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Will Loperamide Prolong Withdrawals

Discussion in 'Opiate addiction' started by daudi81, Apr 15, 2011.

  1. daudi81

    daudi81 Silver Member

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    My friend realizes it's different for everyone, but has anyone successfully stopped using opiate related drugs using loperamide?

    He's read a few reports of people using it for the first few days of withdrawals, then stopped - and it cuts the pain down significantly - but they never report if the withdrawals came back since loperamide is technically an opiate too.

    Anyone have any experience on this?
     
  2. Rightnow289

    Rightnow289 Palladium Member

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    Pacman used loperamide on a daily basis and it did not ease his withdrawal symptoms apart from diarheoa. It did not put him back to day 1 of wd as it cannot pass through the blood brain barrier to tickle those opioid receptors.
     
  3. Der Alte Kreiger

    Der Alte Kreiger Newbie

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    The loperamide has been a godsend for my little dog, Dixie. She has WDed hundreds of times so she no longer has the fear of the unknown associated with WD. All thats left is the nerves, taken care of with benzos and the physical symptoms and the Loperimide takes care of about 75% of that.
    She says its still no picnic but quite bearable. In fact she gets plumb careless with her meds nowdays.
    Taking the Lope (gotta have a junkie slang word for everything) does not prolong the opiate WDs but now I got a really bad Lope jones, my habits up to 37 cents a day. (just kidding about the jones)
     
  4. daudi81

    daudi81 Silver Member

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    Thanks for the responses.

    Junkhead23 - How large were your doses? 30-40mg (15-20 pills) takes away nearly all of my friend's withdrawal symptoms. My friend is pretty sure some of it does pass the BBB - he's read a few reports and studies of a certain % crossing it in high doses (can't post links here, won't let me) - so it only makes sense that it does do something to the opiate receptors since it takes care of almost all W/D symptoms. Otherwise it would have to have some other mechanism by which it stops W/D symptoms - which I don't know?

    Der Alte Kreiger - you stated that it didn't prolong the w/d's, did you start using opiates again after the W/D's ceased - if so how long did you start using opiates again after the loperamide dosages? Reason I ask is that maybe the loperamide was still in your system whilst taking the opiates again - just a thought. If not then it would seem like loperamide indeed did stop the W/D's without prolonging them.
     
    Last edited: Apr 21, 2011
  5. Der Alte Kreiger

    Der Alte Kreiger Newbie

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    My little dog, Dixie sez: " Um, kinda a hard question as my life now is a cycle of simi planned addiction and withdrawal. I never let myself get really strung out and never have really bad WDs so its difficult to say but this last time I went about 20 days free from Opiates of any sort before hitting the starting gate again. A long boring 20 days with all the bright colours removed from the world, I might add

    I don't know a bunch about the chemistry involved but it seems to me that the Lope is enough of a different thing that it stops the physical WD symptoms without resetting the clock, YMMV."
     
  6. daudi81

    daudi81 Silver Member

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    Thanks for the response - maybe my friend will try lope again tomorrow if the W/D symptoms don't subside.

    He is coming off a big kratom addiction, and he was taking lope every 3 days which really helped him taper. Once he got completely off the kratom, he was taking lope every 2-3 days to help the W/D symptoms. On the 3rd day or halfway through the 2nd day - the withdrawal symptoms (anxiety, fatigue, etc) would return. He doesn't know if that's because he is still in Kratom W/D (he's almost on day 6), or if it's the lope resetting the W/D symptoms. After reading lots of posts and kratom withdrawal experiences, the anxiety and stuff should be gone by now, but it's not - so it's got him a little worried that it might be the loperamide.
     
  7. Der Alte Kreiger

    Der Alte Kreiger Newbie

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    Keep us posted on what you finaly decide about whether the Lope is causing reset, Dixie had nothing but good to say about it. She takes high doses, 10-15 pills for a week or so and then nothing.
     
  8. rokman nash

    rokman nash Palladium Member

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    Coming off dope I took massive ammounts(10-15 chewables a day). The only thing lopermide does is shut down the shit factory(and maybe make you a little drowsy), other than that it did nothing else for me.

    The shits were my biggest problem through my many withdrawls, so it definetly did its job. I have never heard of an instance of it prolonging WDS, but then again it never entered my mind.


    Good Thoughts:thumbsup:
     
    Last edited: Apr 21, 2011
  9. daudi81

    daudi81 Silver Member

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    After a little more research, most, if not all who have tried it, say that it does not prolong the w/d symptoms at all - so my friend went ahead and took 15 2mg pills this morning (30mg total). He will wait 2 days and if the W/D symptoms aren't gone yet he will take 10, wait 2 days, take 5-7, etc etc. We'll see how this goes.

