Opioids Big and Dandy Loperamide Adddiction Thread

[shady4091]

Loperamide for withdraws is a huge win. What I don't fully understand though, is how does it work so well on every symptom (even in smaller doses) while still not crossing the BBB in sufficient quantities? Is its activity on the intestinal receptors enough to reduce or even eliminate withdrawal from other CNS opiates?

I've been pondering something else about Loperamide and possible negative side effects of everyday high-dose use. A regular dose is 2-4mg right? So that dose is enough to stimulate the opiate receptors in your intestines etc. enough to cause constipation. Therefor 2-4mg would be a "dose" for your intestines. Now obviously none of that (or no negligible amount) is making it through to your brain in the end. I have; however, taken a dose of 86mg once, a couple years ago, just out of sheer curiosity and I noticed definite CNS effects. Warm body feeling, heavy and sedated and slight euphoria. It wasn't extreme but as I understand that's less than a "recreational" dose, especially since I was already addicted to Codeine. Even so, it was far beyond placebo.

So 86mg. Theoretically, only a tiny fraction of that is actually making it through to my brain. It would be something small, say 0.5mg for the hell of it. It's obviously a very "potent" opioid (Still assuming 2mg is a "dose"). Taking this dose everyday may not cause negative effects any worse than that of everyday, other opiate use but you have to think of how huge of a dose that is for the receptors in your intestines, which are receiving the full amount. It's up to 43 times a regular "dose", of a very potent opioid. Could problems not arise from that alone? I'm not talking about excessive constipation which I don't see as any worse than other potent opiates, I'm thinking more like "over-working" those receptors so-to-speak. Problems like this may not emerge for quite a while.

I'm just speculating here, someone can absolutely correct me if I'm wrong.

 

[i are spectre]

im sure these blood-brain barrier studies are done on significantly low doses. when you bombard your body with hundreds of milligrams of this stuff, the enzymes cant keep up exporting it. there are only so many p-glycoproteins in the endothelial/astrocyte cells. eventually there is going to be more loperamide/substrate than enzymes when you take enough. it's going to get through sometime, it's just not significant at the 8mg to 16mg range, which is obviously lower than what a lot of people take when using it for wd. if you look at LD50 of loperamide with mice/rats/we, the cause of death is respiratory failure, as in it's so smashed it stopped breathing.

 

[i are spectre]

ah yes and there has been some concern for some dangerous metabolites from loperamide. MPP or something i beleive, possibly causes parkinsons by harming cells in the substantia nigra. bad thing about parkinsons is you have no symptoms of it until about 80% of that area of the brain is destroyed, then you notice a few things but it's far too late...

 

[mindash]

i'll vouch for this being a legit problem as i myself have been going to wal-mart and spending aprox 5$ daily for a bottle of 72 2mg pills which i consume as a single dose to keep from experiencing opiate WD. i have been doing this daily now for over a year and the WD sucks just as badly as any other opiate if not worse and for a more prolonged period. also i should add that loperamide has either given me the highest tolerance to opiates ive ever had or has a blocking effect similiar to bupe since last month i took 35 hydrocodone 10/325's in 12 hours (my liver hates me and it was stupid but i forgot to keep count) and did not feel a single effect from the hydro. i plan on acquiring some ibogaine soon tho so hopefully this will finally be over with.

also i will add that while ive not felt a shred of euphoria from lope i do seem to be able to sleep for 12 hours or more whenever i take it which i have no idea why it would have this sort of effect but it does. also one very negative effect i have noticed is if i take anything above my normal dose of 72 pills i experience a "Bug eye" effect where i am fine in small rooms but if i go out to any large open spce i cant seem to fcus on anything without my eyes crossing which is prob not a good sign, i dont know the toxicity or effects of lope in this regard so if anyone else does please do share.

