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  #1  
Old 02-22-2009, 10:03 PM
Druidus Druidus is offline
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Default Loperamide's psychoactivity...

I'm rather interested in loperamide lately. I've found that in large doses, say, 50mg, I achieve quite pleasurable effects. Very opiate-like. I know that loperamide is an opioid, but I had thought that it couldnt cross the BBB. So how does it work? Is it metabolized into an active chemical that CAN cross?

To clarify, these effects are not placebo or the fantasies of an inexperienced drug user. I've injected hydromorphone (amongst other chems) in the past, and used nearly every drug one can think of (barring ketamine, dimethyltryptamine, and actual heroin) and definately know my shit. Loperamide (Immodium - The anti-diarheal) causes a long lasting and profound "nod", and, in me, quite a bit of euphoria.

The problem with using it is that the sedation lasts so long. Literally over 36 hours. You don't feel like moving or doing anything at all. That's not even mentioning the constipation you'd endure using it continually. Just once is a 2-3 day blockage. :bluerazz:

Anyone else discover this? Or have anything to contribute?
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  #2  
Old 02-23-2009, 03:06 AM
NineInchTool NineInchTool is offline
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Default Re: Loperamide's psychoactivity...

its not psychoactive because it never crosses the blood brain barrier
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  #3  
Old 02-23-2009, 05:31 AM
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Default Re: Loperamide's psychoactivity...

That would be the case, normally.

But it is quite obvious to me, through experimentation, that it does have an effect, and that, therefore, something does cross the BBB.

There are supremely noticed alterations to perception and cognition. This requires a cause.
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Old 02-23-2009, 03:08 PM
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Default Re: Loperamide's psychoactivity...

Has anyone else also experienced this? I would be shocked to be the only one. It would also bode well for going through heavy withdrawals. A long acting over the counter opioid might help.
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Old 02-23-2009, 03:13 PM
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Default Re: Loperamide's psychoactivity...

That's fucking interesting man...
Ima pick up a box tomorrow and check it out.

Maybe just because 'it doesn't cross the bloodbrainbarrier' doesn't mean it CAN'T cross it, maybe a few of the molecules make it through.
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  #6  
Old 02-23-2009, 03:32 PM
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Default Re: Loperamide's psychoactivity...

That's what I thought; perhaps enough gets through with mega-doses.

Currently I'd use 2 boxes of 48 2mg pills to get the most effect. I won't go above that for my own comfort, but I find two boxes the peak of pleasure from this chem, if I'm to use it at all.

If you want to try it, I'd suggest one box wholly, if you're 150-160+ pounds in weight, and maybe 75% of the box if you're less.

Make sure you aren't allergic beforehand. I can't be held responsible for others' poor choices.

I wish the boxes of 48 were cheaper, though. 20 bucks or so. Hypothetically easy to shoplift, but in practice not worth the risk. Well, if you get caught, anyway.
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Old 02-23-2009, 10:26 PM
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Default Re: Loperamide's psychoactivity...

Even if it is somehow giving you a buzz at super high doses, it's probably going to be harmful to ingest that much Imodium.
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Old 02-23-2009, 10:29 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Even if it is somehow giving you a buzz at super high doses, it's probably going to be harmful to ingest that much Imodium.
To what system? Not much will reach the brain. GI tract, perhaps.

I think the damage can be negated through infrequent use. It can't be that damaging.
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  #9  
Old 02-24-2009, 05:21 AM
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Default Re: Loperamide's psychoactivity...

I can get better opiates for less, so why bother?
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  #10  
Old 02-24-2009, 03:22 PM
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Default Re: Loperamide's psychoactivity...

For the sake of experimentation.

Not only that, but say you have a physical addiction to a hard opiate and you run out of supply. Loperamide lasts long enough, IMO, to assist with the withdrawals for 1-2 days. It lasts incredibly long, and could ease a lot of discomfort.

If there is something to learn, why not learn it?

Knowledge for its own sake.
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  #11  
Old 02-24-2009, 06:06 PM
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Default Re: Loperamide's psychoactivity...

Bean_Doodle, any word? Did you try it?

I'd also like to say that "better" is subjective. If you're just looking for an intense high, oxy is definately better. If you want a long lasting opiate buzz that will live on far longer than an oxycodone nod, then loperamide is better.

I prefer to combine it with benzodiazepines, a small amount of alcohol, maybe some of the morphine garnered from tea extraction, and some weed.

