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The Plausible Truth about Loperamide
  1. #1
    TeaLikesMeFL is offline New Member
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    Default The Plausible Truth about Loperamide

    Hello All,


    I have been doing a lot of research about loperamide (immodium) and the possible reason(s) why some people can get relief from withdrawal, while others can't. On 5 of the 5 forums I use for some information regarding experiences, the loperamide topic is highly debated, and hotly contested. What I say here has obviously (hopefully you've realize that) not been tested in a lab, or in study groups. It is just an educated guess and hypothesis given the amount of information I have attained.

    I, to, am physically dependent on opiates. Like yourselves, I also have a curiosity. If half of you are like me, you do thorough research before you try something new. I hope to have a go-to guide for loperamide for all users on this forum. Most, if not all, know what loperamide is, so I'll try my best to not be redundant.

    Loperamide FAQ:
    1) Does it cross the BBB?
    Yes! In healthy individuals, there was an extremely low concentration (source:1)
    2) Does it alleviate W/D?
    For me, yes. For you? Maybe.
    3) Won't it clog me up for x amount of days/years/eons?
    No more than oxymorphone, methadone, or fentanyl
    4) Are there side effects?
    I've read that in some cases - dosages higher than 140mg+ daily for extended periods of time (>4 wks) can lead to QT prolongation and ventricular tachycardia. Everyone is different. Could have been a drug induced even
    5) How to potentiate loperamide?
    I don't suggest doing that. Loperamide should not be used like that. If you read the 1st citation, you can see that there may be other factors that contribute to the low BBB diffusion.

    Question: If loperamide crosses in such an extremely small concentration, why do my W/D symptoms disappear?

    Hypothesis: We all should know that we have different DNA to an extent. You have beautiful blue eyes and brown hair. I have brown eyes and black hair. That's the different expression of genetics. To extrapolate this to the effect of crossing the BBB, you may have many more little pumps on your BBB than I do. That too is controlled by nothing more than genetics and feedback. The BBB are cells that have evolutionary adaptations that keep your brain healthy. Some of these adaptations include a very high electrical resistance (ability of electric current to flow through cells), tight junctions which are almost impermeable to fluid, and little tiny proteins ALL over these cells called MDR1. MDR1 = Multi Drug Resistance Protein 1. To you, p-glycoproteins. We obviously know that the other non central symptoms are alleviated with loperamide dosage.

    If I take 32 mg of loperamide and my W/D goes away we know that something is happening. Loperamide is actually a very strong opioid. What people may misunderstand is binding affinity and intrinsic activity. Having a high binding affinity and low intrinsic activity (naloxone) will put someone into precipitated withdrawal. Having a low binding affinity and high intrinsic activity will be almost worthless. They are called inverse agonists. We know that loperamide has a high binding affinity. Based on that, if even a few micrograms pass through the BBB, the intrinsic activity has to be high to produce an effect on the u-op receptors. My educated guess is roughly about the same IA as fentanyl.

    Question: Is there a way to get loperamide to cross in high doses?

    Answer: Yes. It's stupid. I'd much rather you take lortabs then try your hand at kitchen chemistry.



    Question: Will taking buprenorphine send me into Precip. W/Ds?

    Answer: If you have been taking loperamide for an extended period of time (>2 weeks) at dosages above 50mg, you will go through PWD. Loperamide has a half life of about 14 hours. If you load up on loperamide, the receptors will be saturated for some while.
    If you have been taking loperamide for short term (<3 days), at lower dosages (<30mg) you will have mild PWD. Gastrointestinal problems and other non-central effects. The extent will be different for everyone. Some may just need a replacement toilet, while others may need to wash their sheets as well.


    P.S. - Loperamide can greatly affect your tolerance. I know saying this is preaching to the choir, but moderation is key.

    In closing, if anyone has any questions please post them.
    Last edited by Anonymous; 04-10-2018 at 05:33 PM.

  2. #2
    blindbraille is offline New Member
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    Quote Originally Posted by TeaLikesMeFL View Post

    Question: Is there a way to get loperamide to cross in high doses?

    Answer: Yes. It's stupid. I'd much rather you take lortabs then try your hand at kitchen chemistry.



    Question: Will taking buprenorphine send me into Precip. W/Ds?

    Answer: If you have been taking loperamide for an extended period of time (>2 weeks) at dosages above 50mg, you will go through PWD. Loperamide has a half life of about 14 hours. If you load up on loperamide, the receptors will be saturated for some while.
    If you have been taking loperamide for short term (<3 days), at lower dosages (<30mg) you will have mild PWD. Gastrointestinal problems and other non-central effects. The extent will be different for everyone. Some may just need a replacement toilet, while others may need to wash their sheets as well.


    P.S. - Loperamide can greatly affect your tolerance. I know saying this is preaching to the choir, but moderation is key.



    In closing, if anyone has any questions please post them.

    First, he doesn't know how to potentiate loperamide, he doesn't know how to get it to cross the BBB in higher doses. Despite the medical jargon this person is spewing nonsense. There are many sites that describe potentiation of this and many other drugs. There are biochemical antagonists that im sure you could use and abuse to help loperamide cross the BBB but again it's obvious this person has no idea how. For two reasons, one, describing how to get this reaction isn't tantamount to telling someone to do it. You can't be held responsible for providing information if that information is used improperly. This was established years ago specifically in regards to the Internet and freedom of information act. It could only have helped his credibility if he had described how to potentiate it. That he didn't just shows how full of >>>> he is. Secondly, and more importantly BUPE DOESN'T PRECIPITATE EARLY WITHDRAWAL! Suboxone has an additive to the BUPE that induces w/d symptoms because it's a rapid detox drug. Idk if it is narcan or a similar drug. This is why subutex is the preferred source of bupe for addicts. Because you can take it after having taken whatever other opiate and NOT go into w/d. That this person doesn't know this simple fact shows that for all his lingo and pretending to know wtf he's talking about he has zero clue. The only thing he said that was true, inside all of that "genetics and dna" >>>> is that yes, everyone is affected differently. But everything else he said is complete and utter nonsense.
    Last edited by Anonymous; 04-10-2018 at 10:19 PM.