 

[pi^]

ive taken 144 pills everyday for like the past month. im addicted. you get high as hell. some bad side effects, but euphoria like any other opioid

 

[pi^]

Oh yes, I can imagine how loperamide withdrawal is worse than methadone's, dextromoramide's or dipipanone's. Really, there's no comparison. All an average person may get from abusing loperamide is diarrhea and in some rare cases very very weak boneaches, nothing else as it hardly crosses BBB and it also does the job in the gut as a MOR agonist.

Though really if some here have problems with diarrhea that doesn't go away after a few pills, they should really go see a physician because it may something serious. But any leaflet from loperamide product will tell you that so...

loperamide withdrawal CAN be as bad as methadone or any. i really just depends on how much how long. i will fucking gaurentee my 200 pill a day addiction ( thought im still getting high so my tollerance isnt really that high ) is worth than say a 20mg /day methadone addiction. and no im not a troll or w/e the fuck u call it. im on zoloft and i guess sertraline helps it cross the BBB, but honestly i dont care who you are if u take a butload of loperamide and dont have a high tollerance your gonna get high from lope. the negative side effects are terrible though. its stupid. people really under estimate loperamide. my tollerance is already pretty high. when i quit taking loperamide the w/ds were very bad. just as bad as any of my w/ds and that was only the beginning. im seriously scared because i know they would have gotten way worse adn i already couldnt stand it. im sure it would be really helpful to taper though. i could go on and on and on about my knowledge of opioids and experiences and this and that but you gotta trust me. Im not saying im a doctor or anything but iv been around the block a couple times and im smart enough.

 

[pi^]

My god it's been 18 days and I feel way better, but lope withdrawal is horrid. Never, may I suggest to anyone, jump right off of the lope at massive doses. Switch to kratom for a few weeks. My final order of kratom never arrived - even after 21 days - and I may never forgive the mailman. I thought about him while I tossed and turned for days on end.

I finally jumped at - this is embaressing - 250mg a day. Yes m'am, I was taking 125pills each morning. I began waking up feeling so depressed I would just fill a cup with dirty sink water and down the pills (too depressed to walk to the kitchen and get filtered water). I used to pop five at a time. That became too time consuming, so I started taking ten at a time. My throat got better at swallowing the pills with minimal water. Eventually I could take 20 at a time - yet I still had six handfuls to go.

I'm understandably single.

Happy 23rd birthday to me - *blows out whistle*

lol my twin. you sound like me ps im also 23 and single

 

[Fail Fighter]

Sorry to bump, just wanted to add, I've been severely addicted to Loperamide for the past 18 months. I was a HEAVY hydromorphone addict for 4 years, and I was only able to get clean by switching to high-dose Loperamide. But I soon realized that I'm not actually "clean"; the Loperamide itself is almost as addictive as any other opiate. I typically dose 144 pills every 2 days, and if I try and quit, I go into heavy opiate withdrawals by day 4-5.

The only good thing about Loperamide is that it seems to COMPLETELY block all other opiates. I actually TRIED to relapse a few months ago, and I chewed/swallowed 5 Norcos on my birthday... big mistake. Not only was the hydro completely blocked, but it actually seemed to throw me into some sort of awful precipitated Loperamide withdrawal.

Anyone else with experience as to Lope completely blocking other opiates?

 

[Doktah]

I also have abused loperamide - at dosages as low as 48mg - and felt a strong narcotic high for approximately 24 hours. I would swallow one or two handfuls of the generics around dinner time, and usually didn't feel much of anything for 2-3 hours. The next morning however, I would always have a really pleasant opiate fuzz going on

This next part may explain why loperamide gets some people (at least me) high. I am perscribed pantoprozole (sp?) for a pretty gnarly acid reflux issue I have. As it is a proton pump inhibitor within the same realm of omeprazole, it naturally shares many of the same medical characteristics. Take a look at omeprazole's wikipedia entry; It is a competative inhibitor of p-gp along with other proton-pump inhibitors. Now, I am a computer science student, not a chemist... but this is why I think I am able to feel mu-opiod central effects from loperamide. I have tried the quinine thing with no difference, so maybe proton-pump inhibitors are a more efficient means to this sought-after (at least on opiophile lol) end?

