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Drug Addicts Only! Loperamide (Imodium)

Discussion in 'Opiates & Opioids' started by TheBlackPope, Oct 22, 2007.

  1. TheBlackPope

    TheBlackPope Newbie

    Reputation Points:
    Apr 16, 2007
    If your not a drug addict get the hell out of my thread! ...Or continue reading to see how the lowest life forms on earth operate.

    Alright my fellow scum sucking junkies... lets get to work.

    The point of this thread is simple...it is a necessity for our kind to inebriate ourselves anyway possible... and I think I need to experiment w/ this for myself.

    Imodium, availible OTC containing the drug Loperamide, an opiod receptor agonist. may be my new best friend.

    This drug can not cross the motherfucking blood brain barrier because of the same reason that psuedoephedrine cannot pass it either!

    BUT! According to the wikipedia:

    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.

    Thus I wikid polysorbate 80:

    Polysorbate 80 (commercially also known as Tween® 80, a trademark of Uniqema/ICI) [1] is a nonionic detergent and emulsifier derived from polyoxylated sorbitol and oleic acid, and is often used in foods. Polysorbate 80 is a viscous, water-soluble yellow liquid.

    And came to the following conclusion.

    I can alter my conciousness just one more time by taking imodium w/ tween.
    I plan to mass order Imodium and Tween80, extract the loperamide w/ iso and have myself an experiement.

    I will find out how many mg os lope does it take one to get sorta high, moderatley high, and extreamly high.

    Any comments, suggestions, criticisms, etc?

    And BTW, who can guess which drug I am currently on.

    I am on a high dose of it and you could probally figure it out by reading the post.

    This plan will work out if I can get a job...those dirty****at the Apple store dont want to hire a multi-felon...
  2. hoodabudda

    hoodabudda Newbie

    Reputation Points:
    Apr 1, 2007
    you should read these threads. they have a massive ammount of information https://drugs-forum.com/forum/showthread.php?t=29374&page=3
    loperamide would also need to be coated on the molecular level with polysorbate 80, which would require a centerfuge. also I had abused loperamide extensively by smoking the powder on top of marijuana. opiates are potentiated by marijuana around the 6x range in terms of pain relief. swiTBP need not order it offline, I got a shitload of loperamide by buying generic bottles of 96 2mg tabs and extracting with iso. the boxes have 24, so buy the generic bottles. the smoked loperamide with marijuana doses are the same as oral hydrocodone(im not kidding)
    Last edited: Oct 23, 2007
  3. Pennyroyaltea

    Pennyroyaltea Newbie

    Reputation Points:
    Apr 24, 2010
    from U.S.A.
    Loperamide? Really? I guess so.

    I have been reading all about potentiators for a while. I have tried GFJ without concrete results. I have no source for "pool toys" to swim with lately, so I have been doing kratom capsules a few times a week. I decided that it was worth a shot to try to potentiate Swim's Kratom with some loperamide and some tagamet.

    1 2mg loperamide and 1 tagamet a couple hours before (Swim drank a grape fruit juice and tonic water cocktail too for good measure) taking just under 20 grams of kratom.

    Usually, Swim needs at least 30 grams of kratom to feel great and the buzz is very fragile and short-lived. Last night was different for Swim. I was high for hours and even ate a giant meal in the middle of it that did not decrease the buzz as much as it would normally. So I decided to attempt an experiment this morning. I took one tagamet and just over 40 mg of loperamide and I have been feeling a pretty nice codeine/tramadol-esque buzz for hours now.

    Swim certainly thinks that withdrawals will never be the same.
    Last edited by a moderator: Jun 6, 2015
  4. diffs

    diffs Silver Member

    Reputation Points:
    Jul 31, 2009
    from U.K.
    Well You may know more about chemistry, but I think its a bad idea. 4mg may stop diarreha, but might do damage when it crosses BBB. Its up to You and as I say he doesn't really know much about chemistry. Swim thinks You is better sticking to ready made drugs and if you run out buy some poppys (legally bought online) and make some tea. Anyway, thts just swims 2 cents

    Good Luck, let us know what happens.