But it definately works its magic alone, and for extended periods.
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  #12  
Old 02-25-2009, 05:18 PM
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Default Re: Loperamide's psychoactivity...

Bump for word from Bean_Doodle...
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  #13  
Old 02-25-2009, 06:21 PM
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Default Re: Loperamide's psychoactivity...

Still haven't gotten around to it, I'm short on cash and my weekly buprenorphine-day was yesterday, so Ima wait until next week at least.

Also the damn swedish government has a pharmaceutical monopoly and everything is shit expensive and WEIRD.
You can't even get benadryl otc here

Gotta check if there are any loperamide-only pills, most of them contain tons of weird other things.
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  #14  
Old 02-25-2009, 06:24 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Still haven't gotten around to it, I'm short on cash and my weekly buprenorphine-day was yesterday, so Ima wait until next week at least.
Cool.
Quote:
Also the damn swedish government has a pharmaceutical monopoly and everything is shit expensive and WEIRD.
You can't even get benadryl otc here
WTF? That's retarded. In the least condescending way possible, I pity you.

Quote:
Gotta check if there are any loperamide-only pills, most of them contain tons of weird other things.
Immodium brand tend to good, but you're right, get only loperamide pills, they do sometimes mix it up.
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  #15  
Old 02-26-2009, 01:29 PM
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Default Re: Loperamide's psychoactivity...

Have you read the wikipedia article on loperamide?
http://en.wikipedia.org/wiki/Loperam...-brain_barrier
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  #16  
Old 02-27-2009, 03:15 AM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by emag View Post
Have you read the wikipedia article on loperamide?
http://en.wikipedia.org/wiki/Loperam...-brain_barrier
Quote:
Crossing the blood-brain barrier

When loperamide is taken by itself, it cannot readily cross the blood-brain barrier; however, when loperamide-containing nanoparticles are coated with polysorbate 80 and injected, the results were the same as typical opiates and opioids -- long, effective analgesia. A solution prepared using loperamide coated with polysorbate 80 resulted in a very short duration of action and less effective analgesic effect. The same study concluded that loperamide does not cause any analgesic effects when taken by itself.[5]

Concurrent administration of P-glycoprotein inhibitors such as quinidine with loperamide has been found to produce respiratory depression, indicative of central opioid action.
I did. When I'm interested in something, I research it ad infinitum.

However, I never had loperamide coated with polysorbate 80, nor injected it. Neither did I administer P-glycoprotein inhibitors.

I still got an effect. Something crossed my BBB. What?

I can only assume mega-doses allow for enough to cross the BBB or that it is metabolized into something that can.

Then again, it could be a quirk of my biochemistry, and not everyone gets this effect. Hence the thread.
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  #17  
Old 02-27-2009, 06:22 AM
Bean_Doodle Bean_Doodle is offline
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Default Re: Loperamide's psychoactivity...

I think an active metabolite is likely.

Also, have you read the list of sideeffects from loperamide?
Euphoria and drowsiness are two of em.

COINCIDENCE!?!? I THINK NOT!!!!!
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  #18  
Old 02-27-2009, 06:26 AM
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Default Re: Loperamide's psychoactivity...

Exactly, Bean_Doodle. My guess is an active metabolite too.

And the side effects thing is, of course, not coincidence.

I'm trying to keep this thread alive for a while, 'till my next experiment with it and any others from Zokletians.
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  #19  
Old 02-28-2009, 12:04 AM
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Default Re: Loperamide's psychoactivity...

why can't you just smoke a bowl and not take anti-shit medication?
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  #20  
Old 02-28-2009, 12:24 AM
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Default Re: Loperamide's psychoactivity...

Quote:
why can't you just smoke a bowl and not take anti-shit medication?
Codeine is used as an antidiarheal as well.

I'm curious.

Why can't you just explore your world more?
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  #21  
Old 02-28-2009, 03:23 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by Druidus View Post

Why can't you just explore your world more?
Im all for that, bro. Its just that getting high off a potentially addictive anti-poop medication is not a good idea. I'd hate to know what its like to be addicted to anti-poop medication.
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  #22  
Old 02-28-2009, 04:30 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by Vladimir Lem View Post
Im all for that, bro. Its just that getting high off a potentially addictive anti-poop medication is not a good idea. I'd hate to know what its like to be addicted to anti-poop medication.
lol, that's hilarious.

Fortunately, I regulate my usage of addictive substances. Since this is an opioid, I regulate my use.

