days why not just try loperamide? For me it was a lifesaver and I actually thought the buzz was decent.

For the record, I shit two days after taking 160mg of loperamide. With a balanced diet and lots of water of course. Just eat food that will counter the slolwing of the gi tract from th loperamide.

Just try it before passing judgement.

 

[djsim]

I don't know anything about the chemistry behind the drugs I take, all I know is that they are effective.

...
after about 150mg I felt "good". ...160mg of loperamide...

Just try it before passing judgement.

If you did understand the chemistry then there is no way you'd ever, ever consider taking 160mg(!!) to get this phantom "high"

 

[DopaMan]

Shor(er) read: Although there is a clear mechanism which loperamide is pumped out of the BBB via the Pgp pump/receptor, as stated before it has been shown in the literature that 16mg of loperamide co-administered with a single 600mg dose of quinidine caused respiratory depression in 8 healthy subjects (no history of BBB damaging diseases, kidney or hepatic damage. So I don't see why taking an extreme quantity and just inhibiting the Pgp via loperamide alone isn't deemed feasible. One important thing to consider is that this is just a single study in humans, but it appears to be done relatively well despite being so small (you'd be surprised how small some drug studies are - especially when a company is trying to prove their generics are equally as bioavailable as a brand name drug!). So Malfunkshun could just be lucky (low concentration/low quality of Pgp pumps in the BBB and/or poor metabolism of loperamide. OR he just has a lower tolerance than most and found the sweet spot where you fully inhibit the Pgp and manage to get just enough loperamide into the CNS!

I am not completely unconvinced that someone could possibly saturate the Pgp pumps in the BBB with loperamide and then have such an extremely high plasma dose that a miniscule amount may force through the BBB. Certain drugs you assume just do not absorb (such as most ionized drugs passing into tissues) but when the pH calculations are worked out you find that .003% gets through (although this is NOT what is going on with loperamide its an example of small amounts crossing seemingly impossible barriers because a very small amount remained unionized). It could be that Malfunkshun also poorly metabolizes loperamide (I'm not hip to loperamide metabolism, although I assume it’s hepatic) and his plasma levels are even higher than the average person consuming 200mg+ doses of loperamide.

Although I believe that inhibition of the Pgp via a more potent drug may be more effective and easier on the bowels, I do not see why this brute force method might not work, especially at very high doses such as 200mg.

Note: I once tried and failed to obtain a loperamide buzz when I first discovered the others attempts as well as the literature about the addition of quinidine. I used a an antibiotic that was purchased OTC at a pet store (lol) known for Pgp inhibition. I also consumed a smaller quantity of quantity of loperamide (20mg, maybe). My tolerance would have been moderate (40 to 60mg of oxycodone at the time to get off) so this probably played an effect in its failure. Or it is possible I was not effectively inhibiting the Pgp or it just didn't work.


Loperamide + quinidine study

AJ, Wandel C, He H, Shah S, Wood AJ. Increased drug delivery to the brain by P-glycoprotein inhibition. Clin Pharmacol Ther 2000 Sep; 6'8'(3):231-7

 

[emerald07]

I'd just be terrified I'd never go to the toilet again! I couldn't possibly swallow 60 or so diahorrea pills any more than 60 max strength senokot

 

[DopaMan]

^^^ If you have ever used opioids for any significant length of time you will find that constipation can become a problem, especially at high doses. I have a feeling that constipation produced is no more profound than any other opioid at high doses. Loperamide is not used because it is significantly more constipating than other opioids, it is used because it has no CNS effects at the dose which is useful for treating diarrhea.

 

[emjay]

^^^ If you have ever used opioids for any significant length of time you will find that constipation can become a problem, especially at high doses. I have a feeling that constipation produced is no more profound than any other opioid at high doses. Loperamide is not used because it is significantly more constipating than other opioids, it is used because it has no CNS effects at the dose which is useful for treating diarrhea.

Like you said, it's dose-dependent. Let's say, for the sake of argument (precision doesn't matter), that 1mg of immodium has the same effect on the gut as 1 T3. If you take 100mg of immodium just to feel the effect of a few T3's, you still have the constipating power of 100 T3's.

 

[DopaMan]

Like you said, it's dose-dependent. Let's say, for the sake of argument (precision doesn't matter), that 1mg of immodium has the same effect on the gut as 1 T3. If you take 100mg of immodium just to feel the effect of a few T3's, you still have the constipating power of 100 T3's.

Sort of, but i think the mu receptors in the gut would reach saturation far below the 100 T3 mark. You also develop tolerance to effects other than euphoria, including the constipating effect. Once again, because loperamide is marketed for diarrhea people tend to think its far more constipating than a typical opiod, but its really not. People regularly consume dosages equal to 100mg loperamide in the gut on a daily basis, and deal with it as they need to, by hydrating, eating more fiber, or just waiting until it passes.

PS Chronic constipation is not only uncomfortable, it can also be hazardous. Magnesium citrate liquid or other laxatives seem to be very effective in treating opioid constipation. Increasing liquid intake is also very helpful.