    EDIT: OK didnt notice the dude has been banned. Wonder if it worked or if he just wont be able to shit for a week?
    Last edited: Apr 26, 2010
  5. Pennyroyaltea

    Pennyroyaltea Newbie

    Reputation Points:
    Apr 24, 2010
    from U.S.A.
    I tried loperamide a few months back when I had just gotten clean.

    I didn't want to get clean, but swim's doctor took swim off bupe and I live in an area where I has no idea where to get opiates. I had started trying kratom. Swim liked it just fine, but hated how brief the buzz was.
    Swim read about potentiation. I couldn't believe that I have been using opiates off and on for ten years without hearing about all this shit that I was reading about on these forums. swim also, hated swimself for not finding this stuff out when I was wding off suboxone. So swim potentiated kratom by taking a couple loperamide and some tagamet 2 hours before gulping down about 30 kratom capsules and I was stoked and high for 6 or more hours instead of the normal 2 hours tops from kratom.

    Now, mind you, swim's tolerance was lower than ever and kratom was working back then (this past spring). I decided to eat a shitload of loperamide the next day. Swim's girlfriend and he took about 30 2mg pills each and they got high all day.

    She was sick from it for a couple days, but I felt amazing. I took lope a few more times here and there and it only eliminated wd symptoms (completely) but didn't produce a high.
    Swim discovered pods. Swim likes pods, but most places are either completely out of pods or they have jacked their prices so high that it isn't worth it. So now I am forced to go without any opiates due to the pod price and the fact that I don't know anywhere to get opiates. (I would go get suboxone, but cant afford it either since insurance got dropped).

    So I started taking loperamide. A couple months ago, swim's friend was back on H and needed to get off. Swim told his friend to take 60mg or lope, skip a day, then take 30mg. skip a day and so on and so one until it was zero.
    Swim's friend managed to kick his h habit in a week without any wd's. Swim suggested this to other folks too and they used it to tide them over for a day or two without their doc.

    So now I am in the same boat and the loperamide buzz is weird. First of all, I started to feel wd's 3 mornings ago. I took 32mg of lope. wd's symptoms were gone mostly for roughly 48 hours. Then I took around 100mg and waited. 3 or 4 hours after taking this massive dose, I was pretty content and swim's girlfriend said: "hey, Swim. Are you high right now?" I had to ask swimself the same question.

    Oddly enough, its a head high and not really a body high. Mostly a tired buzz, not really the same as other opiates, but certainly triggering opiate receptors in the brain. Kind of equivelant to taking 40mg of hydrocodone with a low tolerance, plus it lasts a very long time. Swim misses real opiates.

    Swim ordered some pods and they will be a real expensive and lame party that arrives in a few days. But at least swim knows that wd's are no longer the problem they used to be. Swim wishes he had known all of this back in february when he kicked his habit cold turkey. 2 weeks of hell could have been avoided.
    Last edited by a moderator: Jul 7, 2013
  6. 1Luckyj

    1Luckyj Silver Member

    Reputation Points:
    Sep 30, 2008
    from U.S.A.
    How could this old research have been overlooked?...ought to spark some ideas...

    Central analgesic actions of loperamide following transient permeation of the blood brain barrier with Cereport™ (RMP-7)1

