Opioids Big and Dandy Loperamide Adddiction Thread

[Hallucinogens R US]

Well it's been a while since iv been on here.. I successfully got off the lope after hellish hellish withdrawals which lasted a solid 2 weeks. Luckily I was able to get through it with the help of exercise vitamins and marijuana. I am now free of it and only chase the dragon on occasion if wanting to visit the company of opiates.

 

[sobriety]

Lope for long periods of time (4-6) weeks is the woooooorst! Im over 5 weeks off and still at night, cant sleep heart beating out of my chest and some pain still during the day. Used it to kick bupe at about 1mg per for 2 years. Helps at first suuuuuper hard to kick. Dxm helps for a little while. Benzos, dont even go there they are worse unless its like for a week or two. what a stupid prisoner of a drug I cant believe they give this to people!!!!! Its going to be suuuper hard. get off and stay off, its MADDENING but whats the alternative????

 

[Mc83]

Sobriety - don't get discouraged, you can do it. I was on an average upwards of 200-300 mg daily for nearly 2 years. Tapered to 150ng then jumped. It was not fun. I found a lot of support here but here I am now over 2 months from jump and I'm doing great . All acute symptoms have gone and the paws is 90% better. I still dont have great physical stamina but it's building .. You got this !!

 

[Mc83]

Lolwhatsdrugz - that's great about the cigarettes. I quit 2 years ago but this last withdrawal made me want to smoke so badly . I didn't but I got real close a few times.

 

[Mc83]

I am now over 2 months clean and feel healed from my lope ct. However now I have to get my gallbladder out and I am terrorized it will set me back into withdrawals. Am I being silly or are my fears justified?

 

[Chaley Tuna]

Hey guys - I too am going through lope withdrawal. I'm currently taking neurontin and got 7 hours of sleep on day 5 of withdrawal. I take my vitamins, neurontin, exercise, an eat pretty healthy. Has anyone else had any success with using neurontin during withdrawal?

Lastly does anyone have a timeline on how long this withdrawal will last? I've been taking lope off and on for over a year now and my highest dose - only done sometimes - was 144mg. For anyone going through this keep your head up, have a good support system, and get healthy!

-2na

 

[Numb19]

I am on day 17 ct off a 2 year 150-200mg day loperamide. How long was it until your malaise lifted? I'm am still fatigued. I will say having detoxes from ultram, fentanyl, and oxy respectively that lope was the worst. Any encouragement would be appreciated. I'm getting discouraged every day the mailaise doesn't lift

That's what I've also heard and it is likely due to lope's long half-life, which is 5-9 times longer than oxycodone.

 

[Hallucinogens R US]

It amazes me how little known there is about lope and the withdrawals associated with, tho the dependence is real!!

With its extremely long half-life the withdrawal symptoms can last weeks. For me it peaked at about 3 or 4 days and then was still really bad till 2 weeks later. But once the RLS faded away and I was actually able to get some sleep, I was ok with the constant chills and diarrhea.. I've heard of some (rare)cases where symptoms persist for up to 4-5 weeks. depends on how long you've been taking it and the amount, and how often.

 

[Hallucinogens R US]

I am on day 17 ct off a 2 year 150-200mg day loperamide. How long was it until your malaise lifted? I'm am still fatigued. I will say having detoxes from ultram, fentanyl, and oxy respectively that lope was the worst. Any encouragement would be appreciated. I'm getting discouraged every day the mailaise doesn't lift

Considering it had been going on for 2 years and a higher dose which you were taking, it doesn't surprise me that the malaise wasn't lifting even at 17 days. How are you doing now?

 

[myrandomchaos]