It's a great idea, if you're able to control yourself.

Besides, you could use any opiate as an anti-diarheal. Heroin, for instance.

Using any opiate is potentially addictive, and therefore risky. Know that, and don't use it often.

Anyway, it's really self-regulating. If you took it every day your intestinal walls would rupture, somewhere, from increasing pressure.
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  #23  
Old 07-14-2010, 01:46 AM
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Default Re: Loperamide's psychoactivity...

Hi, guys. I've been a member of bluelight for some time and just came upon your forum. First off I'd like to say how happy I am to find some intelligent individuals who understand that loperamide can be used recreationally. It's just a question of how.
But I just posted this stuff on BL and would like to post my input here as well.

Today, 17:12
Quote:
Alright guys, I'm not an opiate junkie, and have only played with hydrocodone and codeine really. I took a massive dose of oxys once. They were pissing me off because I didn't feel shit, so I took the rest, and hours later I still felt nothing, so I drank a bunch of vodka.
The next day I didn't leave bed except to vomit. Terrible idea I know now, and I've been told I could have died, but I was young and foolish and had never tried oxy before.
That was my only experience with it... Horrible time...
Anyway, I have terrible GERD and was having one of the worst attacks of my life a little bit ago, so I had my girlfriend take me to the pharmacy. I got a box of cimetidine and loperamide (the acid reflux gives me diarrhea anyway). I've taken one of the cimetidines, but still have mild heartburn so I suppose I'll take another.
I've also taken 12 loperamide tablets (24mg).
I am (obviously) hoping that the antacid will aid in lope's crossing of the BBB, and I'm also hoping (just guessing) that the amount of acid in my gut (and most likely the extensive damage caused by such) might cause better absorption of the loperamide.
At any rate, I'm looking forward to the pain leaving my digestive tract and to not using the bathroom every five minutes.
Today, 18:39
Quote:
I thought that this should interesting to whom it may concern.
http://www.genemedrx.com/PGPtable.php

So, upon reading that and finding that loratadine is an inhibitor of p-gp I promptly took a Claritin-D (pseudophedrine's in there, but we don't have claritin by itself...).
Anyway, I've been sitting here, starting to feel... nifty (?)... I haven't smoked weed since this morning and I've been resisting the urge to do so, for fear of messing up my results with an unrelated euphoria. I did notice that slight pressure you get in your chest when standing on opiates. Heart was slightly slowed (compared to normal heart rate upon standing).
So far so interesting...
Oh yea I forgot, I was getting antsy and took six more lopes, bringing my total to 18 (36mg). I've also gotten a cup of cranberry juice cocktail. Nobody drinks grapefruit, so I mixed it with some Orange-Mango-Peach blend (orange is a mild p-gp inhibitor).
And I'm prescribed sertraline that I consume every day (also a p-gp inhibitor).
So far I have definite effects, however mild, similar to opiate intoxication. It feels REALLY nice to streeeeetch, like vicodin. Ahhhh...

smug huh? I thought he just looked nice and content. Like he's ready to go lalaland, like me...
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  #24  
Old 07-14-2010, 01:54 AM
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Default Re: Loperamide's psychoactivity...

I've IVed immodium before, and definitely felt effects.

mike
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  #25  
Old 07-14-2010, 09:20 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by Druidus View Post
That would be the case, normally.

But it is quite obvious to me, through experimentation, that it does have an effect, and that, therefore, something does cross the BBB.

There are supremely noticed alterations to perception and cognition. This requires a cause.
Maybe at those large doses it creates enough metabolites to cross the BBB?
They do call it poormans methadone because it is similar in duration.
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  #26  
Old 07-14-2010, 09:41 PM
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Default Re: Loperamide's psychoactivity...

Man, I want to try it, but I'm pretty leery of taking 50mg.
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  #27  
Old 07-14-2010, 09:46 PM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by mksnowboarder View Post
I've IVed immodium before, and definitely felt effects.

mike

is this serious? haha crazy.

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  #28  
Old 07-14-2010, 10:08 PM
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Default Re: Loperamide's psychoactivity...

I think I've felt psychoactive effects from loperamide, but it could be placebo.
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  #29  
Old 03-01-2011, 11:28 PM
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Talking Re: Loperamide's psychoactivity...

