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Imodium Abuse and Use in Opioid Withdrawal

Imodium is actually an opioid medication that is sold over the counter to treat diarrhea. Recently, it has become a significant drug of abuse and been used as a self-treatment drug for opioid withdrawal.

Imodium

Loperamide is an over-the-counter opioid agonist medication that is popularly sold under the brand name Imodium. It is also available in generic forms.

It is primarily used to decrease diarrhea in individuals with gastroenteritis and other gastrointestinal issues. It is designed for oral use and has been used for medical reasons since the 1970s. 

Loperamide is on the List of Essential Medicines published by the World Health Organization.

Mechanism of Action

Loperamide acts on the mu-opioid receptors in the large intestine in ways that are similar to morphine. It decreases tension in the muscles located in the intestinal wall, allowing for material to remain in the intestine for a longer period while more water is absorbed from fecal matter. This is why it can treat diarrhea. 

Although it is an opioid agonist and acts in a manner that is similar to morphine, it is not readily absorbed from the intestines into the blood. When used as designed, significant amounts of the drug will not cross the blood-brain barrier. 

With regular use, the drug does not produce the euphoria associated with the use of other opioid drugs.

Availability

As an over-the-counter medication, Imodium is widely available, typically in 2 mg (milligrams) capsules. For adults, the standard dosage is an initial dose of 4 mg and then continuing amounts of 2 mg doses as needed. 

For children under age 12, only half of this dosage is recommended. 

To achieve the types of euphoric effects that occur with other opioids, an incredibly large amount of the drug would need to be taken, such as 50 to 100 2 mg capsules at one time.

All drugs have a side effect profile, and loperamide is no different, even though it is commonly available over the counter. The side effects associated with loperamide use include:

  • Sedation and lethargy
  • Headache, dizziness, and dry mouth
  • Gastrointestinal effects, including nausea, vomiting, and constipation
  • Potential allergic reactions – In rare cases, allergic reactions can include swelling of the lips or extremities, rash, hives, confusion, and anxiety. Allergic reactions should be addressed by a medical professional.

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Abuse

Under normal circumstances, Imodium is not considered to be a potential drug of abuse. However, the active ingredient in the drug, loperamide, is a potent opioid medication.

Since it is not absorbed readily from the intestines, it was not believed to be a potential drug of abuse until recently. Today, there are anecdotal reports of individuals taking extremely high amounts of Imodium to achieve opioid-like effects. 

These amounts are in the range of 50 mg or even higher. Doses this large can be potentially dangerous (see below). 

The drug has been referred by many as “poor man’s methadone” because it is inexpensive, can be obtained over the counter, may produce opioid-like effects in high doses, and is believed by some to address withdrawal symptoms from opioids.

Imodium Use for Opioid Withdrawal

Anecdotal reports have claimed that high doses of Imodium have helped some people manage opioid withdrawal symptoms. However, no formal scientific research studies suggest that high doses of Imodium can reduce pain, and the medication is not designed to treat symptoms associated with opioid withdrawal. 

There have been some animal studies that suggest that the drug may address withdrawal symptoms, but it is not approved for this purpose in humans. 

The use of high doses of loperamide to address withdrawal symptoms may simply result in a person using the drug as an opioid replacement medication or as a substitute for their opioid of choice. 

These individuals would most likely continue to take high doses of Imodium when they begin to experience withdrawal.

Woman holding her stomach and pills

This isn’t a safe practice without medical supervision. Instead, medical detox is recommended to address opioid withdrawal.

Potential Overdose

Loperamide is not meant to be used in single doses over the 4 mg amount that is typically recommended for adults. If you are instructed to use a greater amount by your physician, this practice is safe for a short period. 

However, no physician would recommend that any individual take 50 mg or more of Imodium at one time. Such a high dose could trigger a potential overdose similar to the overdose associated with other opioid drugs

The symptoms could include:

  • An exacerbation of the side effects listed above
  • Central nervous system suppression that could result in significantly decreased heart rate or breathing rate
  • Damage to the liver
  • Slurred speech, problems with motor coordination, and issues with attention and alertness
  • Cardiac dysfunction
  • Urinary retention and gastrointestinal issues
  • Serious dehydration that can be potentially dangerous
  • A comatose state

Treating an Overdose

The potential for serious brain or other organ damage can occur with an overdose of Imodium, and a serious overdose could be potentially fatal.

Because Imodium is typically used orally, overdoses are very often treated with activated charcoal, the application of a stomach pump, and even the use of the opioid antagonist drug naloxone, which is commonly used in cases of opioid overdose.

Restrictions on Imodium

Because of the increased abuse of loperamide, in January 2018, the U.S. Food and Drug Administration (FDA) reported that it would enforce restrictions on the packaging of over-the-counter forms of loperamide to control such abuse. 

Packages would be limited to eight 2 mg capsules. Whether or not the substance will be classified as a controlled substance by the U.S. Drug Enforcement Administration remains to be seen.

Sources

(November 2018). Loperamide Hydrochloride. Drugs.com. Retrieved February 2019 from https://www.drugs.com/monograph/loperamide-hydrochloride.html

(August 2017). WHO Model Lists of Essential Medicines. World Health Organization. Retrieved February 2019 from https://www.who.int/medicines/publications/essentialmedicines/en/

(2013). An Introduction to Medicinal Chemistry. Oxford University Press from

(2017). Complete Guide to Prescription and Nonprescription Drugs 2018-2019. Penguin Press from

(July 2018). Diarrhea: A New Indication Contributing to the Opioid Epidemic? Pharmacy Times. Retrieved February 2019 from https://www.pharmacytimes.com/contributor/marilyn-bulloch-pharmd-bcps/2018/07/diarrhea-a-new-indication-contributing-to-the-opioid-epidemic

(2013). Rosen's Emergency Medicine-Concepts and Clinical Practice E-Book. Elsevier Health Sciences from

(January 2017). Loperamide Abuse Associated with Cardiac Dysrhythmia and Death. Annals of Emergency Medicine. Retrieved February 2019 from https://www.sciencedirect.com/science/article/pii/S019606441630052X

(January 2018). Opioid Crisis Leads FDA to Restrict Imodium. WebMD. Retrieved February 2019 from https://www.webmd.com/digestive-disorders/news/20180130/opioid-crisis-leads-fda-to-restrict-imodium

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