[UPDATE: 1 Jun 2015]

Adding and clarifying.

If you are reading this and are worried that you or someone you love may have a loperamide addiction, know that you are not alone! This is a growing national and international problem. Contact your physician for help, and feel free to print out the medical articles to help educate your clinician.



If you have questions not answered here, please feel free to post it to a comment, and I’ll answer to the best of my ability.

Coming up on two years of clean time from loperamide, I feel as if I can pass along some free advice to other addicts. Just don’t be afraid to quit. Please. Approach it with judicious caution — just try to do it right. Once.

Disclaimer: This is not meant to be a replacement for professional medical advice. See your doctor if you need medical help with an addiction.



So here we go. If you are ready to kick the habit, what should you expect?

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Can I die from Loperamide overdose? Yes. Definitively yes. People have died. I wrote about one here. Death is attributed to sudden cardiac arrest secondary to loperamide overdose. There have been many deaths reported to me anecdotally and countless others that are never reported. Many die at home before they ever get the chance to be treated; the ones who survive were hospitalized after suffering cardiac events, usually ventricular tachycardia leading to cardiac arrest. It’s important to understand that coroner’s reports on deaths cannot detect death from sudden cardiac arrest due to an arrythmia. Sometimes it may report hypoxia (secondary to loperamide overdose) — the hypoxia happens because you stop breathing when your heart stops. Ask me — I remember! And it was not fun.

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Will loperamide show up on a drug test? Generally, it won’t show on one of the normal quick tox screens because they test for certain opioid metabolites. BUT if they run a more extensive drug test, it will show up as a N-desmethylloperamide level. And don’t bother to try to cheat the test because loperamide’s half-life and fat solubility will make that nearly impossible. And beware that as lopermide’s abuse potential becomes more well known, a quickie test for it may be developed. Just a heads’ up.

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Does loperamide (Imodium) cross into the brain?

Damn skippy it does, bucko! It mostly acts peripherally, but in large amounts, it tries to wreak havoc. Like a nerd at a frat party, it sneaks past the Blood-Brain Barrier (BBB), but gets caught and immediately kicked back out by a big bully chemical called P-Glycoprotein, a protein that protects your brain from various toxins that have no business being in there. Take a normal amount of loperamide, and you won’t feel a thing.

So if that’s so, how can people claim to feel high on the drug? PGp can only handle so much at once. In a way, it’s an imperfect system because you overwhelm the PGp system by megadosing. At the risk of mixing my metaphors, think of your brain as a big sink with PGp as the drain — turn on the normal tap and the water pours right out the drain, right? But if you pour a whole gallon of water in there all at once, it’ll hold in the sink while it drains out, emptying as fast as it can. So if you’ve been mega-dosing loperamide, I assure you, your brain IS being effected. Don’t listen to those who tell you otherwise. Your Auntie Margaret speaks the truth.

This means, withdrawal from loperamide will be felt as viciously as any other opiate, minus some of the more aggravating mental aspects. The w/d effects are variants on the traditional withdrawal symptoms, some quite intense, and only now being studied as evidence comes in from those who have mega-dosed the drug.

[But loperamide’s ability to cross the blood-brain barrier in small amounts isn’t why it causes cardiac symptoms. It appears to be tied to lope’s suppression of calcium channels, particularly affecting the electrical conduction of the heart. So get off it and stay off it!]

In loperamide withdrawal, you will feel all or most of the following at some point:

Early symptoms:

Agitation

Anxiety

Muscle aches

Increased tearing

Insomnia

Runny nose

Sweating

Yawning

Late symptoms:

Abdominal cramping

Diarrhea

Dilated pupils

Goose bumps

Nausea

Vomiting

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Loperamide Withdrawal Timeline:



Everybody is different. But from my experience, I felt that withdrawal was not so bad intially (24-48 hrs), but the more time passed, the worse withdrawal got (48-96 hrs). Also, I thought withdrawal from loperamide was much worse overall than other ‘traditional’ opiates. Just my opinion, but other people have been backing me up on this.

In October, when I first stopped taking loperamide, I went cold turkey. The following is my recollection of going from an 80 pill-a-day habit to zero all at once.**

Day 1-2: Withdrawal symptoms resemble the flu, and like the flu, symptoms were mild for about the first 24 hours. I could just start feeling mild racing sensations in my legs and arms (often called RLS – restless legs syndrome), some agitation and anxiety, rhinitis (runny nose), and yawning. But at that point, I still thought “this isn’t so bad”.