I just wanted to share my experience with loperamide. I began taking 10-30 pills a day 2-3 days a week, every other week or so in November to combat withdrawals from on/off (more on) use of stims and opiates for about a year. In December, I pretty much stopped and returned to my pills of choice. Then, in January, I stopped taking all other pills, and ramped up the lope by mid January to around 50-60 pills daily. By early March I was taking 70-90 pills a day. Finally, for about a 4 week time span from mid March to mid April, it progressively increased to ranges of 120-150 pills a day (PILLS, not MG!!!). The moment that finally woke me up was when I took 160 pills one day and 170 pills the next. I had such severe double vision, I was having difficulty driving and I hadn't had a menstrual cycle in over 3 months. I read articles about massive doses of loperamide having a possible link to Parkinson's like symptoms in animals and read a blog about a woman struggling to get off lope (http://madmargaret.wordpress.com/20...e-withdrawal-tips-on-surviving-the-addiction/) that took massive doses over a period of time and ended up in cardiac arrest, which her doctors believe may be correlated to massive doses of lope affecting conduction in the heart. ***I tried to find my original sources so I could link to the articles, but am having a hard time finding them. There is not much research available I suspect because loperamide was never intended to be taken in massive doses and few worried about abuse because of the erroneous belief that it cannot cross the blood-brain barrier.*** Never the less, I was terrified. I looked at my babies and realized that while the lope had allowed me to end a 1.5 year period of abusing pills to function, it was time to learn to function again without any chemical crutch.
I did a rapid taper from 140 pills a day to 60 pills a day over the next 2 weeks. By the end of May, I was down to 40-50 pills a day and today am averaging 20 pills a day. I have had slip ups, especially now that I am so close. Over the last 10 days, I have had one day of 40 pills, one of 100 pills and one of 60 pills. My worst issue initially was anxiety and depression, as the fog cleared and I realized how many horrible decisions I made while at the depths of my addiction. I think the high dose lope dulled all of that. It didn't make me feel "high" in the way that hydrocodone or oxycodone would, but it would give me this kind of warmth all over/energy/"everything is ok" type feeling. At this point, the worst symptoms I am dealing with are extreme cold sweats, usually about 20 hours after the previous dose, restlessness, significant lack of energy and difficulty sleeping. However, I started exercising again about a month ago and taking several supplements:
Fish Oil (am and pm)
Magnesium (am and pm)
Milk Thistle (am and pm)
Sam-E (am and pm)
L-Theanine (am and as needed throughout the day)
L-Tyrosine (as needed throughout the day)
Rhodiola Extract (1 in the am and another if needed during the day)
Ultra Mega Green Active whole food enhanced multivitamin (am)
Stress and Anxiety Supplement:
* am formula = vitamin B-6 and B-12, Folic Acid, 5-HTP and Suntheanine L-Theanine
* pm formual = vitamin E, Calcium, L-Glutamine, Valerian Extract, Grape Seed Extract, Melatonin
Hylands Calms Forte sleep aid (bedtime)
I also have benadryl available if I am really struggling to fall asleep that I will take sometimes and I have Hyland's Leg Cramps and Restful Legs that I take occasionally when having restless legs and/or leg pain.
I take Aleve or Ibuprofen as needed for pain.

Honestly, I feel somewhat like a wimp for not just jumping like some of you have, y'all are amazing! I am with my kids everyday and about to start working extra as well, and I am just terrified of getting thrown into horrible withdrawals. I am hoping that by starting to exercise again, trying to replenish vitamins and nutrients through supplements and healthy eating and taking natural remedies to address symptoms, I can make this as cushioned as possible. I just don't have even 1 day to hide under the covers and shut out the world and get through a withdrawal. I have to be able to function at a pretty high level in order to provide for my family. I sound like such a wuss compared to you guys and I hope you know how impressed and inspired I am reading your stories. There is such little information and resources available about this that finding this thread has been a huge source of motivation for me.
****I am not a doctor and I am not saying that my routine listed above is a perfect way to withdraw. Everyone responds differently and there are safety risks associated with taking supplements and all supplements are not created equally. I just wanted to post what seems to be helping me in case anyone else is interested in researching it further as a part of their recovery.
I am sitting at 20 pills a day and I am determined to be completely done by the end of the summer. I'm going to continue dropping 1-2 pills a day and pray the withdrawals continue to be mild. If anyone has any advice/questions/tips.......please ask. Reading this thread when I was at my worst is what finally gave me the motivation that this will not define or have power over me anymore! Good luck to all!

 

[Cane2theLeft]

^ for the 10,000th time I've said this on BL, it DOES cross the BBB. MOST of it is exported back by P-glycoprotein so at normal doses (2-6mg), there are no central effects. With large enough doses and/or P-gp inhibitors, enough stays across that it produces central opioid effects.

 

[myrandomchaos]

I agree with you that it does. Hence the statement "loperamide 'supposedly' doesn't cross the BBB" in the previous post. I was only hypothesizing that a possible reason it may be difficult to find much in the way of evidence-based information regarding loperamide abuse may be related to the fact that many erroneously believe there is no way to abuse loperamide because of the misconception that it cannot cross the BBB and will not produce central opioid effects. I apologize if I did not clarify that above. I also have a feeling that as more and more people come forward, more research will be done addressing short and long term risks associated with loperamide abuse.

