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Loperamide the OTC fentanyl (reason for no CNS activity)

negrogesic said:
Personally, years ago I attempted to achieve a central narcotic effect from loperamide, and with many attempts at dose in concert with many compounds (p.o. quinidine, omeprazole, etc, etc).

End result after various idiotic attempts: Yes, some central activity when induced with a combination of agents I cannot recommend (the barrier is there for a reason), but of a very "dirty" nature (like meperidine, but even 'dirtier' and far less 'enjoyable'; certainly not worth the exposure risks of the facilitating agents, not to mention the worrisome toxicological unknowns).

Point: Even when introduced centrally, the drug is inherently shitty, and (again) a potential toxicological nightmare.........
Click to expand...

Same, felt very unhealthy. As much as I love opiates I wouldn't try it again.

I haven't tried piperine for PGP inhibition, but there are 2 or 3 good long threads discussing it as a possible potentiator of codeine one Drugs-Forum and BL (sorry, too lazy to google right now. They're in the first few results so easy to find). Last time I checked them nobody could find any definitive answer on CYP2D6/CYP3A4 potentiation/inhibition, however somebody found the average piperine content of black pepper, and also found a study of it's effect on frogs or something like that, so he came up with an amount of black pepper which is likely to give an effect, but it was more likely to fuck up your GI tract before any worthwhile potentiation. IIRC a couple of posters tried it and found this out the hard way. Sorry for being lazy guys after you've all posted such interesting links, don't think I could even get up to take a leak right now.
 
In Finland we have loperamide capsules called "lopex" that dont have magnesium stearate in them at all and I have not felt anything different from basic imodium tablets. But then again those without magnesium stearate are the cheapest but still cost so much that with that kind of money I'd rather buy buprenorphine or methadone from the street than try to get a high dose of those capsules. I have taken 150mg of loperamide once (cheap Russian capsules) and I was nodding for 2 days (also felt really dirty high and was terribly dehydrated by loperamide for some reason)


also a friend of mine who is a pharmacy student said that the reason they use magnesium stearate is to stop the pills from sticking to the machinery while making it (so its just a binder/lubricant or what would you call it)
 
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New, so please don't judge

I'm brand spankin' new here so please be kind. I actually came here because of this thread.

I've used loperamide for about 6 months for maintenance (not on a daily basis). It's been a freakin' miracle and a great help when my very active kids are around. Otherwise I'd spend all day in bed feeling like hell. It wasn't until I happened across this link: http://www.drugsandbooze.com/showthread.php?39037-Loperamide-Works-Finally that I finally got something out of it other than a relief from the w/d's.

That's not necessarily true. When I first started I had some capsules of straight quinine lying around from when they were still being prescribed for night leg cramps. I took about 200 mgs of quinine plus 25 - 2mg lopes. I def. got a dirty buzz feeling that lingered on the edge feeling like it was just out of reach.

Tonight I tried the recipe from the link above and I'm a little surprised. It's not a really "pleasant" buzz, it's still a bit dirty, but it's definitely there. I have been on and off opiates since 2004 due to a botched back surgery and lets face it, no matter how much the docs tell you that x,y,or z should work to kill your pain, sometimes it just doesn't. So you end up taking more, just so you can get out of bed, but then at the end of the month, you're left out in the cold either trying to score some pills or something heavier just to keep you level. And now I have a new doc who drastically lowered my meds and I blew through them in 5 days. SUCK! So lope has been a blessing and this dirty buzz isn't great but it would be nice every once in a while, while you're watching a movie perhaps, or just dicking around on the web.:D

P.S. I'd also tried lomatil but the presence of the atropine (it's belladonna for crissakes) prevented me from taking it in large enough amounts to get anything out of it.
 
negrogesic said:
This topic has already been discussed in considerable detail on various bluelight sub-forums......

Personally, years ago I attempted to achieve a central narcotic effect from loperamide, and with many attempts at dose in concert with many compounds (p.o. quinidine, omeprazole, etc, etc).

End result after various idiotic attempts: Yes, some central activity when induced with a combination of agents I cannot recommend (the barrier is there for a reason), but of a very "dirty" nature (like meperidine, but even 'dirtier' and far less 'enjoyable'; certainly not worth the exposure risks of the facilitating agents, not to mention the worrisome toxicological unknowns).

Point: Even when introduced centrally, the drug is inherently shitty, and (again) a potential toxicological nightmare.........
Click to expand...

^This

Melange died from this stuff btw
 
i find it interesting that you mentioned using doxepin to enable it crossing the BBB...i take doxepin regularly for sleep every night.
 
negrogesic said:
This topic has already been discussed in considerable detail on various bluelight sub-forums......

Personally, years ago I attempted to achieve a central narcotic effect from loperamide, and with many attempts at dose in concert with many compounds (p.o. quinidine, omeprazole, etc, etc).

End result after various idiotic attempts: Yes, some central activity when induced with a combination of agents I cannot recommend (the barrier is there for a reason), but of a very "dirty" nature (like meperidine, but even 'dirtier' and far less 'enjoyable'; certainly not worth the exposure risks of the facilitating agents, not to mention the worrisome toxicological unknowns).

Point: Even when introduced centrally, the drug is inherently shitty, and (again) a potential toxicological nightmare.........
Click to expand...

Thanks negro


sekio said:
Melange was a semi-regular poster here on BL who made the unfortunate choice of experimenting a bit too much with loperamide.

Shrine thread

One of his final posts

RIP. Loperamide is not meaqnt to be a recreational drug and should not be used as such. Even opioid w/d is better than death...
Click to expand...
This is what I was just thinking of before I even read your post. I talked to him the day before he did it. ...... :|
 
listen, i am not nearly as scientific as any of u and i probable shouldnt even be in the advanced drug discussion forum... let me rephrase that.."definitely" shouldnt be in this forum... however, going on experience is almost the best information there is and i can undoubtedly tell you that i recieved euphoric effects similar to that of oxycodone wen i took 72mg of loperamide and ate a shit load of black pepper... i didnt believe it either. i read on wiki that piperine contains something that aids in crossing the BBB and i was nodding my ass off... so yea like i said just my experience.. drugs react differently for everyone i guess...
 
Captisol was being tested with Imatinib to allow the latter to cross the BBB for lowering opioid tolerance. The Captisol website sends free samples upon request, and being a nontoxic cyclodextrin, might easily and freely bind to something such as loperamide as well. Whether or not it would similarly help it cross the BBB I do not know. However it should be noted that cyclodextrins as used in aerosols do indeed act in a manner which freely bind to odorants without special circumstances or reaction conditions of any kind.
 
Yesterday I took 40mg loperamide (the brand that does not contain magnesium stearate) and 10 teaspoons of ground black pepper. After about 1 hour I got histamine release similar to codeine and felt euphoric and anxiety free. Then an hour later I had to go to take a nap because I was feeling extremely tired and while lying down in my bed I felt like I had eaten 5 large poppy pods. So extreme amounts of black pepper and 40mg loperamide do work well and I am still feeling the antianxiety effect and muscle relaxation from loperamide.
 
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