Fail Fighter: It's interesting that you note loperamide's dampening effects on other opiods... Since I have been attempting to quit opiods completely, I was frequently bouncing back and forth between Poppy Seed Tea and loperamide as "legal" and "perscription-free" maintainance solutions to keep withdrawal at bay. I did not notice this phenomenon, but each time I gave in, there had been a few days seperating dosages of either.

On a seperate (and somewhat related) note, I am currently using a dilute alcohol solution with 250mg of etizolam dissolved in it to get off opiods. I don't really get any euphoria from benzos, and I only use this sparingly at night to avoid "The Sweats". So far so good; As long as your careful with the etiz (and don't have a history of abuse with benzos), I think this is the best solution to quit hands down. I only need 2mg to get through the night, and I intend to check every 3 days to see if I still require the assistance of the etiz to sleep through the night. Once I do not, *flush*...

All the best to my fellow Lope-freaks and opi-lovers in general! Quit that shit before the grip becomes unbearable....

 

[z10r]

I'm glad I looked at this thread now that people are posting in it again. I have a good deal of experience with Loperamide. A quick background: I'm from the east coast (High Quality Powder) and I recently moved to the West Coast (Decent Tar), as you can imagine, I've tried A LOT of different batches of Heroin from all over the world. A few years ago, I had a serious habit which grew from IV'ing a .2 of a gram to .5-.6 of a gram. At that point, I was clogging the rig because the dope:water ratio was too high! I had, at worse, a 2-3 gram habit per day which was sustained for a solid 4 months at that dose. I went back and forth, back and forth, from a few months of maintenance on either Methadone or Suboxone then back to Heroin, all the way back up to 2-3 grams a day. It was a yearly cycle basically.

Finally, after two and a half years of playing the back and fourth game, I really decided to do my best to quit. I then switched to Suboxone 8 MG per day for 12 months and by the end of those 12 months, I was weaned down to only 1 MG of Sub... and I just still couldn't kick it! I didn't know what to do. I lasted 28 days of moderate withdrawals after jumping off Sub @ 1MG. Next thing you know, I read about Loperamide and decided to give it a try. I can tell you that Loperamide has saved my life and I owe it that in a way. I started my Lope dose at 50 pills / 100 MG and in the beginning I used to take a PGP inhibitor (Tagamet 900mg) which I found I don’t need at all. Some things I've noticed about Lope...

1. VISION PROBLEMS: Yes, you get very blurred vision in high doses. It's strange though, inside a room or building you can see fine but go outside or get in your car to drive and everything is blurry and it's impossible to focus on ANYTHING. (Someone mentioned this above as well.)

2. CONSTIPATION: Eventually you WILL get constipated far beyond anything regular opiates can do to you. Yes, it will take a long time for this to happen... but put it this way, I have to use an enema (embarrassingly) almost every time I have a BM (which is once every week). It's not fun anymore, but this is a very recent side effect and one of the main reasons I am determined now to quit. I'm not sure why it's happening now after a year and a half on a daily dose of Lope. (I've been stuck now at 450 MG/225 Pills per day since last October so I don't get why this is happening now. No diet or exercise changes either.)

3. LOPERAMIDE TO WEEN = BAD IDEA: I screwed myself... again. I took Loperamide to "get off" my low dose of Suboxone (1MG), switched to about 50 pills of Lope to start (100 MG) and now, after an entire year and a half of use, I was at 225 pills per day / 450 MG just 2 weeks ago - I've weaned down to 190 pills as of this week but I feel kind of crappy and sometimes have to dose a few hours early (I dose every 24 hours ideally). Costco loves me - I go in and buy 5 packs of 400 pills each for about $5 each every week. I feel like an ass going in to buy only Loperamide most of the time. I was asked only once about it, which I guess is good considering how many times I've gone in there to only buy 5 boxes of Loperamide. lol.

