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Providing straightforward information pertaining to drugs, drug use & drug policy. The Grey Pages promotes drug-related literacy and advocates a system of viable and tolerant drug policies. This is my personal collection of commentaries, essays, tid-bits, and other such writings on everything ranging from drug use, drug policy and drug-myths, to drug-science, addiction, human behavior, and the workings of the human brain. I started this blog with a particular focus on opioids, and over the past year have found my interest gravitate toward the intriguing, ever-changing world of designer intoxicants (i.e. "research chemicals" or "designer drugs").

Friday, November 26, 2010

Loperamide In Opioid Withdrawal

I recommend readers refer to my more recent information on loperamide and opioid withdrawal; which most people will likely find more informative/useful.

The active ingredient in the popular over the counter diarrhea medication (Immodium) is a highly lipophilic & poorly water soluble synthetic opioid. It is a non-controlled substance due to the fact it has negligible potential for addiction or misuse. Loperamide does not cross the blood brain barrier in significant amounts. Therefore causes no central activity (all psychoactive drugs act on the central nervous system). Any small amount of the drug that does cross the blood brain barrier is rapidly exported from the brain by P-glycoprotein, a multi drug resistance protein. Loperamide does act on mu opioid receptor sites peripherally, especially within the gut, by decreasing activity of the myenteric plexus (within the large intestine); its way of relieving diarrhea. Most opioid agonists work this way including morphine and codeine, and both have been used for the same purpose.

Loperamide was shown in studies to cause a mild physical dependence, with symptoms of opioid withdrawal upon abrupt discontinuation of therapy; the drug at one point was controlled under Schedule V of the CSA, this is no longer the case.

It is commonly believed that certain drugs which inhibit P-Glycoprotein will allow for loperamide to cross the blood brain barrier, and produce the desired centrally mediated effects (psychoactive rather than simply physiological).

Whether or not one can create conditions conducive to loperamide's blood brain barrier penetration, the drug in fact does serve a valuable purpose in easing opioid withdrawal. Not only the severe diarrhea, but every other symptom that is mediated peripherally; in other words, loperamide in the right dose will completely eliminate the physiological symptoms and discomfort of opioid withdrawal.

Skeptical? I was. Though in theory it makes sense, I had attempted using loperamide in the past while detoxing to no avail; dose range was 24 to 48mg. The dose needed in most cases to make any impact in withdrawal is upwards of 70mg. Yes, this dose is extremely high, and one will ask; "how could you ever sh** again in your life?" . However, loperamide causes no more constipation than the typical opioid; morphine or codeine. Opioid addicts and highly tolerant subjects take hundreds of times the typical therapeutic dose, just showing how widely tolerance can vary and how high it will go.

Note; respiratory depression is obviously a non issue; UNLESS the drug crosses the b/b barrier. Administration of loperamide following doses of quinine (a pgp inhibitor) resulted in respiratory depression; indicating central opioid activity.

After trying this for myself (in a much higher dose) for the last 48 hours, I have not a doubt in my mind as to the validity of the claim that loperamide will alleviate the physiological discomfort of withdrawal. 180mg was taken late last night 24 hours post buprenorphine dose - Initial symptoms of withdrawal were becoming apparent. The drug is extremely long acting, similar in duration to methadone.

Think of a narcotic high without the euphoric-antidepressant properties. So basically a body buzz (hey, at least they can't tell you you're numbing your feelings anymore). Histamine seemed to be an issue, which 25mg diphenhydramine eliminated. Constipation, obviously. Sick? Not at all. Miosis - Pupils pinned. I look like I would had I taken morphine or methadone. I dosed 80mg around 11am; initial dose should be high, with the following doses in the range of 50 to 75% the initial dose, a full 72 hours should be expected for peak plasma. Lope was discontinued at 5pm upon aquiring buprenorphine/naloxone strips.

In conclusion; loperamide is effective in eliminating the physical aspect of opioid withdrawal, and may even make a good maintenance tool for those without access to methadone or buprenorphine; I know of a number of people who do just this.
For those kicking, or those suffering between the scripts or the fix, I reccomend you utilize this easily available aide/tool. I now swear by it.

Note: I now venture as far as to say that loperamide in even higher doses, taken on a regular regimen, will result in significant amounts of the drug effectively crossing the blood brain barrier, allowing for CNS opioid effects.