    I'm really surprised more people don't try this. Maybe it only works on a select few. I guess my friend is lucky that it works wonders for him.

    rokman nash - maybe the chewables are different. My friend only has experience with the little 2mg tablets (really small turquoise things) - and 15-20 of them take away all of the symptoms 100%. Side effects are minimal - slight stomach cramping, slight constipation for a couple days, maybe a little nausea that lasts only a little while (but well worth it). He drinks plenty of water so he doesn't get too plugged up - he thinks that's the key to minimizing the side effects. Opiates + no water = constipation.
     
  10. Der Alte Kreiger

    Der Alte Kreiger Newbie

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    Not sure I understand your dosing intervals with the Lope. Dixie takes 10 or so at intervals three times a day as long as she needs them. The only drawback she could see is that she might never move her bowels again. she takes care of that by drinking citrate of magnesia as needed, Dunno if you are familiar with the stuff but the citrate would blast a hole through a 6" cement plug quicker than C4. She was a little afraid she might explode or something but it works well for her. Glad the Lope works for you.
     
  11. salgoud

    salgoud Newbie

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    No. Because like it was said before, it does not cross the Blood Brain Barrier. Even if it did, I don't think it would be a great opiate. IMO

    Opiate receptors are in the stomach and intestines. Janssen found a was to cure diarrhea without giving any high. To prolonging your W/D's, unless an opiate gets into the brain, you will have no W/D's. The opiates in the brain cause all the W/D symptoms. Amazing drug, loperamide, a strong opiate good for nothing but the craps. Helps for a while. Those little opiate receptors get a tolerance too. I wonder how much that patent brought in for the Janssen chemist.

    It is the number 1 anti-diarrheal, that works great, that won't get you addicted. Lomotil, does cross the blood brain barrier, and if enough are taken, they will eliminate some of the W/D's

    Some info: When loperamide first came out it was a Schedule V, then they found there was no abuse with it.

    Loperamide is a necessity in your W/D kit. Maybe some Clondine (.1,.2 and .3 mgs), some promethazine and lots of toilet paper if you don't use your loperamide.

    salgoud
     
    Last edited: Apr 1, 2012
  12. daudi81

    daudi81 Silver Member

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    Here is what my friend told me:

    "I realize loperamide is just meant for anti-diarrheal, but there has to be some component that hits other receptors in the brain or something. It's not a coincidence that within 30minutes to 1 hour after taking 10-30mg of the stuff that the physical symptoms all but disappear. It's definitely NOT a placebo either - there is a very very noticeable relief of w/d symptoms (severe anxiety, chills, sweats, the usual...all gone). It almost gives me the relief as if I were taking more kratom - without taking any. I know I'm not the only one because I've read similar reports all across the web - whilst others say it doesn't work on anything but the diarrhea. I guess people just respond differently to different drugs."
     
  13. TheBigBadWolf

    TheBigBadWolf Cold Member Palladium Member Donating Member

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    About Loperamide crossing the Blood-Brain-Barrier I found that one:
    from:
    Delivery of Loperamide Across the Blood-Brain Barrier with Polysorbate 80-Coated Polybutylcyanoacrylate Nanoparticles

    Renad N. Alyautdin, Valery E. Petrov, Klaus Langer, Achim Berthold, Dimitry A. Kharkevich und Jörg Kreuter

    I know this was not the OPs question, just to show that under special circumstances loperamide CAN cross the BBB.

    IMO the interaction of loperamide and the opiate receptors in the guts are big enough to suppress withdrawal symptoms (partly).
    from
    Sadeque AJ, Wandel C, He H, Shah S, Wood AJ (September 2000). "Increased drug delivery to the brain by P-glycoprotein inhibition". Clinical Pharmacology and Therapeutics 68 (3): 231–7.

    I found mentioned that the also the use of verapamil, ketoconazol and ritonavir can make loperamide cross the BBB.