4. OPIATE TOLERANCE: My tolerance is UNREAL - most of you probably won’t believe me here. I am nearly invincible to ANY opiate at ANY dosage, using IV of course. - I will not and do not feel it AT ALL, Loperamide has made my tolerance INSANE. About 2 months ago, I found out that two coworkers at my new job have a current heroin habit. I told them about my situation and told them that I can't feel anything anymore because of my tolerance from the Lope. I said, "I've shot a half gram at a time on many occasions and felt next to nothing." Of course, he didn't believe me till I went over his house that weekend and I IV'ed a .8 of a gram of tar that he picked up for us and absolutely nothing happened. He was SO worried I was about overdose. HA! I just laughed. Though I really don't get it, it sucks badly - I really want to feel an occasional opiate high. The strange thing is, I now know that Lope isn't acting as a blocker because one time, I went into withdrawal from not taking my dose of Lope for 4 straight days, then tried to IV a nice amount of Heroin and all it basically did for me was take my withdrawal symptoms away. There was no lasting high and there was the slightest, slightest rush that lasted about 2 seconds. I used to IV a tiny cotton shot that barely had any dope in it and I'd feel it 100 times more than this.

5. LAST HOPE: I'm currently weaning down on Lope (from 225 pills now at 190). I just started 2 weeks ago and have been doing well. The past 3 days I really just became determined and randomly picked up some other drugs to help combat the WD symptoms. I quit cold turkey @ 360 MG per day... but right now, I'm using a small amount of Amphetamine (Meth) during the day, 1 MG of Xanax each night, and I also have two 8MG Suboxone which I may end up taking a quarter of a pill (2MG) depending on how I feel at work tomorrow. The meth is helping amazingly. I almost feel no withdrawal symptoms. I woke up this AM very sick in a puddle of sweat. I quickly snorted a tiny line of Meth and 10 seconds later, I feel fine. I was reading online that back in the 60's, a treatment facility in San Diego treated people with Meth and they were successful with a lot of patients. Lucky, Opiates are the only drug that has a recreational value to me... the meth and benzos, I could really care less about. It is helping me out a ton right now, I feel pretty decent surprisingly... I haven't even considered taking the Sub or Benzo yet which is way better than I thought I'd be doing.

My only question is: Does anyone know (or can anyone calculate or make an educated guess) how long will these Loperamide withdrawals last? Considering it has an 8-12 hour half-life, with an average of 10.5 hours from my research. I'd assume the worst WD symptoms with dissipate around day 10-12 or so? Then probably a milder case of PAWS for the rest of the month. I hope I can handle it this time, it’s now or never.

Oh, another very interesting situation that happened to me. About 14-15 months ago, I was working on a boat at dock with someone who happened to be on Suboxone. Now at this time, I’m taking only 100mg of Lope per day. I STUPIDLY snorted a quarter of a Sub. I wanted to really see if what I was feeling from the Lope was in fact, active in the CNS (as everyone swears up and down it can’t be). Well, 10-15 minutes later, here comes that old familar feeling. Keep in mind that the withdrawal wasn’t *that* bad, but I can say it sucked for about two hours. I was soaked in sweat instantly, goose bumps, stomach felt sick, sneezing, histamine, etc… At least it was at the end of the day and I went home and curled up in a ball on the floor for a few hours. What a dumb mistake to make.

Sorry for the long post, hope it all makes sense as I kind of started rambling a few times. I'm glad more and more people are coming out with Lope experience as there's not that much "real" knowledge out there.

 

[Lady Codone]

My brother takes loperamide every single night before bed, and he's done so for the last 6 years. Not sure whether it's a true "addiction" but I imagine if he stopped he'd experience diarrhea at the least.

On the box it says, "may cause drowsiness, dizziness, etc". Is this not indicative that it COULD cross the BBB?