  3. #3
    AliciaMarie is offline New Member
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    Default Bupe and pwd

    Quote Originally Posted by blindbraille View Post
    First, he doesn't know how to potentiate loperamide, he doesn't know how to get it to cross the BBB in higher doses. Despite the medical jargon this person is spewing nonsense. There are many sites that describe potentiation of this and many other drugs. There are biochemical antagonists that im sure you could use and abuse to help loperamide cross the BBB but again it's obvious this person has no idea how. For two reasons, one, describing how to get this reaction isn't tantamount to telling someone to do it. You can't be held responsible for providing information if that information is used improperly. This was established years ago specifically in regards to the Internet and freedom of information act. It could only have helped his credibility if he had described how to potentiate it. That he didn't just shows how full of >>>> he is. Secondly, and more importantly BUPE DOESN'T PRECIPITATE EARLY WITHDRAWAL! Suboxone has an additive to the BUPE that induces w/d symptoms because it's a rapid detox drug. Idk if it is narcan or a similar drug. This is why subutex is the preferred source of bupe for addicts. Because you can take it after having taken whatever other opiate and NOT go into w/d. That this person doesn't know this simple fact shows that for all his lingo and pretending to know wtf he's talking about he has zero clue. The only thing he said that was true, inside all of that "genetics and dna" >>>> is that yes, everyone is affected differently. But everything else he said is complete and utter nonsense.
    By your own logic everything you have said is complete and utter nonsense. It's not the nalaxone that sends you into withdrawls, it's the bupe itself. I really hope nobody has listened to the cap you posted. If you take subutex or suboxone too soon after opiates it most definitely will send you into pwd. Done it with both and it was horrible.

  4. #4
    Alltoward Infinity is offline New Member
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    "May cause drowsiness", says so right in the bottle, and sure enough -- moderate doses have put me to sleep (like 12-16 mg.). Therefore it's obvious that some if it does cross the BBB. But loperamide isn't exactly my top recomendation for withdrawal. And that's only because it does zero -- zilch -- for the mental depression & lack of energy component. So I don't think highly of clonidine, either, for the same reason.

  5. #5
    cjo777 is offline New Member
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    Alicia my friend I hate to break it to you but bupe DOESN’T in ANY way shape or form send you into withdrawals. It’s the nalaxon they add to bup in many different meds now that strip the receptors in your brain and cause withdrawals. The only way bupe can mess up your high is it messes with your tolerance. I take bupe EVERDAY and I take other opiates to and all burp does for me is increases my tolerance and KEEPS me (and anyone else taking just bupe without the nalaxone) from going into withdrawals! Seriously it would take you 5 min of research to read ANYTHING about it from the MEDICAL community (not blue light and other forums where it’s just ppl talking) to confirm these FACTS I have shared with you. Please know wtf your talking about before you spread even more disinformation around to ppl who might just take what your saying on face value!

  6. #6
    cjo777 is offline New Member
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    Quote Originally Posted by Alltoward Infinity View Post
    "May cause drowsiness", says so right in the bottle, and sure enough -- moderate doses have put me to sleep (like 12-16 mg.). Therefore it's obvious that some if it does cross the BBB. But loperamide isn't exactly my top recomendation for withdrawal. And that's only because it does zero -- zilch -- for the mental depression & lack of energy component. So I don't think highly of clonidine, either, for the same reason.
    Infinity clonidine is used to help your blood pressure during withdrawals. It has some minor effects on some of those side issues but the main reason they give it to you is to keep your bp stable which in turn has some minor help with other systems. They use this one over other hypertension meds is make most ppl very drowsy and sleeping through the worst of the dt is better than nothing. Hope you understand better now

  7. #7
    Randy35 is offline Platinum Member
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    Quote Originally Posted by cjo777 View Post
    Alicia my friend I hate to break it to you but bupe DOESN’T in ANY way shape or form send you into withdrawals. It’s the nalaxon they add to bup in many different meds now that strip the receptors in your brain and cause withdrawals. The only way bupe can mess up your high is it messes with your tolerance. I take bupe EVERDAY and I take other opiates to and all burp does for me is increases my tolerance and KEEPS me (and anyone else taking just bupe without the nalaxone) from going into withdrawals! Seriously it would take you 5 min of research to read ANYTHING about it from the MEDICAL community (not blue light and other forums where it’s just ppl talking) to confirm these FACTS I have shared with you. Please know wtf your talking about before you spread even more disinformation around to ppl who might just take what your saying on face value!

    I realize this is an older thread, but.....

    No, on the other hand it's you that's totally and without question wrong. Alicia is absolutely correct, it's the Buprenorphine that will send you into precipitated withdrawals. The only reason Naloxone is added to Suboxone is to deter IV addicts from abusing the drug. The Naloxone has no other benefit.

    Case in point: If what you say is true then what about Subutex (pure Buprenorphine without Naloxone added). Take it too soon after stopping another opiate and you'll find out. It has no Naloxone so how could it send someone into PWD's? Answer is, it can't because IT'S THE BUPE THAT PUTS YOU INTO PWD's and NOT THE NALOXONE.

    The good people on these forums that have used Suboxone/Zubsolv, etc know what the difference is. Thousands have used subs on these forums and know the real truth.

    I only hope some poor soul doesn't read your post and go into PWD's. That would be a real shame.

    Randy
    Beefaroni7272 likes this.

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