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One more word about getting high with loperamide (Immodium)

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

"Diarrhea: codeine and loperamide are the most widely used opioid for this problem. Loperamide has the advantage of acting only on the gut, since very little is absorbed."

So that theoretically should mean that in large enough quantities it CAN pe psychoactive, right?
 
Theoretically yes. BUT, it doesnt tell you how much makes it through. We have no idea. It could be 5mg for 100mg that gets through, or it could be .00005mg for 100mg or it could be 50mg for every 100mg. Nobody knows. More than likely, its something low, like less than 1mg per 100mg. Much less than 1mg. A recreational dose would be in the micrograms, so if the OP actually got high, than it couldnt have been more than a tiny bit that made it through.

Ok, lets say it is possible, think of the cost/effect part of this problem.

If very little does make it through, that means, like the OP, youd have to take 100 2mg pills to feel anything, at the very least. Do you know what kind of effect 200mg of loperamide is going to have on you? Its not something you want to do to yourself.

Second, if loperamide were able to cross the BBB, its potency is outrageous, similar to that of fentanyl. If I recall correctly, a psychoactive dose would also be in the micrograms, but at the highest, low low single digit milligrams. Now, if you take 200 MILLIGRAMS of loperamide without knowing exactly how much is going to cross the BBB, look at the difference between a psychoactive dose and how much you have actually taken. If more than a couple mg's actually cross the BBB, youre dead. The overdose potential is through the fucking roof.

Also, the high, according to everyone who has ever supposedly been high on it, is dirty and cheap. They say it is nothing like any other opiate that is used recreationally.

Does it sound like its worth it to you now?
 
Whatever floats your boat man. I myself am not eating 100 plus pills to get high. Even if it does work one would question the cost versus another form of opiate. 8) A bit too labor intensive for me but I do appreciate the thread cause it seems your motive is generous=D
 
Absolutely.

Its much easier to buy a 10 dollar bag of heroin and snort/shoot it than it is to buy 10 dollars of Immodium and swallow all 100 of them for very little reward

And youre right. You cant be mad at the guy for trying and posting, but anyone who actually follows his footsteps is making a mistake.
 
Bavanai said:
http://en.wikipedia.org/wiki/Opioids

"Diarrhea: codeine and loperamide are the most widely used opioid for this problem. Loperamide has the advantage of acting only on the gut, since very little is absorbed."

So that theoretically should mean that in large enough quantities it CAN pe psychoactive, right?
Click to expand...

No, that quotation is misleading (not because of anything you did). It's that it can't cross the BBB.

There are active measures for removing what crosses.
 
Thats what I thought. It needs some kind of protein or whatever to help it across, otherwise it will never make it on its own.
 
SixPartSeven:When did I ever bring up my join date? And what does my post count have to do with anything? Considering two of your last five posts consisted of "no," and "yay!hugz," I really don't think the number of posts should be synonymous with the value one has to the overall community. I mainly posted about topics I had actual experience with, which is the reason I started using this site in the first place. Now i just lurk once or twice a month. The two mods in this thread have obviously never taken Loperamide, so why have such a concrete opinion of its lack of potential?

I never once jocked Negro's nuts at all in past posting, I just bring him up specifically because he was really the only OD mod that provided anything interesting to the board

But its funny to see two mods have divergent opinions on a subject, but I get warned because I used the word "fucking?" SixSeven's last post was so completely jumbled I can't even begin to dissect it properly. Your first paragraph states you believe a tiny bit gets through. Then the third paragraph warns the kiddies that "OMG if you take 200mgs you are gonna get hit with a 2mg blast and UR DEAD." Why don't you stick with your first paragraph, where you said that the ratio is likely MUCH less than 1%?

Chimpo-Here you go, it took two min to find something. http://www.pnas.org/cgi/reprint/91/1/68.pdf Tagamet would be the pH affector. http://www.nature.com/clpt/journal/v77/n2/abs/clpt2005125a.html Quin is not that hard to come across. We certainly are not talking about nanoparticle coating here. It's pretty obvious that your rigid stance that Lop does not cross the BBB AT ALL is incorrect. Thats really the only reason I bothered posting in this thread to begin with...to illustrate exactly why BL is clogged up with garbage posts like yours in the first place. And you are a mod no less. If you don't know much about a topic, resist the need to chime in with your opinion...the two mods in this thread have obviously never taken Loperamide, so why have such a concrete opinion of its lack of potential?
 