    Dwaine F. Emericha, Pamela Snodgrassa, Melissa Pinka, Floyd Bloomb and Raymond T. Bartusa, c, *
    a Preclinical R and D, Alkermes, Inc., 64 Sidney Street, Cambridge, MA 02139, USA
    b The Scripps Research Institute, La Jolla, CA 92037, USA
    c Tufts University Medical Center, Boston, MA, USA
    Accepted 25 May 1998. Available online 9 September 1998.
    The bradykinin analog, Cereport™ (RMP-7), was designed to increase permeability of the blood brain barrier (BBB). Over the past several years it has been developed primarily as a means of increasing permeability of the blood brain tumor barrier, where early evidence indicated a particularly robust and reliable effect. The present series of experiments were intended to determine whether Cereport might also be used to increase delivery of pharmacological agents across the normal (i.e., non-tumor) BBB. This was accomplished by testing the ability of Cereport to enhance delivery of the peripherally acting opiate agonist, loperamide, to the brain, as evidenced by induction of a centrally mediated analgesic effect. Intravenous administration of a combination of Cereport and loperamide produced a significant analgesic effect (2-fold increase in response times) when animals were tested on a hotplate apparatus. Loperamide alone did not produce analgesia. An analysis of the time course of analgesia revealed a graded onset of analgesia which peaked at 30 min, maintained asymptote at 60 min, and began to diminish by 120 min following Cereport and loperamide administration. Finally, the analgesic effects of combining Cereport and loperamide were completely blocked when animals were pre-treated with the opiate antagonist naloxone, demonstrating that the analgesia was mediated through opiate receptors. Collectively, these results suggest that Cereport was able to increase delivery of loperamide across the BBB, allowing it to gain access to opiate receptors in the CNS to produce a centrally mediated analgesic effect. They therefore provide clear evidence that safe and well-tolerated doses of Cereport can increase permeability of the normal (i.e., non-tumor) BBB. Moreover, they provide the first evidence of a pharmacological effect specifically enabled by controlled (i.e., receptor-mediated) modulation of the BBB.
  7. ChiselD

    ChiselD Silver Member

    Reputation Points:
    Sep 28, 2009
    31 y/o from U.S.A.
    So I've been toying w/ this idea, as many others have...I have been trying to get off opiates again, except I find the fear of w/ds keeps me using instead of trying to get clean...anyways, no drugs to buy, so I downed some immodium...however, I DO have mannitol, pomegranate juice and extracts...now, surprisingly enough my w/ds did go away...could be placebo, but I even woke up, not feeling SUPER awesome, but not feeling super depressed n what not...anyways, does anyone know what I would have to do to get the mannitol working properly to allow passage of the drug thru the (hopefully)permeable BBB? In a rush, hope anyone can shed some light...mannitol was easily found years ago, but never had too much testing w/...also, was NOT constipated this morning, after eating 20-30 mgs of lope
  8. &rew


    Reputation Points:
    Sep 15, 2010
    from earth
    Taking loperamide will help only with diarrhea all other is just placebo. There was studies that showed that loperamide 520 times stronger in binding on receptors before BBB that binding to receptors after BBB. Getting high or remove WDs required opioid to cross BBB, all "right" receptors grows after BBB. If it helps with diarrhea with two tablets then to get same help on central nervous system one should take 1040 tablets. 1040 is an open way to get retention of feces then it fast grow into blocking of digestive system. And next is surgeon's scalpel.

    There was guy who tried to eat 20 tablets after reading another thread about miracle loperamide. All story ended with gastric lavage on second day. On WDs it wasn't so pleasant.
  9. psycronizer

    psycronizer Newbie

    Reputation Points:
    May 29, 2011
    47 y/o from new_zealand
    ok...I have my own take on this, and its not some half arsed dribble that u all seem so intent on perpetuating....no..this is serious science for the serious junkie. For those of you with some knowledge (ok, a lot) about the chemistry of opioids read on-the rest,leave now. ok fellas, have a gander at the structure of Loperamide.....do you know your history about the analogs of the diphenylheptanes that Jansen et al conjured up? u know, the methdones,dextromoramides,dipipanones, propoxyphene etc?ok...now, have a look at that darn chlorine dangling off the end of the loperamide molecule? I'm willing to bet dollars to donuts that using a simple reduction method will kick off that annoying chlorine...youre thinking so what? well, if u know your pharmacology, you'll know that that chlorine is the reason that p-glycoprotein can grab that molecule and pump it back across the BBB (contrary to popular belief this sucker DOES cross the blood-brain-barrier but is immeadiately pumped back across by P-glyco...and then youre thinking, yeah? but what about that dimethylamide ,isnt that also a complete non starter? well no, actually it isnt, turns out that when our good freind Dr. Jansen was brewing up his analogs that the pyroldine amide (in Dextromoramide)was the stronger of two that were tried, the other being the dimethylamide......are we having fun yet?
  10. tramerall