I believe that by 1) Using a PGP Inhibitor such as quinine, and 2) completely overwhelming the workload of P-Glycoprotein with excessive dosing of loperamide; The drug will act centrally in addition to peripherally, rather than peripherally alone.

Note: This is simply a theory, which should NOT be attempted outside of a clinical setting. Assuming loperamide was allowed to act centrally, it is unknown what an acceptable dose would be, or what the therapeutic to toxic dose margin would be. Making yourself a guinea pig to this experiment outside of clinical research could easily result in your death. Loperamide is a relative of the Phenylpiperidine class of synthetics which include the highly toxic drug pethidine (commonly known as meperidine). Acute and chronic effects of loperamide on the central nervous system are unknown, and could likely be harmful.

31 comments:

  1. I concur. I've been taking it for the past two days and absolutely no w/d symptoms. Absolutely amazing. I wish I had known about this years ago.

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    1. I agree, I just discovered this with the use of quinine and cimetidine, it completely does rid you of withdrawal symptoms. Only an addict would be able to tell. Physiological withdrawal symptoms are just that, they are not perceived, they are not imagined, and there is no placebo effect. I have been doing this for two days now as well, and nothing. I even feel a bit of a buzz from it, dry mouth, the typical side effects of opiates. This is great knowledge to have, because now I don't need to freak out about going to school or work or being sick again.

      Anyone addicted to opiates should have this knowledge and trust this post. 60-100 mg is sufficient.

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  2. Question ...as I am using imodium for detox currently, how long do you think I need to take it? How long will the previous opiates remain in my system? Opiates have been my only vice for the past several years, half the time legitimately prescribed. I'm on day 3 of lope only now, following high opiate usage...high even for myself. If I continue for maybe 3 or 4 more days should the worst of what I would have considered wd be over? After the last dose of imodium should I expect withdrawal? Lastly, I assume lope shows up in a urinalysis, and I'm sure the high dose would be cause for concern. How long can I expect lope to be in my system?
    Id like to add this is a truly great sight. Love love love what you're doing and the presentation.

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  3. Hey there, from what you describe I assume you're pretty highly dependent? Knowing the particular narcotics you've been on would help to better give an idea of the withdrawal profile, but let's assume it's intermediate to longer acting opioids you've been taking; After several years of continuous use, the worst of acute withdrawal should last 5 to 10 days for your typical morphine/codeine type drugs (likely toward longer end of the spectrum in the case of XR meds such as OxyContin). Generally, people detox from opioids using other opioids as a taper tool.. Depending on what your tolerance was, you could be using loperamide as either a taper tool, or more of a comfort tool (the latter is likely if your tolerance is high enough).

    If lope has simply barely taken the edge off, then it's likely a positive indication that your system (being your neurons, receptors etc)has significantly adjusted downwards; simply put, the more discomfort, the better likelihood that you've become closer to baseline as far as tolerance/dependence is concerned.

    On the other hand, if you've been comfortably euphoric with lope for the past 3 days, then I would believe that little progress has been made; unless obviously you've tapered it down gradually (which likely takes a bit more than 3 days if you plan to do it comfortably)

    There are so many variables to something like this, and I'm not completely aware of those.. As I suggested, a few questions can help you better have an idea;

    Have you gradually reduced the lope? What is your current dose?

    Have you felt much discomfort so far?

    What opioids were you on and at what dose?

    Generally speaking, three days away from the regular agonists even on high doses of lope is a good thing, and if you've dosed appropriately, you're likely to have lowered your tolerance. But regardless, mega dose lope should be thought of just as something like methadone when it comes to detox, and should be tapered accordingly. Even if you had taken lope for three straight weeks while staying clean from regular narcotics, you've still been taking an opioid. Hopefully you've tapered it? I might suggest a few more days of it to gradually get the dose down to nil. I'd wait to jump the lope until at least a week after the last dose of regular opioid.

    As for loperamide and urine screens, what are you being screened for? And is this a standard dipstick test? If it's related to employment or probation/parole, there is no way that any loperamide metabolites would register, unless they were specifically tested for (which is quite a hassle), loperamide is a piperidine derivative related to diphenoxylate and difenoxin. The only drug remotely related to lope which may be tested for in employment/probation screens is fentanyl; which isn't even included in most common test kits, and requires a specific test.

