Loperamide for Opiate Withdrawal: Is it dangerous?

What Is Loperamide (Imodium): effects, signs, symptoms & how to use it?

Loperamide is a medication used to treat diarrhea. The brand name is Imodium. It is taken orally.

Loperamide is used over the counter because it does not have psychological effects at normal doses.

Loperamide can be used for the following conditions:

1. Chronic Diarrhea
2. Irritable Bowel Syndrome
3. Gastroenteritis
4. Reduce ileostomy output
5. Traveler’s diarrhea
6. Recurrent diarrhea of bowel resection
7. Inflammatory bowel disease

Loperamide is not to be used for bloody diarrhea, bacterial enterocolitis (diarrhea with infection), liver failure, HIV, and acute worsening ulcerative colitis. Not recommended during pregnancy or nursing.

Interactions:

Loperamide can interact with p-glycoprotein inhibitors like ketoconazole, ritonavir, and quinidine such as contained in Nudexta. Loperamide can inhibit as much as half the absorption of saquinavir.

Risk and severity of constipation can increase if loperamide is administered with other opioids, anticholinergics, antihistamines, and antipsychotics.

Loperamide mechanism of action

Loperamide acts as a mu-opioid receptor agonist that agonizes opioid receptors in the large intestines. It slows activity in the intestine just as other opioids can relax the mind and body. As food remains longer in the intestine, more water is absorbed so that stool is not runny. There is reduced contraction and pain in the intestine. Loperamide is little absorbed into the blood, is further reduced by the liver, and does not cross the blood-brain barrier well. This is why it has no psychoactive effect at regular doses.  Combining it with quinidine or other p-glycoprotein inhibitors can cause it to cross the blood-brain barrier and produce effects similar to other opioids. P-glycoprotein inhibitors include:

• Omeprazole and other proton-pump inhibitors
• lansoprazole,
• ketoconazole,
• felodipine,
• erythromycin,
• diltiazem,
• colchicine,
• clarithromycin,
• ciclosporin,
• amiodarone,
• verapamil,
• tamoxifen,
• sertraline,
• saquinavir,
• reserpine,
• quinidine,
• paroxetine,
• nifedipine,
• duloxetine

FAQ about loperamide

Loperamide pros & cons

Opioid withdrawal symptoms

Figure 1.https://americanaddictioncenters.org/withdrawal-timelines-treatments/opiate

Opioid withdrawal happens when a person addicted to opioid-like heroin misses a dose or runs out. They will experience withdrawal 6 to 24 hours after the last dose which can include shaking, tears, muscle pain, yawns, fear, sense of doom, racing heart, diarrhea, feeling like you’re on fire, cold flashes, craving for drugs, nausea, projectile vomiting, fever, flu-like symptoms, insomnia, incontinence, anxiety, and depression. They may cry, lack the motivation to do anything, or be in great fear and pain. Many addicts will go to extreme lengths to avoid going into withdrawal.

How much loperamide for opiate withdrawal?

Using loperamide for opioid withdrawal is something fairly new, born out of the desperation associated with the opioid epidemic in the United States. The preferred means of handling withdrawal symptoms at home is to use the herb kratom; however, it is not available in some states. And some users have used loperamide to stop withdrawals and then to wean off. While we will not endorse this practice, we will look at social media and see how people have claimed they have been able to do this.

“Almost all of my symptoms have abated.”

This user was treating withdrawals from the abuse of 30 to 40 mg of oxycontin per day. Oxycontin is the pill that started the opioid epidemic. It’s expensive and highly valued. Her dose is not a large dose. However, she was able to stave off withdrawal with 30 mg of loperamide. For her, the dose was pretty much the same as her oxycontin dose. Loperamide is related in structure to methadone. People use up to 200 mg of loperamide per day to try to stave off withdrawal or experience the high which is described as ‘dirty’ compared to preferred opioids.

Users say they may still be a little dope sick after using loperamide, or ‘lope’ in street terms. However, they are able to function and are not in severe fear and pain, on fire one second, then freezing cold the next. Opioid withdrawal nearly always requires that the sufferer cease all life activities until it lets up, which could take a week or longer, though they will be over the hump in just a few days. Opioid withdrawal is not fatal in and of itself as alcohol withdrawal is. Some in opioid withdrawal have died from secondary and related causes, but not from the withdrawal itself, alone.

“I can honestly say this is a GODSEND”

This Erowid user gives a glowing account of an 80 mg dose used for heroin withdrawals. The says he feels great. There is no high but he feels giddy and his withdrawals are gone completely. He says loperamide is for him a godsend. He plans to use a laxative for constipation in a few days.

“I saved 4 – 5 full days of puking bile…”

This Erowid user claims to have successfully used loperamide to get off of heroin, then tapered off of loperamide. He apparently only took enough loperamide to take the edge off the withdrawals, starting with 30 mg. He then reduced the dose daily by 5 mg or 10 mg. We will assume he got off and stayed off for at least a few days. Tapering slower, say 10% each day might have been a reasonable avenue to explore as well. When you go for professional help, you may be put on methadone. Methadone has a similar structure to loperamide. It has more cerebral effects and the withdrawal is horrendous. It can induce a high similar to heroin when combined with benzos. Subutex or treating withdrawal symptoms with kratom might be a better avenue.