At about 36 hours, the hots/colds set in. I was constantly cold — when I wasn’t having a hot flash that is. Yawning constantly. Sneezing constantly. Profound weakness and fatigue, especially in my solar plexus. RLS got a lot worse too — much worse at night! Insomnia also set in strong. Racing thoughts and a generally increased anxiety feeling. Couldn’t concentrate. Electric “zaps” in my spinal column at the radial and sacral junctions. Started feeling really grumpy about then too.

Day 3-4: Between 72 and 96 hours all those feelings just got worse. Depression set in. My pupils got really big! Even bright light began to bother me. Around the 4th or 5th day, the diarrhea started, soft at first, then liquid. Monumental fatigue, unlike anything comparable, made simple movements (including simply sitting upright) absolutely exhausting. Just walking around, I felt as if I had lead weights attached to my feet.

Heart rate and blood pressure increased. I felt anxious and crawling out of my skin while at the same time feeling completely fatigued. Every time I laid down to rest, the closer I got to actual sleep, my legs and arms would “zap” like crazy. Maddening! I drifted off to sleep once—briefly—only to dream I was being electrocuted. Yeah, that’s pretty bad. I was up all night for days. Thank God for TV, Internet, and movies.

Day 5-7+: Once at least a week had gone by (maybe a bit more) the symptoms were raging away, I did not feel any better, and I began to notice things. Weird smells. I thought that I, myself, smelled rancid — like the lope was seeping out of my pores. All my sheets had to be washed and re-washed because of the stink (that was really distressing, but it went away after a few days). Lights were too bright and everything was too loud and too sharp. And I absolutely hated being touched! My skin was hypersensitive. Even something light brushing against me made me violently uncomfortable.

The one good thing is, detoxing off loperamide didn’t seem to result in traditional cravings or nausea, so I didn’t have to deal with that. I’ve heard that other people had horrible problems with nausea thought. One might also consider the raging return of the libido a fun thing. Enjoy.

**Full disclosure: after about 10? days of these withdrawal symptoms, I gave up and went back to using the lope, but with a strict taper down schedule which was completed 21 November 2013. I jumped from 6 per day to zero and STILL had to go through a slightly milder version of this same withdrawal syndrome.



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How long does loperamide withdrawal last? For me, it was about 8 weeks, but the worst of it was over after about 5 weeks. Keep in mind, prior to quitting, I did a fast taper — if I’d just gone cold turkey from 80 pills/day, the withdrawal would have been much more intense and would have lasted much longer. That’s experience, not assumption talking.

Now, at 10 weeks, I’m still having trouble sleeping (and sometimes diarrhea), but just about all the symptoms have passed and it’s not nearly as bad as it was when I started.



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Why do I go through withdrawal?

No matter how you look at this, it’s gonna suck. Do it by yourself, it’ll suck. Get help from a doctor, it’s gonna suck, but it’ll probably suck a lot less with help. so you might as well ask for it. Speaking for myself, I KNOW I couldn’t have succeeded in detoxing off the loperamide without the support of modern medicine.

This is a major change for you and your body. Understand that there is an underlying science to why your body is reacting the way it is. For instance, the Restless Legs Syndrome (the zaps in your arms and legs) will be occurring because of the way that loperamide interacts with the nerves throughout your body and in your heart. It isn’t just those opioid receptors, but loperamide suppresses certain aspects of the conduction of your nerves as well. Think of the loperamide as a big, warm, wet blanket, extinguishing the ‘fire’ in the nerves and suppressing any normal activity that might occur. Lift that blanket off and you get cold, harsh hyperactivity — nerves zip along full blast, just as if you were panicking. The brain also goes a bit nutso firing on all cylinders. All this hyperactivity is exhausting which is why fatigue becomes such a huge problem. Some of the weakness is likely related to all the opioid receptors being depleted along the myenteric plexus along the digestive system. The small intestine, and even the large, are basically just big muscles propelling digestive material along the gastrointestinal tract. Simply put, weakened muscles = fatigue.

Important note: This blog intends to supply anecdotal guidance and assistance but is not a replacement for professional medical advice. See your doctor and discuss your options with him/her before taking any medication.