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Hey man, I didnt warn you, and youre the one who said Negro, I never said his name. In fact, thats not even who I was talking about, and I never said your join date had anything to do with anything. I simply used it to make the assumption that when you said "what happened to OD," or "it never USED to be this boring" you were referring to a time when it was ran differently years ago.

Negro was an awesome mod, i agree, but again, thats not who I was talking about.

And no, you read my post wrong. I never said either of those possibility were right or not, because to be honest, I dont know everything about loperamide, and I have no idea which one of them would be right. I admit the post is jumbled, but thats because I edited it like 7 times to add things in when I would remember them later. I just detailed different possibilities of what could or could not happen given the OP's scenario. I do agree that the ratio is MUCH less than 1%, in fact, I believe the ratio approaches 0%.

What pissed me off about your post is your "it was better when..." attitude. Its offensive to us mods because we try hard to keep OD good, and then everyone just bitches because we dont run it like PhreeX did. Fuck that, were not going to run it how he did. We will run it the way we see fit, and so far its working quite well, so its just a pain in the ass when people come along with the attitude similar to yours, jocking PhreeXs nuts for some reason or another. I have nothing against the man, but this is not his OD anymore. At least try to have some respect for the current system. Thats all I ask.
 
Unless you inhibit p-Glycoproteins, it doesn't matter how much is getting through. It's going right back out.

sertraline is probably the best drug to take a go with it.
 
Hey I understand where you are coming from SixSeven, the only real reason I brought that attitude to the table was because when I was an active member, no mod would ever make such a grand sweeping statement like Lope does not cross the BBB AT ALL, then belittle the worth of the entire thread in the first place, when they have NO EXPERIENCE WITH IT WHATSOEVER. Sure Phreex let the board get a little out of hand, but he fucking knew his painkillers.

You can all laugh at the ridiculous nature of taking handfuls of pills to get a relatively weak opiod buzz...and like i admitted prior, I stopped screwing around with it because of the constipation. But it did so SOMETHING. And it was not a placebo.
 
I got ya. No hard feelings.

Personally, I wont say what I think about this lope shit, because Ive never tried it. Ive heard conflicting reports arguing for every different angle of the subject, so I dont know what is true and what isnt. Ill leave it up to the people who actually tried it and who want to try it to figure it out. The only thing I will say is that I dont suggest doing it.
 
hey, hypothetically if one were to get some fish oil tablets or something with polysorbate 80 in it (it is in some household products)

and take this with a large amount of loperamide

would it increase the amount able to cross the bbb? even if only by a miniscule potential, with large doses, it could work hypothetically..


no?

would love if ham-milton cud look at this
 
^if you know anything about making nanoparticles of loperamide coated with polysorbate 80, it might work.

risefromruin:
your first link was common sense, but said nothing about loperamide itself.
your second link only said that loperamide made peoples pupils smaller.

As 6/7 said: a bag of heroin is cheaper than 100 imodium pills. and PROVEN to work.

So I guess I'm speaking in absolutes: I guess loperamide can cross the BBB in miniscule amounts, it just happens to be removed instantly. In my book, thats just as good as never crossing at all.
 
I imagine that we are all very familiar with the article regarding quinidine and loperamide; I remember people thought it was a big deal in 2001 (shortly after it came out, I believe). It is perhaps somewhat misleading:

Although the antidiarrheal loperamide is a potent opiate, it does not produce opioid central nervous system effects at usual doses in patients. On the basis of in vitro studies demonstrating that loperamide is a substrate for the adenosine triphosphate-dependent efflux membrane transporter P-glycoprotein, we postulated that inhibition of P-glycoprotein with quinidine would increase entry of loperamide into the central nervous system with resultant respiratory depression. METHODS: To test this hypothesis, a 16-mg dose of loperamide was administered to eight healthy male volunteers in the presence of either 600 mg quinidine, a known inhibitor of P-glycoprotein, or placebo. Central nervous system effects were measured by evaluation of the respiratory response to carbon dioxide rebreathing as a measure of opiate-induced respiratory depression. RESULTS: Loperamide produced no respiratory depression when administered alone, but respiratory depression occurred when loperamide (16 mg) was given with quinidine at a dose of 600 mg (P < .001). These changes were not explained by increased plasma loperamide concentrations. CONCLUSION: This study therefore demonstrates first the potential for important drug interactions to occur by a new mechanism, namely, inhibition of P-glycoprotein, and second that the lack of respiratory depression produced by loperamide, which allows it to be safely used therapeutically, can be reversed by a drug causing P-glycoprotein inhibition, resulting in serious toxic and abuse potential. http://www.ncbi.nlm.nih.gov/pubmed/11014404
Click to expand...