Anyway, OP might want to look into kratom for withdrawals, as it seems to be milder than other opiates and you wouldn't have to take 100+ pills for effects. It's probably cheaper too. Not that it couldn't cause addiction, but it might be easier to quit than what you're doing now.

 

[Znegative]

Yeah that's probably good advice, though if lope truly has a blocking effect at chronic monster dosages, then a taper would most likely need to be set in place first.

Also, as for the warning, it definately is referring to the small ammounts that can cross over the BBB. I read young children are especially sensitive to the effects of loperamide as they are still developing. I've used loperamide several times at relatively high dosages (48mg, 120mg) and can say for certain that I definately did experience some CNS effects. Definately not full on euphoric bliss, but a noticeable sense of feeling content and calm. I used it in place of my usual dose of methadone (40 mg) which I had not taken in two days and it more than kept me straight. Though the half life is significantly shorter than methadone or buprenorphine, for some reason it seems to hold me for a longer period of time.

What I'm truly interested in is the cause for the blocking effect that I've heard reported by so many who use high dosages of loperamide for maintenance. I wonder if this is caused by a high affinity to opiate receptors like buprenorphine, or whether it has to do with tolerance and saturation of the receptors (like methadone). I've researched the stuff a bit, and keep coming up with different answers regarding loperamides potency, we're it able to completely cross the BBB. Some claim that it's actually a very weak opioid similar to Codiene (something I cannot believe due to my owne experiences with it), while others claim that it is incredibly potent.

 

[pgcc]

Wow. I believe you guys but this is crazy. I never thought lope could cause addiction and wd. To go on methadone or subs for this seems overboard because you would be trading a lesser addiction for a greater one BUT if one can't stop no matter what is tried then I can see the use of meth or subs as reasonable. Taking 100's of pills of anything has to be bad for the organs (I have no proof of this, just common sense). I guess this proves that a very, very wide range of otc and prescription drugs are addicting. If meth or subs are used I really hate maintaince programs, I realize some need it, but I believe these drugs are better used to transition the person to become clean.

 

[kajamas]

I am undergoing testing for a possible CSF leak that caused my chiari malformation. My doctor lowered my OxyContin and of course I was going through withdrawal symptoms (hot/chills, nausea, diarrhea ect) this morning I'd had enough of the gastro symptoms and took 1 Imodium. My withdrawal symptoms are gone. Could the immodium have crossed my BBB due to the CSF leak? I am pretty positive I have one, I'm just blown away right now that I feel not only not withdrawaling, but actually pretty relaxed. Is this possible??????

 

[Znegative]

Wow. I believe you guys but this is crazy. I never thought lope could cause addiction and wd. To go on methadone or subs for this seems overboard because you would be trading a lesser addiction for a greater one BUT if one can't stop no matter what is tried then I can see the use of meth or subs as reasonable. Taking 100's of pills of anything has to be bad for the organs (I have no proof of this, just common sense). I guess this proves that a very, very wide range of otc and prescription drugs are addicting. If meth or subs are used I really hate maintaince programs, I realize some need it, but I believe these drugs are better used to transition the person to become clean.

I agree that too often people are put on maintenance too soon (for instance, in 2007 I was put on suboxone after sniffing heroin for about 6 months..I wasn't even fully Dependant, and in the end, my first bad withdrawals were from coming off of subs), or are put on maintenance drugs when their habits are small enough to be detoxed easily without switching to Methadone or suboxone maintenance: two very strong forms of therapy.

However, I feel as if people are underestimating loperamide. If 50-100mg of this stuff can keep me out of withdrawals (my tolerance is 40mg of methadone/day), than it must be pretty potent stuff, especially since not only does it hold me, but I actually don't feel half bad mentally either. So from that point of view, I don't see why it would be so unreasonable to assume that the withdrawals would be any less painfull than a more "conventional" opiate, even if only a small portion crosses over the BBB.

