From the Guidelines
Weaning off Immodium (loperamide) is unlikely to cause significant opioid withdrawal symptoms in most individuals, as it does not readily cross the blood-brain barrier and has minimal central nervous system effects at therapeutic doses. Loperamide is an opioid receptor agonist that primarily acts on the intestinal tract to slow bowel movements, with minimal absorption into the bloodstream and limited access to the central nervous system [@1@]. Although it is theoretically possible for individuals taking very high doses of loperamide for extended periods to experience some withdrawal symptoms when stopping, such as stomach cramps, diarrhea, anxiety, or restlessness, these symptoms are typically mild and less severe than those associated with withdrawal from traditional opioids like morphine or heroin.
When considering the potential for opioid withdrawal symptoms, it's essential to differentiate between the effects of loperamide and those of other opioids. The study on ensuring patient protections when tapering opioids highlights the importance of gradual tapering to avoid acute withdrawal symptoms in patients taking opioids for pain [@1@]. However, this guidance is primarily aimed at patients taking full mu agonists, which have a much greater potential for dependence and withdrawal compared to loperamide.
For individuals who have been taking Immodium at recommended doses for short-term diarrhea treatment, stopping the medication is unlikely to result in significant withdrawal symptoms. Even for those who have been taking higher doses or using it long-term, the risk of severe withdrawal symptoms is low. If concerns about dependence or withdrawal exist, consulting a healthcare provider can help determine the best approach, which may include gradually reducing the dose over several days to minimize any potential effects. This approach allows the body to adjust to decreasing levels of the medication, reducing the likelihood of withdrawal symptoms.
From the FDA Drug Label
DRUG ABUSE AND DEPENDENCE ... Loperamide is primarily being misused for relief from opioid withdrawal, and abused by a few users who obtain some (reportedly mild-moderate) level of euphoria. In animals, parenteral administration of loperamide hydrochloride can cause physical dependence, cross-tolerance to opioids, and all the other pharmacologic effects typical of muopioid agonists Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented signs of morphine withdrawal.
Weaning off Immodium (loperamide) may cause opioid withdrawal symptoms in some individuals, especially those who have been taking high doses (60 mg or greater) or using the medication for an extended period. This is because loperamide can have CNS opioid effects at higher doses, and it is being misused for relief from opioid withdrawal. However, the FDA drug label does not provide direct evidence of withdrawal symptoms in humans after stopping loperamide use 1.
From the Research
Weaning Off Immodium and Opioid Withdrawal Symptoms
- Weaning off Immodium (loperamide) can cause opioid withdrawal symptoms, particularly in individuals who have been taking high doses of the medication 2.
- Loperamide is a peripheral mu-opioid agonist that can cross the blood-brain barrier at high doses, leading to central nervous system opioid agonism and potential for abuse 3, 4.
- Cases have been reported of individuals experiencing opioid withdrawal symptoms after stopping or reducing high-dose loperamide use, including symptoms such as euphoric effects, respiratory depression, and cardiac conduction abnormalities 2, 5, 6.
- Buprenorphine has been used to manage loperamide-associated opioid use disorder and withdrawal symptoms in several case reports, suggesting its potential as a treatment option for individuals struggling with loperamide addiction 2, 5, 6.
Key Findings
- High-dose loperamide use can lead to opioid withdrawal symptoms upon cessation or reduction 2, 4.
- Loperamide abuse can result in cardiotoxicity, including QTc prolongation, ventricular tachycardia, and torsades de pointes 3, 4, 5.
- Buprenorphine may be an effective treatment for managing loperamide-associated opioid use disorder and withdrawal symptoms 2, 5, 6.