 

[lolwhatzdrugs]

^ for the 10,000th time I've said this on BL, it DOES cross the BBB. MOST of it is exported back by P-glycoprotein so at normal doses (2-6mg), there are no central effects. With large enough doses and/or P-gp inhibitors, enough stays across that it produces central opioid effects.

I assume you're addressing me. I make you definitive proclamations but am very interested in the details of this dynamic, not just for loperamide and certainly not 'getting high' from this kind of drug, but more 'can WD be reduced from the beginning of treatment by a better understanding of this PNS/CNS dynamic?' and 'if so are there certain disease processes which show better results by altering this dynamic.'

This amount of crossing the P-Gp in inhibition/high doses you refer to isn't directly documented as far as I know. Everything that you say should be testable at what levels this is occurring. What I really want to see (again, I'm not disagreeing with your conclusion, this is just my idea of an empirical experiment to test it) is a design which could give you an idea of CNS over PNS effects for both analgesia and their relationship to cessation syndrome. There are probably experiments that measure analgesia specifically to see what disease processes methyl-naltrexone would help most with preventing side effects while not removing any analgesia mediated by the PNS.

Double blind crossover experiments measuring both acute W/D effects after weeks on a first line opioid - high dose morphine, and studies with other full mu opioid with longer half lives and higher binding affinities and longer half lives and shorting binding affinities (and vice versa). Maybe there are opioids that can be more correlated that have similar and different half lives/binding affinities and only their g-glycoprotein affinities are the controls but for this last group it seems that only loperamide/methyl-naltrexone are picked because of this feature. Maybe there are good agonists/antagonists that fall between these that just were never picked up for other undesirable features that would still be relevant for their mu agonism and analgesia effects.

Does loperamide (or methyl-naltrexone) have any appreciable affinities/method of actions for the multitude of receptors - kappa/delta ligands of every kinda class -agonist or inverse agonist/antagonist actions. Are their studies which have drawn correlation to affinities at these other receptors and analgesia/withdrawal. I thought I remember reading something along these lines that action at other receptors could very well be tied to why certain opioids have analgesia not removed from a naloxone challenge.


Your answer seems kind of terse, so maybe there is an experiment that gives all of these answers, or at least relevant ones that rule out further investigation and definitively answers some of the stuff I propose testing more thoroughly for. I also am unaware as to whether there are some selective kappa/delta ligands which could make some of these tests easy to carry out (like one single huge double blind study with a ton of designed pairs of the different ligands that would carry out the differential dynamics on paper.

A nice clean scatter plot on PNS agonism/antagonism and the same for the CNS correlated on a scatter plot with analgesia would clear this up definitively. Also tests with the drugs with very high specificity which are supposed to used for large chemotherapy molecules to make the P-Gp do our bidding tested - if it has a linear response curve measured against the other tests in slowly increasing doses across a fair sample size? Maybe different animals with different structured P-Gp systems (P-Gp with different specific ranges of binding if this exists? Or are they an identical membrane protein folded in the exact same 3D structure?) Maybe there are ways to linearly control and measure P-Gp expression linearly in various animals (like a gradient of a knock-out gene) to add another dynamic to this experiment?

Again, sorry if I'm ignorant of the literature and many of these things have been completely settled.

I also have a feeling that as more and more people come forward, more research will be done addressing short and long term risks associated with loperamide abuse.

You'd have to define loperamide abuse better. Is it taking it to stop W/D with no intention to get high, the standard definition of dependency (like I've never had the energy/nice feeling that regular opioids would provide that you seemed to experience). Is it only when you're trying to catch a buzz and W/D aren't in the picture? For this last category at least one person (or at least their mother has documented here) that they were opioid naive and ended up dying because they read they could get high. There are a few other people who thought they felt 'high,' I'd question what they were feeling *shrug*. Then there are tests with quinine and doses of loperamide that asked for subjective effects I believe but also got conclusive results doing pupil dilation tests (the pupils constricted indicated CNS effects in non-tolerant - opioid naive - individuals).

 

[Mc83]

Myrandomchaos- don't feel like a wimp for tapering and not jumping at a high dose. Some people can taper some people can jump from high doses. I never could taper so I had to jump. You are doing great, stick with it! It may take some time but you will be feeling better one day soon! I admire your determination to be able to stick to your taper!

 

[Mc83]

Considering it had been going on for 2 years and a higher dose which you were taking, it doesn't surprise me that the malaise wasn't lifting even at 17 days. How are you doing now?