I do feel however that switching to bupe or methadone from loperamide is a bit baffling, as in my experience it works in a similar manner: long onset, long duration, not very intoxicating. I would think that tapering with loperamide would be just as easy (if not easier) than tapering from subs or methadone. I suppose if someone finds loperamide to be incredibly euphoric, then there might be some difficulty in disciplining oneself to taper, but I can't imagine anyone would prefer a loperamide buzz (if they can even achieve one) to suboxone or methadone.

 

[deeSUHAL]

IMO i think being addicted to Loperamide is like being addicted to shopping or texting. but that's just IMO. I actually using it now to help with the W/D's

So from that point of view, I don't see why it would be so unreasonable to assume that the withdrawals would be any less painfull than a more "conventional" opiate, even if only a small portion crosses over the BBB.

.

I read that actually none of the drug crosses the BBB . zero zilch nada!

 

[Znegative]

I've read that as well. I've also read that some does, and I've also read that some does, but is pushed back out by P-Glycoprotein.

I feel that when it comes to loperamide, everyone is ultimately just different in how it effects them. There are too many credible people I've known on and off of bluelight who have claimed to have felt opioid effects from it. I know from my personal experience with it (though limited) that I definately was not just relieved of my withdrawals, but I also felt a noticeable body high, as well as anxiolytic effects. I do not believe that it was placebo as I truly had no expectations of alleviating anything but a portion of the withdrawals I was experiencing. That being said I would only use loperamide in a clutch situation. To call it recreational would be far fetched IMO, but it does have some anxiolytic properties that make things a lot more barable, especially since I personally hate the anxiety caused by opiate withdrawal the most. In the end, what is not arguable is that loperamide is an opioid agonist, and I therefore cannot see why it would not cause withdrawals when stopped abruptly after chronic use.

 

[DooMMooD]

People forget its NOT JUST the opiate crossing the BBB that gets you high.

Considering the vast majority of your opiate receptors exist outside of your brain (what is it like 60-80%?) activating these plays just as large a part in getting you high as the ones in your brain.

 

[IRONMAN420]

Loperamide ,Opiates, and my experience

i have had severe IBS since i was 15 years old, at which time i would use imodium (loperamide) to try and control symptoms as long with antispasmatics ,levsin,bentyl, i eventually noticed benzos helped with the spasms, When I was 20 was in a severe car accident , at the time just doing opiates recreationally occasionally very under control,after my accident i had a severe back and arm in jury,was in prosyethis arm cast 2 surguries..

Once i became legit I noticed the opiates oxycodone,hydromorphone whatever instant release seems to be the only drug to give me relief from my ibs/diareah,when low on meds I can take 10-20 imodium hardly get any effect , probably cause my tolerance but imodium stopped workin b4 my accident,have also been prescribed lomitil which is scheduled but Dr wont prescribe anymore ,says its insignificant with my opiate dose

My Point is this it all makes since the relief i get from opiates and the ineffectiveness of loperamide probably built up my tolerance, nothing else has helped for my stomach, and i have heard from SWIM that when in w/ds they have taken 10-20 loperamide w/ tagamet and had relief from w/d , i dont experience the same feeling as even on subs i had severe diareah and tried imodium to no avail.....

GOOD QUESTION : DOES anyone know if the bupe in the subs would prevent imodium from workin , ive only taken subs twice , when my rxs where not availble and needed something but it seems to make since it would block it if opiod based????

 

[IRONMAN420]

also I wonder if my teen years of takin imodium every day prempeted and helped start my opiate addiction/tolerance, at one point i was doing like 500-600 mgs of oxy a day, thats 6 yrs ago though it just got out of hand , now im strictly for my back pain and mainly stomach maintaince,roxi 6 times a day (sometimes subsitute Dillys depending on pharmacy availibility but thy are both hard to find in south florida)and opana for long acting ,f8ckin trfs!anyway justsayin imodium defenitely builds a tolerance!!!!!!!!!