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Opioids Loperamide (Imodium) Megathread v. 2

Mr.Scagnattie

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NYC, the heroin hall of fame.
Version 1

Loperamide



Loperamide is an opioid drug used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor, Fortasec, Lopedium, Gastro-Stop and Pepto Diarrhea Control.

Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system. It works similarly to morphine, by decreasing the activity of the myenteric plexus, which in turn decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.

Ability to cross the blood–brain barrier:

It is a misconception that loperamide does not cross the blood–brain barrier. Loperamide does cross this barrier, although it is immediately pumped back out into non–central nervous system (CNS) circulation by P-glycoprotein. While this mechanism effectively shields the CNS from exposure (and thus risk of CNS tolerance/dependence) to loperamide, many drugs are known to inhibit P-glycoprotein and may thus render the CNS vulnerable to opiate agonism by loperamide.

Concurrent administration of P-glycoprotein inhibitors such as quinidine and its other isomer quinine (although much higher doses must be used),PPIs likeomeprazole(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.
Loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. Symptoms of mild opiate withdrawal have been observed following abrupt discontinuation of long-term therapy with loperamide.


Loperamide 2mg


Imodium (brand name loperamide)




Use in Opiate Withdrawal

In high doses, loperamide has been shown to alleviate withdrawal symptoms from opiate dependency. Dose varies based on tolerance, but many people report (at the correct dose for their individual tolerance), total removal of withdrawal symptoms.


*****Warning*****



More and more people, non-opiate tolerance individuals, who are attempting to take high doses of loperamide to get high, are overdosing and dying. We have had 2 just very recently.

Loperamide should NOT be taken in such high doses unless for the purposes of treating opiate withdrawal symptoms, by individuals with a history of opiate use, and a high tolerance.

The recreational properties of loperamide are almost non-existant. It is not known for its "high". So, attempting to take enough to cause euphoria is simply incredibly dangerous and lacking any possible reward. This is not a recreational substance.

Do not attempt to ingest high does of loperamide to achieve a high.


*****Warning*****

 
Last edited by a moderator:

lilczey

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Just enough for withdraw...

Did you read my post in the last thread?

20mgs was perfect for me.. was still wothdrawing but it took the edge off now im clean
 

SlumberMachine

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Jul 5, 2006
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2
I was addicted to lope for about 4 years taken daily. At the apex of my usage, my dose was ~400mg (1 bottle of 200 2mg pills a day), but I've done even more at times and to get off it I slowly went down 10mg per day. I think it almost killed me a couple times with crazy pressure in my head and loud pops that felt like someone dropping a piano inside my head. I had to do enemas daily to keep my bowels somewhat normal. It became a pain, but was worth it at the time because I was a happy warm camper.

I survived it and have been off it for about 6 months and just got a healthy checkup from my doc. Pot helped get me clean off it.

Some may ask why I took it. Well, I get depressed and I found it fixed my depression. Opiates (even in low dose) have the affect of making life more happy and warm for me, even without the euphoria feeling of stronger types. Other drugs are not possible because I look like a cop and don't have connections.
 

lolwhatzdrugs

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You should copy the last ten posts, from the just archived post here.

I was addicted to lope for about 4 years taken daily. At the apex of my usage, my dose was ~400mg (1 bottle of 200 2mg pills a day), but I've done even more at times and to get off it I slowly went down 10mg per day. I think it almost killed me a couple times with crazy pressure in my head and loud pops that felt like someone dropping a piano inside my head. I had to do enemas daily to keep my bowels somewhat normal. It became a pain, but was worth it at the time because I was a happy warm camper.

I survived it and have been off it for about 6 months and just got a healthy checkup from my doc. Pot helped get me clean off it.