First of all, whatever you do, don’t take the loperamide. It’ll be unbelievably hard because you know this will fix it. Please put that away, get rid of it, flush it, and don’t even consider it as a way out. It’s a way deeper into addiction, just delaying the inevitable withdrawal syndrome.

My doctor chose not to use Suboxone or Subutex therapy (opioid replacement drugs) which I am ultimately grateful for. I’ve heard nightmare stories about people who say it makes them feel like crap, then they get hooked on the buprenorphine and can’t avoid long-term withdrawal. You don’t need suboxone to get through it — it may simply add to your misery and further prolong withdrawal. Talk to your clinician and let that decision be his/hers.

There are other medications that can help.

First of all, be a good communicator with your doctor. If you get confused easily (and in a withdrawal state, you might!) make notes and take them with you. Be honest with the doctor too. Constant rigorous honesty is going to be your best friend from now on, so get started right now. Docs take you more seriously if you communicate well and are honest with them.

Clonidine is most commonly used to treat opioid withdrawal symptoms. It’s an “Alpha Blocker” that functions through the brain to block some of that adrenaline that’s causing the racing feeling throughout your body. It will calm your fired up nerves and ease that RLS that’s so excruciating. It should also suppress the Hot/Cold flashes. Trust your Auntie Margaret on this. As I learned the hard way, everything will feel so much better once you take it properly. Don’t chintz on the clonidine — it’s worth it.

Your moods will likely be all over the place, so this is where your doc can be your new best friend. An anti-depressant may help with the deep pit of depression that can settle in, but not everybody needs it so talk to your doc. Even though loperamide doesn’t cross into the brain in any quantity ordinarily, if you’ve been on high doses of the stuff, that’s a different story. As your brain heals, you may need an SSRI antidepressant to combat those feelings of hopelessness. It can take up to 6 weeks for these types of medications to work, but don’t let that stop you from trying it if you need it. I’m traditionally a fast responder; I know within a day or two if I’m starting to lift out of the fog, so it’s worth it if you need it. I’m on Viibryd, but that’s a very new medication; they may try you on Lexapro or Prozac or something of that ilk first. The anti-depressant thing is best determined by a physician (or your own Square-Jawed NP).

Sleeping will be a problem. There are non-scheduled drugs that can help. First line of defense will probably be Hydroxyzine which is rather like Benadryl on steroids. Some people respond very quickly to the hydroxyzine so don’t scoff until you try it. My NP also tried Trazodone — another drug often used in opioid withdrawal management because of its deep sedating qualities. Used responsibly, these medications can really help so if insomnia is a big problem for you, give them a try.

Once you start feeling a bit more like yourself, you can use all that extra energy to get out and do things (like walk, run, exercise) but for now, lay back and let the meds do their jobs. Keep your brain busy though. Lots of movies, marathon watch some TV series, do crosswords if you can concentrate long enough. Start a hobby if you have enough energy to.

The diarrhea is going to be the least of your problems until the other symptoms get under control, and that’s what you’re left with. Sadly, there isn’t much you can do about it. It has to run its course. Get a good quality toilet paper and indulge in some flushable wipes — lots of them. The minute you think you have to go, GO. Don’t try to be a hero. Dietary changes (eat more cheese, for instance) will help a little. Pepto-Bismol can help a little too. Mainly — as I have discovered — it’s going to be a long time before it gets back to normal, and you’ll have to just wait it out and do what you can until it resolves. It could be many weeks before that gets back to normal (mine’s still raging after 2 months).

Good nutrition — watch your B-Vitamins and make sure you get enough Potassium, Magnesium, and Calcium (basically, all the electrolytes) — will be vitally important. Your doc may want to check things by running a Blood Test to see where you are and monitor you in the future.Mainly, the big thing you need between you and the drug is time. And it will take a lot of time. Loperamide has a very long half-life, so it takes a few days to get into complete withdrawal (about a full week, usually), and it’ll take multiple weeks to start feeling like yourself again. And even more weeks to have the various symptoms of withdrawal ease off. Use that time wisely to improve yourself and to make sure you don’t need to go back and use — ever — whether that’s your original drug of choice or the loperamide. Either one will kill you, so you really have little choice. Buck up little camper.

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Do I have to join AA or NA?