    tramerall Silver Member

    Reputation Points:
    Aug 9, 2011
    from U.S.A.
    Hello All, I haven't posted much on here, so pardon me if I sound strange or if I posted this in the wrong spot. But I just wanted to post my opinion on the use of loperamide as a way to make the withdrawls of opiates easier to deal with. I am not going to bother to use "swim" for this, since lope is an OTC medication. Twenty-two years ago I was diagnosed with a severe case of Crohns' Disease, which is a disease that attacks the intestines, for me, it hit my large intestine. I spent two years in the hospital battleing this. They have resectioned my intestine many times, and currently I have only a foot and a half of my large colon left. Since then, I have been prescribed tramadol to battle restless leg syndrome that was caused by a blood clot that formed in my leg from being bedridden and not moving my legs. I have become extremely addicted to tramadol, my tolerance is so high, it takes at least 15 50mg pills to do anything to me. I have never had a seizure or anything. Lately, no matter how much trams I take, I don't feel anything except the quieting of my RLS. I spend so much money getting as much trams as I can, and I have decided to start to taper and quit trams all together.

    After much research for ways to help with the taper and withdrawls from opiates in general, I found that loperamide(Imodium) seems to be a possible way to do this. Since Crohn's causes constant diahrea, I am actually prescribed loperamide. I get 360 2mg capsules every month. I take them as needed, and I take alot of them. Sometimes they help with the shits, sometimes they don't.

    Well, last week, I started my taper. I gave all my trams to my mother to hold and keep them from me so I don't take any. Now, the amount of loperamide I take might scare some of you, but I have the OK from my doctor, since my situation with Crohn's makes me a bit different than a normal person. I started by taking 5 Tagaments 30 minutes before I take my first dose of lope. My normal dose of Lope that I take on a daily basis is twenty 2mg capsules. I know that seems like a lot to the normal shitting person, but remember I am not normal, lol. Well, for my first dose, I decided to take sixty 2mg capsules. I OK'd this with my poop doctor cause he wants me to stop the trams too. And I must say, about 30minutes after I took them, I felt as if I took some 10mg Norco's. My pupils were pinpointed, full of energy, no withdrawl symptoms, felt great. So lope will help people with the withdrawls from opiates.

    I plan to slowly take less over a period of time. I will post my progress as I go. So those doubters out there, go on and doubt, but I can honestly say, Lope works! But I got an advantage tho, no matter how much lope I take, I will never get stuffed up. LOL I do wish I could pinch a loaf, been so long since I had the satisfaction of pinching one, but alas, it will never happen.
  11. Mindless

    Mindless Gold Member

    Reputation Points:
    Feb 23, 2011
    from U.K.
    One thing to bear in mind when taking more than the recommended daily amount of loperamide is that the risk of adverse effects increases. While loperamide itself rarely causes dangerous adverse reactions, there have still been isolated deaths. Those most at risk are children, and those with hepatic impairment (who are at risk of increased toxicity due to deficits in first-pass metabolism). Signs of overdose can include sleepiness, slow breathing, drowsiness, stomach cramps, bloating and vomiting. Mega-doses of loperamide would probably increase the risk of serious adverse reactions. These include:

    "abdominal cramps, dizziness, drowsiness, and skin reactions including urticaria (skin rash); paralytic ileus (intestinal obstructions) and abdominal bloating also reported." Source: BNF 63 March 2012.

    Mixing polysorbate 80 with loperamide in an oral solution may induce a lesser and more short lived effect on the central nervous system, at least in mice, where I seem to remember the effect was measured by responses of the mice to having their tails flicked. Loading PBCA nanoparticles with loperamide, for intravenous injection, is probably beyond most users capability. The only drug that produced central effects in combination with loperamide in human subjects is quinidine, where respiratory depression was used as a measure.

    A solution of polysorbate 80 and loperamide did produce "a much less pronounced and very short analgesia", but this was administered intravenously (to mice). If the solution were ingested, I wonder what impact the process of digestion would have? The only effective intravenous solution was formulated by incorporating loperamide into PBCA (poly(butyl cyanoacrylate) nanoparticles:

    "Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.

    Some users also advocate the use of Piperine, a constituent of black pepper.