Ah yes, I too have experienced loperamide euphoria. I have little opiate tolerance, so when I took 70mg of loperamide, 2 hours later I am euphoric, itchy, and feelin nice I also take zoloft which is a potent p-inhibitor almost the same potency as quinidine. It's not bad at all, here I get a bottle of 96 tabs for less than 7 bucks. It lasts almost the entire day. As far as constipation, ive never gone more than 2 days without. It's fun, cheap, and worth it if you are withdrawing or just want to have a little fun.
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  #30  
Old 07-26-2011, 09:19 PM
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Default Re: Loperamide's psychoactivity...

Had to necro this bitch because of interest.
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  #31  
Old 07-26-2011, 09:34 PM
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Default Re: Loperamide's psychoactivity...

So if you take 70mg with little tolerance then I'm gonna have to take like...

*does calculations*

*Explodes after not shitting for a month*
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  #32  
Old 07-26-2011, 10:37 PM
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Default Re: Loperamide's psychoactivity...

Piperine in black pepper assists in BBB crossing and tonic water w/quinine (in the 2L+ range) contains a pgp inhibitor for those without access to pharms. Snorting the powdered loperamide is another option.

Last edited by nshanin; 07-27-2011 at 12:57 AM.
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  #33  
Old 07-26-2011, 11:45 PM
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Default Re: Loperamide's psychoactivity...



*Runs off to pharmacy*
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  #34  
Old 07-27-2011, 02:43 AM
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Quote:
Concurrent administration of P-glycoprotein inhibitors such as quinidine and its other isomer quinine (although much higher doses must be used), PPIs like omeprazole (Prilosec OTC) and even black pepper (piperine as the active ingredient) could potentially allow loperamide to cross the blood-brain barrier. It should however be noted that only quinidine with loperamide was found to produce respiratory depression, indicative of central opioid action.[14]
From Wiki. I saw this yesterday and actually meant to post it; a coincidence that this thread got bumped. I have a couple PPIs (like Nexium), so I'm seriously considering trying this.

I don't like messing with the digestive system, though, so I'm uncertain. One thing to note is that 50mg of loperamide won't necessarily stop you up for longer than 4mg would - AFAIK, it will be processed and excreted almost as quickly. I'm not positive, so use at your own risk, but it should work like that.

Once you've taken enough to saturate your receptors, more won't have any extra effect. I'm not sure how much that is, though - I have a little slip of paper with loperamide info, and it says not to take more than 16mg a day. It also mentions drowsiness being a side effect, which is promising.

Quote:
Originally Posted by nshanin View Post
Snorting the powdered loperamide is another option.
You mean that snorting it would work even without using any PGP-inhibitors?
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Old 07-27-2011, 02:57 AM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by AdMech View Post
You mean that snorting it would work even without using any PGP-inhibitors?
Yes but not significantly at all; my point is don't just nom on the pills: rail them, do an enema (I think this works, might be thinking of another substance), or run an extract and take the goo sublingually (it's deliciously alkaline). Do the most that you can to reroute your metabolism and you'll get a high on par with illicit opiates.
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  #36  
Old 07-27-2011, 03:08 AM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by nshanin View Post
Yes but not significantly at all; my point is don't just nom on the pills: rail them, do an enema (I think this works, might be thinking of another substance), or run an extract and take the goo sublingually (it's deliciously alkaline). Do the most that you can to reroute your metabolism and you'll get a high on par with illicit opiates.
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  #37  
Old 07-27-2011, 04:01 AM
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Default Re: Loperamide's psychoactivity...

Do it, for Science!
but that all sounds like an awful lot of work for dubious reward. So let us know how it turns out please?
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Old 07-27-2011, 05:09 AM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by a334jv2df View Post
Is it the lack of information on different bioavailabilities? Or the opinion that a loperamide high can be as subjectively "good" as an "illicit opiate?"
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Old 07-27-2011, 06:18 AM
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Default Re: Loperamide's psychoactivity...

Quote:
Originally Posted by kingOfCrash View Post
Is it the lack of information on different bioavailabilities? Or the opinion that a loperamide high can be as subjectively "good" as an "illicit opiate?"
Probably the fact that loperamide isn't supposed to be able to pass the BBB at all, no matter how you administer it. There are persistent reports of central effects, though, and drowsiness/dizziness are listed as side effects... so perhaps there is an active metabolite er summat.
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  #40  
Old 07-27-2011, 06:25 AM
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Default Re: Loperamide's psychoactivity...

the way your intestines feel can affect the way your conscious mind feels. Any euphoria you experience is likely related to loperamide's activity on the GI opiate receptors
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