Well nobody’s going to force you (unless you go to jail) but it’s worth a shot. It’s another way to continue strengthening yourself so you can deal with real life again.This is not endorsement, but I do have to recommend (and I can’t believe I’m actually saying this) the AA (Alcoholics Anonymous) or the NA (Narcotics Anonymous) programs. Check In The Rooms for scheduled times/locations near you — bigger cities have AA meetings on virtually every corner at every hour. If you live in a small crap-town like I do, expect the meetings will be much less frequent. It would have helped me if someone explained what happens, so I’ll pass what I know on to you.

What to expect: People at these meetings are usually very friendly and helpful. Don’t be afraid to go. That was my big thing when I first started — I was afraid of what to expect, and I was also deathly afraid of being recognized at one of the meetings. Don’t worry about it — you’ll be fine. They’re called “anonymous” for a reason and members respect that. The meetings are structured usually with readings for about 10 minutes, then discussion on a AA/NA related topic. Just like Robert’s Rules of Order, there are certain traditions that are strictly followed. For instance, everyone introduces themselves prior to talking (i.e., “My name is Joe and I’m an alcoholic” — the response from the group is “Hi Joe”). And do not interrupt a speaker at all! It’s considered very bad form and you may get scolded! Otherwise, sit back and listen. You’ll find you’re not alone in how you feel now, and what you did when you were using.

When you go in, someone may ask you if you need ‘numbers’ — this means phone numbers and names of fellow members whom you can call who will help support you through the process. This is perfectly cool — take them and say thank you. You’ll find lots of new friends this way — it doesn’t suck. When you call, introduce yourself (i.e., “This is Joe, the new guy from the meeting”) and just discuss whatever. They’ll ask you how you’re doing; feel free to be honest. They’ve been there and can help you get through it. You might be thinking you don’t need this crap, but go with it anyway — what do you have to lose? It does help — so try it!

They’ll talk about the steps, and may ask if anyone needs a copy of the Big Book (the Alcoholics Anonymous Text is now available online!). They’ll tell you to get a sponsor and start ‘working’ your steps. You’ll start with the first three and go from there. Look ’em up! These groups really do help, so go to as many meetings as you can, especially at first. You’ll find there are a lot of old timers who go all the time too, just for the feeling of community and cameraderie, so you won’t be the weirdo who attends too many meetings. These old timers feel like that it’s a safe place they can be honest and share the things that only other addicts/alcoholics can understand. So will you.

Also, you may find you get sick and tired of hearing the platitudes after a bit (Easy Does it, One Day at a Time, etc.), but just go with it. There’s a method to their madness.

I’m not a huge proponent of the 12-step programs; I’m often critical of them to be honest. But — they’re still useful, so it’s still worth a shot. Give it a chance.

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Do I have to go to therapy or see a shrink?



Again, unless ordered by the courts, nobody’s gonna force you to do anything. But it can’t hurt. If you need therapy, use this time to get it. It’ll help you to get to the root of why you were using in the first place which will, in turn, give you fertile ground to build a new life from that doesn’t include drugs or booze. It can also help you deal with the destruction you’ve left in your wake (which, depending on how much/long you’ve used, could be pretty overwhelming). I’m still seeking a real therapist, and have an appointment set up for next month. In the meantime, my Square-Jawed NP (that little Nazi!) has been indulging in a little ‘therapy’ with me keeping me on the straight and narrow even though he’s technically medication management only. (He knows I haven’t been able to find a shrink in this crummy ‘burg).

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But what if I don’t have insurance?

Don’t let that stop you! There are options. Either try to get signed up to the Obamacare thing, or, if you have little-to-no income, go to your local Social Services Department and get yourself signed up for Medicaid. You can ask for emergency assistance if you qualify. You won’t get your choice of the best doctors in the universe, but seeing somebody is better than nobody — it’ll pay for your meds too — and there’s NO COPAY with Medicaid (at least here in NY).

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What else?

You’re going to feel tired and crappy for a long time. Some exercise will help, believe it or not. Work those abdominals as much as you can. Take it easy on yourself. Someone told me to think of myself as being in the ICU in these first few weeks of sobriety. After that — and you’ll know it when it happens — you’ll feel like you’ve finally raised your head above the fog. It’ll feel strangely cool. That’s how you know the worst has passed.

The rest will come. In time.

Best of luck.

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“Success is not final, failure is not fatal: it is the courage to continue that counts.” ― Winston Churchill

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