I used higher doses than this study, and I only noticed dizziness/stimulation (sort of like the nasty stimulation you often get from meperidine), as well as some constriction of the pupil. However, I did have quite a tolerance at the time, which essentially makes my results meaningless.

I do think loperamide could be centrally acting in some extreme or unusual circumstances, but not only is this highly impractical, I have a feeling the full effect would be quite terrible.

Edit: I forgot about this one

BACKGROUND: The antidiarrheal drug loperamide is frequently used to treat ritonavir-associated diarrhea in patients with human immunodeficiency virus. The absence of marked central opioid effects has been attributed to its low bioavailability and its poor penetration of the blood-brain barrier, both of which might be altered by ritonavir, a potent P-glycoprotein and cytochrome P4503A inhibitor. METHODS: A 16-mg dose of loperamide was administered to 12 healthy male and female volunteers together with either 600 mg of ritonavir or placebo. Detailed pharmacokinetics of loperamide and its metabolites were determined over 72 hours. Central opioid effects were measured by evaluation of pupil diameter, cold pressor test, and transcutaneous PCO2 and PO2. RESULTS: Ritonavir caused a major pharmacokinetic interaction, increasing the area under the concentration-time curve of loperamide from 104 +/- 60 h x pmol/ml after placebo to 276 +/- 68 h. pmol/ml and delayed formation of the major metabolite desmethylloperamide (time to reach maximum concentration after drug administration [t(max)], 7.1 +/- 2.6 hours versus 19.6 +/- 9.1 hours). The urinary metabolic ratio of loperamide increased 3 times whereas the total molar amount of loperamide and metabolites excreted in urine remained unchanged. No central pharmacodynamic effects were observed after coadministration of loperamide with either ritonavir or placebo. CONCLUSION: This study demonstrates a major metabolic interaction probably by cytochrome P4503A4 with no evidence of P-glycoprotein involvement. This might explain the lack of central effects after ritonavir.
Click to expand...

This one identifies no central opioid-like pharmacodynamics of loperamide following the addition of ritonavir, but it did significantly alter the kinetics. The first studies suggest some significant P-gp inhibition from the quinidine, so perhaps a combo of ritonavir, quinidine and loperamide could produce some long lasting, relatively profound results (don't try this). Perhaps this would be worthwhile if loperamide was not such a shitty drug.
 
Haha, I didn't read the above posts. No one has jocked my nuts since last weekend...
 
man malfunktion your either really lucky or just incredebly stupid *dont take this personally*

poppin immodium sounds like something i would have done way back in 5th grade. smoke some weed,for fucks sake! either way, some stuff in this thread made me laugh. heh.
 
Malfunkshun, fuck these pretentious haters, don't forget that they're all on drugs. But for real, even if it gets you high you have to consider your organs here! Do you really trust the pharm companies, even the OTC pigs, enough to take that much of this shit, give your poor liver a break, dog! BTW, I love your user name, is it perhaps a reference to the precursor to Mother Love Bone? Being from Seattle I can appreciate that. Just don't follow Andy Wood's example.
 
Ham-milton said:
Unless you inhibit p-Glycoproteins, it doesn't matter how much is getting through. It's going right back out.

sertraline is probably the best drug to take a go with it.
Click to expand...

This topic is the whole reason I found Bluelight, and I had never seen this specific thread, but this ^ is very interesting.

Im up and down on prescription opiates all the time. When I have to go without for a few days, and im feeling really bad, I reach for the Loperamide. I usually take 10-15 of the generic 2mg. I always feel noticeably better, but had never thought of it as anything but me feeling better because I dont have the withdrawal shits and stomach issues.
Id read up on Loperamide and the BBB, and had dismissed it as not worth pursuing, but stumbled across this thread today and decided to see if there was anything I didnt know yet in here.
I also take 100mg of Sertraline daily, and varying amounts of Ranatadine (zantac). I take small amounts of fish oil as a dietary supplement.

I have noticed effects off of Loperamide at the 40-50mg doses, certainly more than most of these posters think is possible. I wonder if my 'drug-cocktail' of the sertraline etc. is having an effect, and wonder to try higher doses and experiment further. Neato burrito!8o
 
WOW, I just read this whole thread and I am amazed. I was laughing at times and at others I was just shaking my head.

My input: To each his/her own, if you like to take 100 immodium and get a buzz, cool. I dont care if its placebo or not. I am amazed that this thread is now up to 5 pages...

Bupe works for me...%)
 
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