Some may ask why I took it. Well, I get depressed and I found it fixed my depression. Opiates (even in low dose) have the affect of making life more happy and warm for me, even without the euphoria feeling of stronger types. Other drugs are not possible because I look like a cop and don't have connections.
So you're saying you tapered off 400mg a day and it was fairly painless? How long was the taper>

400mg is quite a lot, you probably wouldn't need that much unless you need 1000mg of IV morphine just to "feel normal," or like 275mg of methadone daily.
 

lilczey

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Why would you want to take this in high enough doses to get it through the BBB?

Neurotoxic much?
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1246550/?page=1
Listen bro i understand what your sayin i lost a friend to lopermide a BLer i was pretty close wit...

I agree but i also disagree...

So stop reading here if yu gonna get all sididdy and argue wit me, over the internet.. its pointless

1. Its a opiate that does its job, as far as blocking you up.. it supposedly doesnt cause cns depression and only makes a very small aloud to cross the BBB..

2. Makes sense you can take a large dose to get more across the BBB.. this would also cause CNS depression...

3. We are fucking junkies do you really give 2 fucks about what we put in our body.. we buy pills from companies that tell you how much of a drug is or isnt in the pill... which sometimes or alot of the times untrue.. for exsample roxies companys getting sued for putting more oxycodone in their roxies then 30mg.. or we buy our drugs off the corner from some dude thats telling you that its "heroin".. he doesnt even kno whats in it.. all he knows its sum fiiiiyaaaa.. we dont give a fuck as long as it gets us fucked up..

Ok now heres where i tell you what i agree with you about.... if your still reading...

1. PEOPLE SHOULDNT USE IT TO GET HIGH........

It should be used for withdraws and not often... it should be used only when desperately needed.....

I took 18mg im sorry for the confusion... and that was just right at a 6 month oxy run at 60mgs a day

Repost from last thread for noobs
 

lostinthespace

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Feb 4, 2014
Messages
124
Ethanol is neurotoxic too. Who the fuck would take that, cept nearly erryone?

Are you seriously trying to compare ethanol to the neurotoxicity of *POSSIBLY* MPTP like chemicals? Really? Rather irresponsible at best. *shakes head*

Listen bro i understand what your sayin i lost a friend to lopermide a BLer i was pretty close wit...

I agree but i also disagree...

So stop reading here if yu gonna get all sididdy and argue wit me, over the internet.. its pointless

1. Its a opiate that does its job, as far as blocking you up.. it supposedly doesnt cause cns depression and only makes a very small aloud to cross the BBB..

2. Makes sense you can take a large dose to get more across the BBB.. this would also cause CNS depression...

3. We are fucking junkies do you really give 2 fucks about what we put in our body.. we buy pills from companies that tell you how much of a drug is or isnt in the pill... which sometimes or alot of the times untrue.. for exsample roxies companys getting sued for putting more oxycodone in their roxies then 30mg.. or we buy our drugs off the corner from some dude thats telling you that its "heroin".. he doesnt even kno whats in it.. all he knows its sum fiiiiyaaaa.. we dont give a fuck as long as it gets us fucked up..

Ok now heres where i tell you what i agree with you about.... if your still reading...

1. PEOPLE SHOULDNT USE IT TO GET HIGH........

It should be used for withdraws and not often... it should be used only when desperately needed.....

I took 18mg im sorry for the confusion... and that was just right at a 6 month oxy run at 60mgs a day

Repost from last thread for noobs
1. Agreed.
2. The majority of anecdotal reports say otherwise. In fact most of those who have had a loperamide "high" have called it sort of jumpy rather than chilled.
3. Forgive me but isn't this a harm reduction forum? Allow me to apologize for adding to the wealth of opinion and fact in the hope that it might save someone a trip to the ICU or morgue, or that it may save someone's son, daughter etc etc etc...
 

lostinthespace

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Feb 4, 2014
Messages
124
I'm going to elaborate of the pharmacos of loperamide a bit here. For the unenlightened.

