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Opioids Loperamide (Immodium) Megathread: We have now lost at least 2 of our own from Lope

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Mr.Scagnattie

Mr.Scagnattie

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Loperamide

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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 mildphysical 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.

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Loperamide 2mg

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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 it's "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*****


​
 
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I thought loperamide was unable to cross the bbb, so how are you getting actual effects,?? I dont think it is CyP2d6 inhibition by the juice. I know it is closely related to fentanyl, but with very little ability to cross the bbb, so little to no recreational value. What else are you doing??
 
Quercetin is said to have p-glycoprotein inhibiting qualities that allow loperamide to cross the bbb. It is a boiflavanoid found in grapefruit.
Anyone have journal abstracts or other good info??
 
No BS. I'm aware of the BBB issue, but for some reason I'm abile to bypass it. I swear it is not placebo. The effects are similar to poppy tea for me.

My first attempt was to grind up about 30mg and mix it with a teaspoon of olive oil, not sure if that worked because at the same time I also tried GFJ and plugging.

I also get similar effects without using the olive oil or plugging.
 
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It seems that a CYP450 inhibitor is required as well as a p-glycoprotein inhibitor in proper doses to force loperamide through the bbb. Placebo anyone??
 
"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.[2]

Also, it may be possible for loperamide to bypass the blood brain barrier completely through insufflation.[3] Recreational users may attempt to isolate the loperamide from the inert fillers through a typical cold water extraction, and then snort the resulting material."

From Wikipedia, the great source of all knowledge...
 
Definitly not a placebo when my eyes are pin points, my friend asks me if I'm stoned, and I feel like I'm wrapped up in fresh from the dryer warm blankets.
 
so does this mean that i were to take a bunch of immodium along with a few grapefruits worth of squeezed juice i can feel something?

or even do a CWE i can snort the active chemical and feel something?

im confused man.
 
Are you just strait drinking imodium? if so your fucking nuts man, how the hell can you shit? Lets get some more info going about this, i know there has been studies with loperamide and monkeys or something, but i want to see how this stuff works on humans, and if it actually does have any recreational value. Also are you opiate tolerant?
 
Ok, details:

I buy the 96 count 2mg pills for $15.99 at the drug store. Half of the bottle is enough for a good 8 hour trip.

I always drink GFJ (100% pure).

I've been on paxil for a month. 20mg daily.

I use tobbaco (snuff).

age = late 20's.

~200 lbs male.

Used poppy tea almost daily all of last year, but not in the last 2 months.

The reason I first tried Loperamide was for tea wd. Then I noticed that when I took about 5 pills I started feeling in a good mood. From there I experiemented with more and found out that my mood increased and I started feeling euphoric.

Any other details needed?
 
You won't be taking a crap for quite some time if you try it. This is fucking retarded.
 
it's been my experience that loperamide should not be pursued for anything but withdrawal therapy. i'll list a few reasons, all from 1st-hand or 2nd-hand experience.

1) delayed effect, even when snorted. you don't know how this dose will treat you, and it could be barf o'clock before you realize you had too much.

2) build-up effect in the body can leave you feeling hung over for days after a long binge.

3) if you aren't committed to using loperamide solo (as the only opioid you take), you run the risk of impulse-loss; it's quite competitive but not nearly as euphoric as any other opioid, so if you're not committed to abstinence you have the possibility of an expensive dose of something else going down the drain.

i always used insufflated loperamide after oral cimetidine (800mg-1.4g); it's established that there's a great bbb loophole in the olfactory system and you can withdraw effectively using it. i would consider pursuing proton pump inhibitors based upon further reading, but i have no experience in this arena so i can't speak to it.

- amar
 
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