    TBBW
     
  14. Poet51

    Poet51 Silver Member

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    Poet knows a poet who is a service-connected Disabled Veteran. He suffers from chronic pain due to a leg injury. The VA sends him 180 5mg tablets of Oxycodone each month. He’s been taking the Oxy for several years now. It helps him to workout and get through the day at work, however, it also makes him drowsy and sometimes moody, and sometimes he runs out two weeks early because he takes much more than what’s prescribed. He’s suffered through some withdrawals that caused him to miss time from work. He doesn’t want to stop taking his OXY because of its benefits, however, he isn’t too fond of the withdrawals. After some on-line research, he read about Loperamide. So, Poet decided to stop Cold Turkey Thursday night. He did have some Oxy ready in case the withdrawals were too bad. Thursday he took a total of 70mg, with his last dose coming at 2100 Thursday night. He did not have to work Friday, so he slept in until 0930. He had cold sweats when he woke up and he felt fatigued and achy all over. Within in an hour, he started feeling much worse. Immediately, he took 40mg of Loperamide and some L-Tyrosine. Within 30 minutes, most of his withdrawal symptoms were gone. He felt a little tired but that was it. He took 40 more MG’s of Loperamide Friday evening and then 40 more this morning when he woke up. He has suffered virtually no withdrawal symptoms, including depression, which for him was the worse side effect from withdrawal. He has experienced no craving to take more OXY. In the beginning, Poet was skeptical, but no longer is that the case. He’s very pleased and in a few more days, plans to discontinue all Loperamide.
     
  15. salgoud

    salgoud Newbie

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    Not that I don't agree this happened, 140mgs of loperamide, then 40mgs, 40mg and another 40mg. Some will enter the brain depending on what he is eating and what enzymes he possesses in his liver.

    It is a great story, Buddy has tried it himself with Quinine to no avail. Loperamide not being able to cross the Blood Brain Barrier, I am curious how this was accomplished without nanoparticle intervention. However, I will admit, 300 mgs of loperamide is a lot. Maybe the trick is to saturate oneself with the drug. Bravo for this man who kicked 180 5 mg oxycodone with loperamide. Maybe by saturating the body, some can cross the BBB.

    salgoud
     
  16. Descartesx

    Descartesx Newbie

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    Loperamide DOES enter through the blood-brain barrier. But as soon as it does, it is removed by P-glycoproteins. The idea with loperamide is to take doses around 30mg- 3 times a day. This is because there is only a finite amount of Pgp that the body can make at a given time and using enough loperamide will saturate the proteins, so that any other loperamide molecules will not be removed.

    It may also be noted that a lot of users have noticed Loperamide easing nearly all of their withdrawal symptoms- enough for them to maintain on, but it does have its own nasty WD, apparently.
     
  17. Mindless

    Mindless Gold Member

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    As DescartesX has said, loperamide is removed from the central nervous system via p-glycoprotein efflux. I do wonder if whether the benefits ascribed to loperamide in withdrawals are more a result of the individual's strength and detemination, rather than the effects of this drug. Adventures in attempting to use loperamide as a centrally acting opioid have met with mixed results. In one study quinidine was found to allow loperamide to exert central activity. As far as I know, this is the only study that has successfully done so with human subjects:

    'Loperamide is a potent opiate that is widely available without prescription as an antidiarrheal. Absence of analgesic efficacy, respiratory depression, or impairment of CO2 response reflects its normal lack of CNS effects, which appears to be due to the fact that it is a P-glycoprotein substrate that is so efficiently removed from the CNS by the P-glycoprotein efflux pump that pharmacologically effective concentrations are not normally achieved in the CNS. We found that the inhibition of P-glycoprotein by quinidine resulted in respiratory depression after administration of loperamide that was not seen after administration of loperamide alone."

    Increased drug delivery to the brain by P-glycoprotein inhibition. Abu, J et al. 2000.

    One of our members had some results by using black pepper, containing piperine. iamamangod's experiences can be seen in this thread. There is evidence that piperine is a potent cytochrome inhibitor as well as a P-glycoprotein inhibitor.

    Sources:
    Piperine, a Major Constituent of Black Pepper, Inhibits Human P-glycoprotein and CYP3A4 Rajinder K et al 2002:
    http://jpet.aspetjournals.org/content/302/2/645.full
    Biochemical basis of enhanced drug bioavailability by piperine: evidence that piperine is a potent inhibitor of drug metabolism. J Pharmacol Exp Ther January 1985 232:258-262

    "since Piperine can influence drug levels of a number of drugs, care should be taken when using with other drugs whose levels are influenced by it. It can potentiate the efficacy of drugs hence, dose reduction is required to prevent toxicity. The list is still being researched and updated.”

    Source: Bioenhancers: Revolutionary concept to market Navin Atal and K. L. Bedi1 J Ayurveda Integr Med. 2010 Apr-Jun; 1(2): 96–99.

    Inhibition or induction of P-gp by coadministered drugs or food as well as herbal constituents may result in pharmacokinetic interactions leading to unexpected toxicities or undertreatment. On the other hand, modulation of P-gp expression and/or activity may be a useful strategy to improve the pharmacological profile of anticancer P-gp substrate drugs.”

    Source: Concise Review: Clinical Relevance of Drug–Drug and Herb–Drug Interactions Mediated by the ABC Transporter ABCB1 (MDR1, P-glycoprotein) Marchetti S, Mazzanti R, Beijnen JH. 2000.