    I hope you found some type of insight here.. Like I said, there's much more to consider in order to better lend insight. Let me know if there's anything I missed, and thanks for reading. It means alot.

    MWL

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  4. My best friends son just died from what you are doing.....

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    1. HOW MUCH? IT probably is NOT a good IDEA to take TOO MUCH more..of course TOO MUCH means TOO MUCH....but what dose is TOO MUCH...I would say over 60mg is HIGH RISK

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    2. I regularly take 144 mg without any issues. I think if there was a death that involved loperamide there must be other substances in the body that contributed or caused it.

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  5. So, for someone that takes approx 150mg of oxycodone a day...then has to drop down to approx 100mg of hydrocodone a day...approx what mg of this should one take to get thru DT's?

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    1. Unfortuntately there's really no way to know with loperamide. It's trial and error for the most part. I can't really advise anyone on this, as it would be irresponsible of me. In situations where I was detoxing, I would typically start with around 60-90mg, and see how I felt from there (going up by 20 or so mg at a time every few hours).

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  6. Yes, Loperamide will bind to any peripheral opiate sites in the body and the ability to completely eliminates all physical opiate withdrawal symptoms. As for the CNS and brain, the physical relief of stopping a opiate withdrawal it all I needed. When my body tells my brain the withdrawals are over I do not give a crap what it is. By the way, Loperamide is a opiate of the piperidine class and milligram for milligram it's effects are similar to Meperidine (Demerol). Yes, if you take 150-200 mg of Loperamide for a while and abruptly stop you will experience severe withdrwals.
    Warning: if it's the first time you use Loperamide start with a dose of 20 mg (10 2 mg tablets), and repeat every hour making sure you do not have an alergic reaction.
    To avoid constipation there is mineral oil and fiber.

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    1. Not much is known about the actions of peripheral opioid sites. I can say for sure that peripheral opioid activity does not eliminate the physical withdrawal symptoms, as peripheral opioid receptors are not known to play any role in the physical dependence producing properties of opioids. The only peripheral action known to suppress any withdrawal symptoms is mu and delta binding in the gut - which relieves only a portion of the diarrhea and GI discomfort. Most of the physical component of withdrawal is associated with excess excitation of the sympathetic nervous system (HPA axis, locus coeruleus, hypothalamus); the hypothalamus regulates blood pressure, body temperature, GI function, perspiration, pupil size, etc. The locus coeruleus in the medulla (brainstem) controls the "stress response", triggering anxiety, muscle tension, shaking and tremors, restlessness and a general state of agitation or panic. Other areas such as the pituatary and adrenal gland become excited as well - all these areas that are inhibited by typical opioid agonists are excited during withdrawal.

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    2. You are wrong and need to drop the book theory as that is wrong also. Just cause it is in your books not not make it true. You are insulting all the users who have found the opposite effects of what you are stating. This might be a good lesson for you to open your willingness to learn the truth (real world stuff) and not just be book smart. Books on this topic have destroyed lives. You are spewing false information.

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    3. DM, do you have or have you had a habit? Have you tried Lope & Omep? It really works. I'm a 43 yr old skinheadpunkrocker, I'm not a bullshitter. If you give it a shot (no pun intended) it will most likely work. Perhaps though, it doesn't work for EVERYONE. Nothing does.