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

    Increased drug delivery to the brain by P-glycoprotein inhibition. Abu J. M. Sadeque, PhD, Christoph Wandel, MD, Hauibing He, PharmD, Selina Shah, MD, and Alastair J. J. Wood, MD.

    One of our members had a very close call following use of heroic doses of loperamide, you can see his post here. I'm not sure that it's safe to alter the pharmacokinetics of loperamide and allow central activity, or to take large doses. Loperamode is a potent opioid after all. If it does work, there are no dosing guidelines and a possible risk of overdose.

    I can see how loperamide could help with Crohn's, my mother has the same condition and it's pretty painful. I'm glad loperamide is also helping you through this transition. However, despite your doctors advice, the risks bear consideration.
    Last edited: Jun 11, 2012
  12. Shwags

    Shwags Mercury Member

    Reputation Points:
    Jun 29, 2005
    37 y/o from U.S.A.
    Funny joke you thought? It's not....

    BTW, you weren't kiddin about 'drug addicts only' but I am on the borderline so, here I am. Does Immodium really potentiate Kratom? Just had my 3rd shoulder surgery like 3 months ago, and ordered some Kratom for the first time since its past the acceptable timeline for Doc to prescribe. Although I enjoy it, it is fairly weak and if Imodium in combination works I might try that out.
  13. hypernihl

    hypernihl Titanium Member

    Reputation Points:
    Sep 28, 2008
    from U.S.A.
    I've always wanted to try this with proper opiates (x-morphone, x-codone, etc), the theory being that the loperamide occupies all the receptors in your gut, freeing up more of the the proper opiate to be available to cross over into the brain.

    Not sure how this would work, since agonist drugs spend very little time bound to a receptor. It's a matter of concentration in the area of the receptors and affinity of the drug to the receptor. If loperamide has a higher affinity to opiate receptors in the gut then proper opiates, this might work.
  14. El-producto

    El-producto Newbie

    Reputation Points:
    Mar 25, 2013
    from U.S.A.
    This is no joke, been in wd..decided I was going to go all out and try to get high with imodium
    i have a slight tolerance right now (30mg hydrocodone) so I took 72-2mg loperamide with 150 mg zantac
    and I shit you not!

    Took zantac 30 min before 72 all at once, had to put up with slight stomach pain at first but holy shit, I am very high right now(no bullshit) took away wd and got me a great codone-(oxy?) High

    No stomach pain the last few hours and get this, I got very small pupils,slower breathing and im even itching which I havent got from opiates in a yr
    seems like eating alot of imodium could have paradoxical effect and cancel out constipation/cramps

    I cant believe this..i cant recomend somebodt else try this but fuckkkkkk!

    El-producto added 13 Minutes and 13 Seconds later...

    I should also say, I had a weird/nasty drowsiness at first w/ stomach pain. Also got dehydration but its managable, then it went away

    Not an insane amount of euphoria but its def. there looked in the mirror, eyes were half open,bloodshot and very small haha
    and the feeling has been pretty consistant the last 6 hrs
    this might have cost me 5$ at the store
    Last edited: Mar 25, 2013
  15. longbeachone

    longbeachone Silver Member

    Reputation Points:
    Feb 13, 2013
    from U.S.A.
    For those who warn these addicts about horrible bowel problems, it's important to remember that most of the posters using loperamide have been bathing their intestines with constipation causing opiates for a long time, possibly years. Loperamide is pretty much the same thing as heroin or oxycontin, but it does not cross over the blood brain barrier. The discovery of this otc drug as an aid for withdrawals is an enormous blessing, and its use will save many people from awful withdrawal symptoms.
  16. Nefret