Doing great actually 70 some odd days clean ( I have a calendar marking the exact days) I'm id say 95% normal or at least what I think normal was before I honestly can't remember exactly how normal should feel. I have a bad day occasionally and by bad I just mean I feel lazy nothing like the malaise of lope wd. The symptoms really started lifting about 30days then one day around day 45 or so I woke up and realized I hadn't taken a sleeping pill in days and hadn't had any rls. I can
Say that the lope has left 0 psychological attachments. I don't crave it or dream about it, I can walk past a 200ct bottle at the store and not even think about getting it so that's good. The best thing is my naturallibido is back after years of being suppressed during use and being enhanced during wd.

 

[Lorne???]

The doses you people are doing are insane. By using a CYP3A4/PPG inhibitor, you could literally cut your dose by 75%, and it would definitely help your bowels.

Seriously people, check out my posts on the loperamide mega thread. Taking over a gram of loperamide a week is restless and unnecessary.

 

[Lorne???]

^ for the 10,000th time I've said this on BL, it DOES cross the BBB. MOST of it is exported back by P-glycoprotein so at normal doses (2-6mg), there are no central effects. With large enough doses and/or P-gp inhibitors, enough stays across that it produces central opioid effects.

Yes, it is a misconception that it doesn't cross the BBB. It does, it's just that it's penetration is poor as to make it impractical under normal circumstances. The real problem is that it has a RIDICULOUSLY LOW oral bioavailability. However, with CYP3A4/PPG inhibitors, you can exponentially increase the bioavailability, thus exponentially increasing the amount that reaches systemic circulation.

This is not speculation: multiple studies have confirmed that 3A4/PPG inhibitors increase BA; the increase varies from 2x with a single, compound, up to 5x with 2 combined.

Of course, taking very large doses will send some across the BBB, but for me, I've taken high doses and never got significant relief, and the intestinal effects were unbearable.

But for me personally, using CYP3A4/PPG inhibitors, I have no problem getting CNS effects. Seriously, loperamide is far more effective than hydrocodone for maintanence, and this is from someone who IV's drugs, every single day.

 

[Awareness2014]

Absolutely legit!! I live with a person going through the same struggle. It sounds absolutely insane which is why word needs to get out there so these people can get REAL help for this problem.

 

[Awareness2014]

Somethings just wrong with having to take 150 pills of ANYTHING. You need to quit. Cold turkey should be fine. Don't even think about suboxone or methadone for Lopermide! LOL

Have you ever seen someone go cold turkey from Loperamide? It is EXTREMELY difficult for these people, especially when they are taking around 100 or more pills a day. The withdrawal symptoms last between 4-8 weeks and include extreme fatigue, weakness, diarrhea, pain, and depression. Yes, they absolutely need to quit but the nature of the drug ("harmless" OTC) isn't taken seriously by the medical community. It's embarrassing to these people so they almost never disclose it to their Drs either.

 

[Awareness2014]

I read probably 75 posts from 2 or 3 threads on loperamide. I decided to post my experience with this drug. In 2003 I was addicted to opiates and decided to quit (again). While researching what helps, what to expect, etc. during withdrawals (again) I came across a blog touting the benefits of using loperamide for the symptoms. The writer used the term "over the counter methadone". Here it is 5 years later and I have gone back and forth from rx opiates to Loperamide. This is embarassing, virtually impossible to get help for - no professionals have ever heard of or believe it - and for me, has been impossible to kick - due in part to it's price (one writer said $15.99 for 196 pills - the warehouses carry it even cheaper - and the fact that for me, the symptoms of wd are closer to methadone than hydro, etc. I don't know about the blood brain barrier and all that chemistry stuff (I've read it, but it's Greek to me). All I know is I do take ALOT of pills anywhere from 20 to almost 100 daily and occasionally have taken more. I've never done heroin, so I don't know if it's like that, but for me, it is similar to the painkillers I abuse. That is how bad my addiction is.


Moderator Note: In the past, we have has issues with loperamide threads. Any form of doucebaggory and flaming will get you warned, and eventually banned. I have unapproved a few posts in here, so consider this your warning. This is a harm reduction site, and we should try and help eachother out as productively as possible.

I don't know if you are still struggling with this but taking REALLY good multi vitamins (like GNC Men's Multi) and an iron supplement has helped my boyfriend with some of his withdrawal symptoms (from about 100 pills a day)(especially the diarrhea). It's still a LONG & sucky process! Good luck to all of you who are dealing with this. I think we need to get the word out to the medical community so these dosages can be studied so people know what kind of damage it's doing to your bodies, especially in the long term.