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  7. This is by far the most 'to the point', straight forward, assesment of using loperimide for this purpose. For what it's worth I'd like to share my experience (which as we speak is commencing heh). First, for the sake of background I should say that I have a 'history' with opiates but for roughly 10 years have been 'relatively' clean (as needed w/scrip for pain, recreational on occasion when the opportunity presents).
    I broke my back several months ago (lowest two vertabrae, most damage was to where my left leg 'necessities' met up at that point on my spine, to keep it short). They started with Dilaudud and Valium; I feared I was on a bad path back to full blown dependence (Dilaudud has a 'special' place in the pantheon of abuse and it's not swallowing them, nor are they known to last long regardless) . Went back to the doctors a couple days later and said they weren't effective for very long after taking them (they really weren't, hoping for a long acting morphine or something maybe that I could keep a better handle on). They gave me 10mg percs which, in a happy surprise, were actually much more effective. Then, now under care of my GP, he gave my vicodin, then tramadol (he knew that I had some fears of addiction).
    All was right with the world I thought, tram = non-narc I thought. Wrong. Now 3 days hence running out of trams (taking roughly 50, 50mg tabs a week for several months) I realized I was going into actual withdrawls, did some research and sure enough. Not nearly as severe as what I know to be possible but still not a picnic. Insomnia, diarrhea, aches / pain, RLS. Enough I didn't want to see how much worse it could get. So I began taking ibuprofen, immodium, etc., usual stuff. Realizing I was taking a fair amount of loperimide I decided to google a possible counter to it's 'primary purpose' and found prolific info on this practice I had no clue existed.
    Anyhow, here I sit, roughly 6am, took 40mg lope about 4 hrs ago.
    Honestly? Yes, all my phys. symptoms have been relieved and I even feel a twinge of euphoria and relaxation. If I had to compare the sensation I would put it in the realm of the more 'natural' pain meds: morphine and codine. If you've taken those and can differentiate between them and hydro/oxy - codone in sensation, that is what you are in for.
    Additionaly, I take prilosec for heartburn and had some tagament. I took both of them in advance to potentiate the effects but have no baseline to compare.
    I am a 180 lb. male, opiate usage and potential for tolerance / withdrawl severity can be insinuated from above and 40mg def. did the trick for me. So there is what I can offer the inquiring mind. I have NO qualification to reccomend this usage of loperimide or any medicine, this is simply what I experienced. Actually experiencing right now :). If I ever find myself in a need to alleviate these symptoms with minimal hassle (trip to the pharmacy), barring some future development as this is my first time trying this, I won't hesitate to repeat the treatment.
    Good luck all. Believe me I know, that cute fun little monkey you can get a kick out of can quickly get out of hand and become a raging 800 lb. silverback demanding to be 'fed'. This method, for me personally, has been the first I've seen that is legal and won't cost a fortune in Drs. fees, to make that raging beast sit down and shut up! At least so far ;D.

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  8. If I read correctly, you dosed Lope at 11am and at 5pm you scored some bupe and dosed that? Does the Bupe precipitate early WD's in lope? I've been on lope for about a month, tapering down after a 3 month bender on methadone. I'm about 12 hrs past the last dose and happen to have some suboxone on hand (8/2). Will the bupe react with it?

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  9. First.. to answer the question in the comment above... (though this is several months after the comment was originally posted..) I was worried about the possibility of precipitating withdrawal with my bupe script after trying this as well. I had a terrible experience with precipitating w/d in the past. I had originally started detoxing several years back with a bupe script which didn't pan out well, relapsed for a year or so, then decided to go to a methadone clinic so I could still get high. I finally decided to grow up and knew that if I really was going to stop using opioids for recreational use, bupe was the only way to go. So I went back to the doc and got back on bupe. Though I knew precipitating was a possibility with a long acting opioid such as methadone, I didn't fully take into account the length of time needed to completely eliminate the methadone from my system, and ended up being induced on the bupe only three days after stopping the methadone. I was taking on average 400-600 mg of methadone a day. Sufficed to say, within half an hour of my first bupe dose I was in the worst withdrawal imaginable. I ended up testing positive for methadone for 21 days, and was in severe withdrawal for 29 days. Anyway.. sorry for blabbing on. Figured I'd tell my story lol. To answer you question, when waiting for my bupe script refill, I took lope two days after the cessation of the bupe. It did work after drinking a bunch of tonic water with quinine. It was very slight, but noticeable. After only that one day on lope, I got my bupe script the next day. After taking it, I did not precipitate at all.. which for obvious reasons was in the back of my mind. On a side not though.. Since I've gone and written all this, I may as well bring up that when I took the high dose of lope, I was rather uncomfortably constipated.. Much more so than the usual constipation felt during any other opioid, as well as feeling an over all sense of slight "discomfort?". This could be due to the very small CNS effects of high dose lope, which may (in other clinically prescribed opioids) cause the alleviation of discomfort that would usually be felt from such constipation with their euphoric effects. I'm not sure. But all in all, if you're worried about severe withdrawal for whatever reason, I would definitely recommend taking a somewhat high dose (maybe 40-60 mg to start out..?) of loperamide. It will relieve at least most of your discomfort. I would not recommend it's habitual use for such reasons due to the lack of studies on the possibility of permanent CNS damage.