This Erowid user would use between 60 mg and 100 mg. She says the complete removal of withdrawal symptoms happened around half a day later. She also claimed loperamide has a half-life of 24 hours, by which likely meant that’s how long it stays in your system, which would actually be a full life. She says a single dose gave her relief for 24 to 36 hours, so there is a long duration of effect.

How much loperamide to get high?

People use from 30 mg to 200 mg of loperamide to get high or to stop opioid withdrawals. The high from loperamide is said to not be strong or very pleasant. It is not a preferred high and you can expect it to come with constipation. People use it in desperation when they are withdrawing from another opioid and can’t get kratom for their withdrawals.

Is it dangerous to treat an opioid withdrawal with loperamide?

Dysrhythmias with high doses of loperamide used for opioid withdrawal.

In short, yes, it is dangerous. This Reddit user abused high doses of loperamide for a year and a half. He experienced heart problems, problems walking, blackouts, lost 3 jobs, became homeless, and ended up in the hospital with an enlarged heart. Abuse of loperamide can cause torsades de pointe, arrhythmia or irregular, fast heartbeat which can be fatal in some cases. The research currently is mostly case studies. One shows a 48-year-old woman who presented with cardia dysrhythmias after taking up to 80 mg of loperamide at a time, up to twice per day (so up to 160 mg per day). Even doses as low as 20 mg can be associated with heart problems. The maximum daily dose on the bottle is 8 mg and is not expected to be taken daily.

A study in Clinical Toxicology from 2018 combed through records of 26 patients presenting with overdoses of loperamide. Ten patients had abnormal EEG results, showing conductance problems in the heart. That is close to half. It’s safe to say high doses of loperamide prolongs QT interval and causes electrical problems for the heart. The mean dose for this study was 200 mg.

The risk of using loperamide as medicine for detox from heroin and other drugs

If you use loperamide as a way to detox from heroin and other drugs, you expose yourself to the risk of death from cardiac problems, in short. You can get an irregular heartbeat, then the heart could stop beating. You could also die from respiratory depression if the dose is too high or it is mixed with benzos or other potentiators. You could become dizzy, fall asleep, and your breathing becomes more and more shallow till it stops and suffocation ensues if no one finds you and hits you with the naloxone. Lastly, you could get severe constipation which could cause a tear in the gut lining.

The rate of these adverse effects from loperamide is not really known since abuse of loperamide is a fairly recent phenomenon. However, in the aforementioned study of those hospitalized for loperamide overdoses, about half of them had heart anomalies.

Overdose symptoms and Abuse Treatment

If you take too much loperamide, you will get symptoms of overdose.

Overdose symptoms:

• abdominal pain
• burning pain
• drowsiness
• vomiting
• constipation
• tachycardia (fast heartbeat)
• dysrhythmia (irregular heartbeat)
• dizziness
• fainting
• respiratory depression
• fatality (rare as far as we know)

How do I stop using opioids like loperamide as a drug to get high?

If you become addicted to loperamide and would like to stop doing it, you should see professional help to get off. They may put you on a methadone or buprenorphine program, or have you taper down your loperamide dosage. You may have to explain to them that loperamide in high doses is a synthetic opioid-related to methadone. The antidote for acute overdose is naloxone.

Some have successfully use the herb, kratom, to help ease some of the non-medical symptoms of withdrawal while being treated for addiction by a professional.

In order to use kratom, just purchase some ground leaf Maeng da kratom powder from a reputable vendor. Take about 4 grams or one teaspoon of the powder at the time you would have taken your opioid of choice. Simply put the teaspoon of kratom into about 4 ounces of water and give it 10 minutes to dissolve or stir it up till it’s all in the water. Drink it down. It will kick in in 20 minutes and can get rid of all or most of your withdrawal symptoms. The duration of the effect of kratom is not long so you may have to dose often. However, take no more than an average of one teaspoon every two hours. Opioid users all over the world have had success with kratom. Kratom produces a mood boost but very little or no euphoric high. It can treat the non-medical symptoms of withdrawal from loperamide.

General Medical Disclaimer

Leaf Expert does not give medical advice. Consult your doctor if you believe you need medical treatment for a DSM diagnosed the addictive disorder. This article is about what social media reveals about how addicts are using loperamide to stave off opioid withdrawal symptoms.

FDA Disclaimer

Loperamide is sold as an OTC medication regulated by the FDA. Leaf Expert does not sell loperamide nor advocate or discourage use or abuse.

Drug Screening Disclaimer

If you use kratom for loperamide withdrawal, it could be tested for in some contexts.

Kratom is not regularly tested for in drug tests; however, because it often shows up in users of other opioids, some medical based drug tests will look for it and its presence can affect treatment. Especially tests at methadone clinics may look for kratom and there could be punitive actions taken if it is discovered.