Loperamide is a mu-agoinst - TRUE.
Loperamide is psychoactive - FALSE *at recommended doses*
Loperamide readily crosses the blood brain barrier - FALSE
Loperamide can stop diarrhea with very small doses - TRUE
Loperamide in fucking massive doses may pass the blood brain barrier and get you high *maybe* - TRUE (decided to humor the believers)

Can you see where I'm going with this?
Small dose of loperamide = stops the shits.
Small doses of loperamide = will never get you high
Massive doses = may get you high.
Massive doses = paralytic ileus.

Paralytic ileus can result in tissue death and necrosis, leading to gangrene.

Not to mention the fact that loperamide can cause V.fib in these doses. Especially when combined with other stuff like cimetidine. We have had this actually happen to a bluelight who has spent several weeks in the ICU. I am currently unaware of his status. He had to be cardioverted multiple times.

But hey, if you guys wanna go fucking kill yourselves or walk around with a shit bag attached to your abdominal wall for the rest of your lives. Be my fucking guest.
 

Captain.Heroin

Sr. Moderator: H&R, Words, SLR
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^ very graphic warning

Thanks for sharing.
 

EP158207

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Aug 12, 2013
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London
The things you learn on BL.

I have never liked the idea of stopping the runs. I figure its better out than in, so never use the stuff. Interesting to see that some people get high off the stuff.
 

lolwhatzdrugs

Bluelighter
Joined
Jun 20, 2007
Messages
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Location
Always got it blown like Al Capone
The things you learn on BL.

I have never liked the idea of stopping the runs. I figure its better out than in, so never use the stuff. Interesting to see that some people get high off the stuff.
Diarrhea is one of the leading causes of death among children in undeveloped countries. Although it is true, in several disease processes that cause it, stopping it is contradicted. But there are several where it's better to stop having to take a shit every 5 minutes.
 

Sprout

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Oct 13, 2009
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Finding new lows.
I presume this is the best place to post this.
Recently, I came into possession of some 4-Acetyl-Loperamide, acylated by SWIM (first time that acronym has been used honestly). It came as a brown, odourless, hygroscopic 'powder', in ten or so chunks with a total weight of 100mg. I was expecting minimal results given my less than lacklustre experience with standard Loperamide and the fact I have somewhat of a tolerance (120mg Morphine). I found a total dearth of literature on 4-AL and so I began with a dose of 10 micrograms, which was ineffective, as expected. 100 micrograms - nothing. 1mg - zero. These doses were all consumed orally.
I eventually decided to freebase it, crudely, using the 'crack spoon' method. After some more experimentation I worked up to 15mg smoked off foil and experienced... threshold opiate effects! 'Shocked' doesn't suffice! This was no placebo, pupil constriction was apparent, itching, vasodilation, calmness and anxiolysis.
Naturally, I upped the dose. The yellow oil that resulted from freebasing another 30mg was added to tobacco, which was rolled into two cigarettes. The vapour was acrid and difficult to inhale, opiate effects grew with every inhalation and I struggled to finish the second cigarette. This chemical is active - I was high, this was centrally active.
The high itself was... strange. The first 2 hours consisted of great stimulation, without anorexia. Later on came the sedation, heavy sedation which allowed me to 'nod' very easily. Nausea hit at the 3/4 hour mark and signalled the arrival of euphoria, mixed with mild disorientation. It felt similar to a dissociative, strangely. Like Oxycodone and low dose Ketamine - stimulating, mild NMDA feeling, but overall; an opiate high.
I was visibly intoxicated, my pupils were absolute pin pricks and the area around my eyes was red. I think the hardcore gouching may have contributed a little, also...
I have to make note of the duration - 28 hours. Yes, 28 fucking hours! I dosed at 12pm on Monday and had to drink coffee to stop gouching at 3pm Tuesday. It was incredible.

I never expected anything noticeable from 4-AL, let alone a solid opioid high that lasted longer than PST!
 
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