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  10. This was really informative. I am on my 5th day of detox from subutex and I have been using this method. I have been pretty amazed. I was on subs for almost 2 years (after being on and off heroin for 10 years) and have had a easy time of detox. This is my second time coming off this crap...and on the 5th day of this last time...let just say I wanted to remove my eyes with a spork. ;-)

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  11. It just works... 148mg will completely hold off any wd.

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  12. 60mgs in 3 hours and im really feelin it, along with shortness of breath and tightness in my chest. hard to catch my breath and feel down. will it work for wds? sure. i guess this is better than wds but its not something id do for recreational purposes. when the wd is over, so is the lope.....but not the baseball sized turds its leaving behind. or on the behind. wakka wakka wakka.

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    1. the second to last sentence should have read:
      "IN the behind"

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  13. Just want to add my experience to help keep this current. My habit is hydrocodone, usually 75 to 100 mg a day. Been doing it for about 5 years and have had many bad withdrawals during dry spells. I got turned onto lope though my own research on the Internet and other blogs and forums. For me personally, after first 24 hours since last dose of hydro I will take 24mg (12 x 2mg) lope then do the same 8 hours later, then 8 hours after that. After 48 hours I drop the 24mg dose down to 12mg every 8 hours. 72 hours into detox I drop my dose down to 6mg every 8 hours. Next two or three days 6mg every 12 hours. Then I jump off CT.

    I've used the above schedule a couple of times in the past year, the most recent last month. Both times I suffered no real withdrawal problems except for fatigue. For me it is like a miracle drug for WD's. However, it can be abused to. Even jumping off at 6mg twice a day is uncomfortable and it is tempting to does again, but the discomfort from jumping off lope at such a low does is a frigging picnic compared to regular withdrawal.

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  14. Common misconceptions are half life of this lopermide, when first trying to get clean I dosed 60mg lope every night thinking I could feel it wearing off.. Which only lasted until I could score(a day or so) then until recently I was found without any option but to dose a big dose 50 and had nothing for 48 I woke up and still feel bad but more so lazy third day I took 10 actually a picnic come the fourth day I plan to take 5 in 30 hours if needed for work. The half life is real, like dipping your feet in Cold water making sure its right, I'm sure everyone will mess around with it but I've tested its limits of thewith drawl thresholds borderline crawling out of skin/being lazy depressed and ambitious less. Not to mention its 5degreees outside freezing. 5 days, lope or not(lope with aggressive taper) 5 days, longest I've been off of black for 1year. Never been happier. Its best to be in bad withdrawl before lope because if not then you never will feel sick from switching from doc to lope. It is necessary to not let it be too easy because that's what stops you from picking up on days your not.sick because your on lope but depressed so you STILL pick up. Attempt No. 33423 is looking like a success. For everyone trying to kick, you have to acknowledge the dark passenger you have that wants to get high or well, that knows its bad but still does it acknowledging and fighting this person gets you your life back. you will drag your negative half, kicking and screaming to sobriety, where you will then kick yourself for not doing sooner

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  15. I just found out my doctor is gone after 2 years of her having me on a pain plain, for a genetic condition i have that causes ulcers on the bottom of the feet. I have always taken my reg. does of 7.5 mg of percocet every 4-6 hours max 8 daily. Now the replacment doctor gave my 5 mg only 4 a day script for 120 for the month. I am so upset because I have 2 children 1 with the same condition as me that is 3 so I am constantly carring her around and having to help with her boo boos. I have heard of this immodium a few times, will this work as I wean down because I don't want my body dependant anymore I would rather deal witht he pain on my feet then deal with doctors doing this to me forever. It's been about 2 1/2 years on pain meds, any suggestions would help.

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  16. Ann, I "feel" your pain, I am Oxy as part of a pain management plan for chronic degenerative disease after a severe accident, and I have metal body parts, la la la. I hate being a prisoner to this medicine, especially after having switched Drs numerous times due to insurance changes, and even being threatened with prison by one doctor after I lost my pills at a funeral, and the police would not take a report, and my regular Dr was in India, so my PCP prescribed a bridge, and I got threatened with arrest by my Specialist. Aaaanyway, I am on day one of ZERO, after tapering down from 120 mg a day of Oxy. The taper was miserable, to be blunt, and now, I am completely desperate for help. I also heard about Loperamide as a possibility to lessen withdrawal, as well as Gabapentin, lots of water, Bendryl, and low doses of Xanax, and Tylenol PM at night. Good luck!