    Nefret Silver Member

    Reputation Points:
    Mar 13, 2013
    from Canada
    I have been researching Lope and how it can cross the BBB for a few days now, from other forums and other info on the subject from the net, with me being the test subject. I have found a combination that not just takes away the withdrawal (from Oxycodone) but has gotten me a nice high and given me the nods at times. This is what my protocol with Loperimide (Imodium) is:
    * I take Pri-Losec 20mg and 2400mg Vitamin 'C' that has Quercetin added to it,I like SISU brand and it's called " Ester-C, Supreme" which helps the Lope cross the BBB, and the Vitamin C, in large doeses is quite safe and helps you to not get too bunged up...I take 5,000mg per day for that very reason, and it's safe for the average person to take in that large dose...the only usually side effect of taking that high dose is loose stools, but with taking the Lope, I don't get the diarreah, I just have a normal poop, about every second day...but again everyone is different.
    * wait 30 minutes to an hour, to get into my system (It is a PPI,(protein pump inhibitor) which helps get the Lope cross the BBB)
    *Drink at least a cup of 100% Grapefruit juice (it potentiates any opiate/opioid)
    *then drink at least a cup of Tonic Water( tonic water has Quinine in it which helps get the Lope across the BBB) with 15 - 20 Lopes, equaling 30-40mg of Lope. I have heard of people taking way more Lope (like 60 to 100mg but personally I am too afraid to take that amount, but that's just me), but found this to be a safe starting point. You can go up or down with the Lope depending on your tolerance with opioids. I have taken up to 50mg safely, but everyone is different so be safe!!
    I have also taken Benedryl with it, or a benzo or even a Gravol to add to the effects of the Lope.
    * the effects will be felt between 45 minutes and grow for a couple of hours and will last all day. :) Some people say that it last from 24 to 36 hours with the higher doses. Read this in a couple of places.

    I took this concoction at around 7pm and it is now ater 1am and I feel very relaxed and have nodded off a few times while sitting on my patio. I hope I wrote this all out OK LOL I think I have as I read it over a few times, and don't believe I left anything out :)

    I have taken a laxative every second day and a stool softener everyday to help with the constipation, and of course the large dose of Vitamin C. And glad to report that I had a B.M today, even with doing this receipe today :) Also a lot of people have said that 2 days after stopping this cocktail thay are able to go. I would highly recomment doing it one day, and waiting to see how afterward, it will take you to have a B.M-poop. You don't want to do this everyday for like a week. If you don't get your bowel moving and are taking huge amounts of Lope, you could get your stomach sick to having a bowel obstruction. You just have to be safe and smart with this. Drink lots of water, lots of whole grains and leafy green and other fibers in your diet. And even just reg. Vitamin C and Magnisium as they help the bowels get moving. Just don't take the Mag with any medication as it could lessen the efficacy of the medication. The Lope or otherwise.

    I took this yesterday as well and slept for 11 hours!! I needed it, as I was only sleeping around 5 to 6 hours a night which is not enough for me at all.

    And this is so not a placebo, as I have take a number of herbal supplements claiming to relax you, and really thought that it would work....but next to nothing with the herbals...still major anxiety was present. The would probably have worked if I weren't in withdrawal. However with this Lope cocktail , I have tried this maybe 5 different times. And everytime it has worked, even my eyes were pinned, and that doesn't happen with a placebo. Try it, and see if it works for you, if you are looking for something for the "in between days of having opiates" or you are in withdrawal and you must get out of the house and be somewhere.
    IMPORTANT: Do not drive with this cocktail, until you know how it will affect you. You don't want to fall asleep at the wheel.

    Everyone, the first priority is to be safe. This does work. Be happy and safe :)

    (Let me know if you tried this, and let me know how it worked for you!)
  17. Mindless

    Mindless Gold Member

    Reputation Points:
    Feb 23, 2011
    from U.K.
    I appreciate your detailed reply here, but there seem to be a few misconceptions. Be wary of advising others to try your proposed combination, or any excessive dose of loperamide.

    If this combination is used it would seem practically impossible to separate any central nervous effects arising from loperamide from those of diphenhydramine (benadryl) or benzodiazepines.

    It was Quinidine, not quinine, which was shown to enable central nervous effects from the use of loperamide. Sadeque et al found that Quinidine permits central nervous system effects via it's inhibitory effect on p-glycoprotein efflux, this might increase loperamide's toxicity. See Increased drug delivery to the brain by P-glycoprotein inhibition.