 

[emerald07]

You also develop tolerance to effects other than euphoria, including the constipating effect. Once again, because loperamide is marketed for diarrhea people tend to think its far more constipating than a typical opiod, but its really not.

Constipation is just about the last thing you gain tolerance to. ie you will have long since started to need a larger dose to regain the euphoria while the original constipating effect has not worn off at all.

Opiods aren't typical - some, like codeine, dihydrocodeine are far worse for causing constipation than say, methadone.

 

[emjay]

People regularly consume dosages equal to 100mg loperamide in the gut on a daily basis, and deal with it as they need to, by hydrating, eating more fiber, or just waiting until it passes.

This is true, but they've usually developed a really high tolerance over time. And these are the last people who are going to be able to get high off loperamide. What it comes down to is at what point the receptors are saturated, like you said, and I don't think either of us are going to come up with a definitive answer in this regard.

 

[lucid scream]

BUT, can you snort it?

 

[QuasiStoned]

^^
Sure, but I doubt it would help to get it through the BBB. You'd be better off just eating it.

 

[malfunkshun]

Bra honestly if it works for you than great but 2 things

1. You can't convince yourself of a placebo, if you could we'd all be eating gummy bears and getting an opiate buzz while smoking cigs for a sativa high.

2. Snorting an 80 will fuck most people up. Especially compared to pods and seeds and even morphine unless maybe iv. Unless your doing 320mgs of oxy daily or some huge ammount of opiate/opiod you WILL at least feel something.

I myself had previously posted in this thread that i thought that your post was genuine. I thought regardless of the science you were trying to nicely inform the rest of us of a way to get high, however after reading this post I for 1 am calling shennanigans. I really think your reaching to defend this and am pretty positive your flat out lying at least to some degree. A good way I've learned to tell a liar is when someone details an explanation that no one asked for.

First off, that's what I said, that I can't convince myself of a placebo.

Second, I didn't get high off of the oxy, ok? I made a trip report thread about it years ago and some people said that it was because I snorted it, somehow it got wasted like that.

Third. You can put your 'liars detection method' in your pipe and smoke it. 8) Retard.

edit: Ok, I really am done with this thread now as I just realized what a pathetic waste of time it was to reply to that guy.

 

[Unknown]

^^^
I think you need to get check for auto-immune diseases. Immodium should'nt pass the BBB, and if it is for you, you should take this as a sign to get help!

 

[Tchort]

If you search any recreational drug website or forum you will find the obligatory Loperamide debate. All of the studies that have (and have not) been mentioned in this thread and the rest make me wonder;

Do professional scientists debate this same point in their multimillion dollar, Federally funded labs? "No, really, I swear I got high on this the other night," 'No you couldn't BBB BBB BBB BBB!' which eventually gave birth to the pgp/MDR1 / polysorbate 80 coated nanoparticles articles?

I can't think of any other reason anyone (let alone a medical research facility in a major university or private lab) would pursue Loperamide to this extent other than to prove you can get high on it, some way.

 

[Unknown]

edit: Ok, I really am done with this thread now as I just realized what a pathetic waste of time it was to reply to that guy.

No one is asking you to waste your time replying to that post. Im not denying that immodium makes you high. But if this is the case, you need to seek medical treatment. If your BBB isn't working correctly, theres a major health issue at hand.

 

[Mr Blonde]

If you search any recreational drug website or forum you will find the obligatory Loperamide debate. All of the studies that have (and have not) been mentioned in this thread and the rest make me wonder;

Do professional scientists debate this same point in their multimillion dollar, Federally funded labs? "No, really, I swear I got high on this the other night," 'No you couldn't BBB BBB BBB BBB!' which eventually gave birth to the pgp/MDR1 / polysorbate 80 coated nanoparticles articles?

I can't think of any other reason anyone (let alone a medical research facility in a major university or private lab) would pursue Loperamide to this extent other than to prove you can get high on it, some way.

That made me laugh.

I'm guessing it had more to do with exploring how the BBB works and possible ways to overcome it's mechanisms. It may be useless to get loperamide to be centrally active, but there may come a time when the lessons they learned from that could come in handy in getting a more desirable drug across the BBB.

 

[ATF]

^ Or they were researching exactly that; is this drug at all potentially psychoactive? But with the interests of those who like to keep all the OTC meds boring. Maybe they've been reading bluelight and want to make sure the kids aren't onto something, like with DXM and pseudo-ephedrine.
Hypothetically of coarse. I dont think they would be utilizing polysorbate-80 or whatever for those kinds of studies. Mr. Blonde has the right idea.

 

[ilovechronic]

No one is asking you to waste your time replying to that post. Im not denying that immodium makes you high. But if this is the case, you need to seek medical treatment. If your BBB isn't working correctly, theres a major health issue at hand.

What if he is part of the population that can get high from. In the trials a certain very small percentage got euphoria from it.

 

[Unknown]

What if he is part of the population that can get high from. In the trials a certain very small percentage got euphoria from it.

Then is that case, his BBB isnt functioning properly. He needs to get checked out.