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  17. Lope withdrawal is very difficult. Start out low and taper quickly. It binds to the mu receptors in the large intestines. That it does not activate CNS receptors, or get you high, makes little difference. You will have RLS, aches, depression, etc. I would have gone cold turkey off a massive pill habit had I known this. Those who say Lope withdrawal is easy, haven't used Lope to kick a pre-existing opiate habit. It's up there with Methadone, except with tapering off Methadone, you feel relief after your next dose. You're just in pain for months non-stop while tapering off large amounts of Lope.

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  18. I am a chronic pain patient with ankylosing spondylitis....I am on a total daily dose of 120 mg of oxycontin (3 20's every 8) and 4 15 mg ir roxi. I had recently been taken off 40 mg of methadone I had a shortage 1 month for 4 days where I had to cut my dose down to half do to pharmacy employee theft of my meds being short 12...I have a pretty high tolerance for opiates..I found a comfortable low dose of 8-10 mg of lope was sufficient and a .5 mg of klonopin.should further mention I have only been off the methadone for 3 weeks and I am still having rather "uncomfortable" withdrawal though not full w/d , which I still believe it to be from being on methadone for 2 years...never again will I not count my meds before leaving the pharmacy.I also HIGHLY suggest Marijuana for an adjunct med for w/d along with lope and a long acting benzodiazepine (if Possible)

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  19. I've been doing this off & on for two years. It. Absolutely. Works! My regimen: Take one, two, or three Omeprazole (OTC PPI--Protein Pump Inhibitor for acid reflux, etc--Prilosec is the brand name, I think.) wait fifteen minutes (not necessarily a must...waiting that is) then take 30 - 40 Loperamide tablets (60mg - 80mg). Start reading a book, get online & goof around--whatever. In less than thirty minutes YOU WILL FEEL MUCH BETTER! Don't count on nodding out or itching & scratching....although I HAVE experienced both, albeit very slight. Mainly I was buying some time until my Suboxone script could be refilled (approx 2 - 3 days) or until I could obtain a Subx strip on the streets (the streets are literally FLOODED with them here in Detroit, $5-$7 each, no more than that. Sometimes $4. Everyone & their mother has them for sale, usually.) But I'm getting off topic....I would rather take the Lope & Omeprazole "cure" then waste money on three or four (almost) worthless Vicodin's that BARELY alleviate my withdrawal symptoms. Doubters can doubt (as many "know-it-all's" on the Opiophile Forum do) but this shit really works!! Placebo effect my ass. It works. End of story. Oh, and I generally can pinch a loaf just fine after a day or two of using this concoction. Seems my body has adjusted to it.

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    1. So taking Loperamide really will help with my withdrawal? I am shooting 10 bags a day not at once but throughout the day. And I wanna try this but am skeptical......

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  20. Wow, this really works! I'm day 1 into a 200-300 oxycodone habit. I just took 8 2 mg pills about 20 minutes ago and a cup of coffee. Mind you , I woke up with the sweats, headache, fatigue, horrible smell, you know..anyway, I feel normal! I only took 16 mg. I would say, start small and work up. No sense in taking a large dose if it's not needed. I can't believe this worked! I'm going to clean my house and go run some errands , I could never do that day 1 of withdrawel. It's a miracle drug!

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  21. I probably will not respond to any replies, but LOPERAMIDE ( IMMODIUM ) has SAVE MY ASS ON NUMEROUS OCASSIONS!!!

    IT DOES WORK (FOR MOST PEOPLE).

    I have been taking Suboxone for about 2 year now and I have fluctuated dosage from 8mg-1mg and what not.

    A few times I ran out of Suboxone early and all I did was went to Costco (or Walmanart) and bought bottles of 300 2mg Loperamide or the later, 2 boxes of 72. I would take the generic versions of Prolizac* and Cimitide before taking it. As well as parachuting a large amount of grounded/powder pepper, and I would be "High".

    I put the "s because it is a weird high, enjoyable, but not that great. Regardless, one day of a 72mg--144mg dose and I would not feel withdrawal for over 2 days!

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