    The use of cytochrome CY2PD6 inhibitors (such as contained in grapefruit juice) seems unlikely to potentiate loperamide or other opioids. These inhibitors may prevent or inhibit the metabolism of codeine to morphine in 'extensive metabolisers'. Those who are poor metabolisers of codeine to morphine due to genetic deficiency are also unlikely to either benefit or lose out when combining codeine with CYP2D6 inhibitors. 6%-10% Caucasians, 2%-5% African Americans, and 1% Asians are poor metabolisers of CYP2D6 substrates such as codeine.

    Drug Interactions: insights and observations. Understanding an Important Variable in Patient Response. John R. Horn, PharmD, FCCP, and Philip D. Hansten, PharmD, Pharmacy Times 2006.

    However, it does seem possible that grapefruit and seville orange juices may increase bioavailability of opioids, via CYP3AF and p-glycoprotein inhibition:

    The effect of grapefruit juice and seville orange juice on the pharmacokinetics of dextromethorphan: The role of gut CYP3A and P-glycoprotein.

    Grapefruit juice / CYP2D6 : clarifying a common misconception
    by Paracelsus.

    Last edited by a moderator: Apr 30, 2017
  18. tcoro

    tcoro Titanium Member

    Reputation Points:
    Apr 14, 2013
    from U.S.A.
    Forgive my ignorance - but what is the difference between Quinine & Quinidine? (in laymans terms please!) I tried searching but I am not getting past isomers, molecular structure & chemistry - and that is all way over my half-empty head!
    I understand they both come from Cinchona, quinine is in Tonic Water...etc but I have not heard of Quinidine.
    I have read many posts besides this one where quinine is referenced when maybe (as mindless points out) Quinidine is the proper term/item instead?
  19. Mindless

    Mindless Gold Member

    Reputation Points:
    Feb 23, 2011
    from U.K.
    My understanding is limited, but it looks to me as if these two drugs share a molecular formula. The spatial orientation of their atoms is the sole difference. However, slight differences in structure can produce quite different results for those using the drugs in question. Smith (2009) says:
    Chiral Toxicology: It’s the Same Thing...Only Different.

    It does seem that quinine and quinidine may share some potential effects to a greater or lesser extent. Some individuals have reported that quinine use permitted central nervous effects from loperamide, although this effect has not been demonstrated in any studies. Quinidine itself is not a particularly safe drug to experiment with; in clinical use it may give rise to QT-interval prolongation at quite low doses (Murphy 2012). This risk applies particularly (but not exclusively) to women. QT-interval prolongation is a disturbance of the heart's electrical cycle, it is associated with torsades de pointes (a cardiac arrhythmia) and sudden death.

    Greater quinidine-induced QTc interval prolongation in women. Benton et al, Clin Pharmacol Ther. 2000 Apr;67(4):413-8.

    Clinical Pharmacokinetics- 5th Edition. Murphy J, 2012.
    Last edited by a moderator: Sep 10, 2017
  20. Smeg

    Smeg Opiates & Opioids Staff Member

    Reputation Points:
    Oct 26, 2009
    55 y/o from U.K.
    It (sort of) does feel appropriate to mention that loperamide can have the capacity to help alleviate some of the consequences of the mid to long long term opiate/opioid use/abuse and withdrawal.

    I'm going to suggest that it can somehow aid with body pain. By this I mean that any kind of euphoria felt by its ingestion, may just be that.

    The sudden joy of (subjectively) felt comfort during any terrible time can bring about a sense of euphoric hope, that may be interpreted as a "high".

    After all, who in this sub-forum wouldn't translate it as precisely that feeling of being awash with consolation, and relief during a storm of withdrawal?

    To me, it often feels that there's some kind of clingy hope attached to the loperamide intervention. And yes, there's a validity about it too.

    There's no question of that.

    The difficulty arises (I reckon) in that zone when it's viewed as an alternative to the opiate drug of choice.

    I must admit from my corner here that I found loperamide a wonderful source of comfort ten years ago (2003) when I asked my doctor to reduce my own use of prescribed tramadol.

    It was 400mgs daily from a trauma injury to my left tibia, but really didn't (and still don't) view it as an alternative avenue for replacing my prescribed dose then.

    By fuck it helped though, and I read various "snake-oil" tricks on the net to help convert it into crossing the blood brain barrier.

    None worked for anyone I knew then.
    Last edited: Jun 3, 2013