    And as TheBigBadWolf has already said, a ploysorbate80 solution has been used to achieve a very short lived analgesia in mice, although "Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain."

    Source: Delivery of loperamide across the blood-brain barrier with polysorbate 80-coated polybutylcyanoacrylate nanoparticles. Alyautdin RN et al 1997. PMID:9098875

    Using Loperamide off label, especially with drugs or substances which alter it's metabolism, can be dangerous. There are no safe dosing guidelines available beyond the use of up to 16mg daily in divided doese, and it is important to remember than loperamine is a potent opioid when central activity is possible. This could lead to overdoses. It may be risky to tamper with the action of p-glycoprotein, it serves to keep unwanted matter and infections such as bacteria out of the central nervous system.

    Taking heroic doses is also potentially dangerous. Cooe's experience of overdose and subsequent problems with treatment illiustrates the risk in this post. My own impression is that the only benefit of loperamide in withdrawals might be the treatment of diarrhoea. If taking more than the recommended amounts of loparimde adverse effects are also more likely. These may include "abdominal cramps, dizziness, drowsiness, and skin reactions including urticaria (skin rash); paralytic ileus (intestinal obstructions) and abdominal bloating also reported."

    Source:British National Formulary 63 March 2012.
    .
     
    Last edited: Mar 31, 2012
  18. (NS)-M-Lo-Reason

    (NS)-M-Lo-Reason Titanium Member Donating Member

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    I want to bump this thread and ask for an update. My manticore has been taking large amounts of kratom for a month, up to 24 gms per day in 6 gm doses. He wants to stop because he wants to be clean, but he has to be able to function and, although the withdrawal is a joke compared to morphine withdrawal, he's kind of a wimpy manticore and the desire to punch walls and scream is not something he enjoys. Plus he's home for the first time in 6 months and his parents have no idea how to deal with his moodiness and explosive anger. He drank last night and that helped, but he woke up with a hangover and an affirmation of his serious hatred of ethanol.

    Anyway, please don't bother saying that loperamide doesn't help with withdrawals. In manticores it does, and if it's placebo he doesn't care because he feels a lot better. He's taking a small pawful and it makes him feel fairly normal and a little bit strange (specifically heaviness in his front legs and kind of a pleasant cheerfulness. This is with no Tagamet or anything else. He's currently on it right now and wants to continue using it for the duration of the kratom withdrawal and then stop. Above poster:

    What did you experience? Did the withdrawals continue on? My manticores experience is that kratom withdrawal lasts about a week, although by day 5 it's mostly anxiety and restlessness. Is it feasible for him to just keep taking lope for a week and then stop?
     
  19. hypernihl

    hypernihl Titanium Member

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    In my experience No, it did not prolong withdrawals. Last year when I was using oxymorphone heavily, I went cold turkey a few times, then started using small doses of Kratom (1 gram 3-4 times per day), and then finally settled on using loperimide (8 mg) + quinine (100 mg) (the quinine helping the loperamide cross the blood brain barrier) once per day.

    Cold turkey oxymorphone withdrawal typically lasted 3-5 days for me. I did not find low doses of Kratom or loperimide + quinine to extend the withdrawals at all. At the low doses I was not 100% comfortable, but it really took the edge off ~80% comfort without extending withdrawals beyond a cold turkey withdrawal.

    All that aside, loperimade alone should not extent your withdrawals.
     
  20. (NS)-M-Lo-Reason

    (NS)-M-Lo-Reason Titanium Member Donating Member

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    Thanks a lot hyper. My manticore broke down and took some ridiculously overpriced head shop branded kratom yesterday (and he feels guilty about even supporting that shit, considering it says things on the bottle like "take 3-5 capsules with full glass of water" "satisfaction guaranteed" "do not operate heavy machinery" "do not take more than 10 capsules in a 24 hr period" "do not take kratom every day". It forgot to include "fuck you FDA and your approval for human consumption, we don't need your blessing to sell unapproved drugs, it's not like your a government agency constantly on the lookout for legal highs". Honestly why the hell do these companies feel the need to ruin a good thing. Start stockpiling kratom because it will be outlawed shortly.) Anyway.

    He's taking what Dixie the dog did (manticores are related to dogs, being Carnivora and all), that's 30 mg of loperamide 3x daily. He will report back but it's making the anxiety and shitty mood much more bearable. Good to know that it isn't a case of having to go through it sooner or later. He really wants to stop, it's expensive, makes him feel shitty after 4x daily dosing, and he's going to get found out and his parents don't deserve it they think he's sober. Anyway peace all.