Is Loperamide the Next Drug of Abuse?

I always had this weird feeling in pharmacy school about loperamide (Imodium).  I remember learning about it when we were taught about opioids.  At the time, I couldn’t help but think why isn’t this a controlled substance if it has opioid activity?  I’m sure I learned at some point that the rate entry of loperamide across the blood-brain barrier and into the brain is extremely low.

In a recent article on Medscape, loperamide abuse is discussed.  Apparently if you take enough Loperamide, the blood-brain barrier can be overcome to a certain extent.  There are reports that people, looking to find a cheap and easily accessible opioid are turning to Loperamide.  So what’s the problem with that?

The dose that one has to take to get enough in the system to experience the opioid activity on the central nervous system is ridiculously high.  There are reports of Loperamide use in the range of 50-100 times the usual dose.

The problem with high dose Loperamide is that it can stop your heart, which is obviously a really bad thing. With Loperamide, at these crazy high doses that can have central acting opioid activity, it can also have significant cardiac effects that can be lethal.

So what do you think, with tightening restrictions on opioids, is loperamide the next drug of abuse? If so, is it going to go the way of Sudafed or become an Rx only product?


  1. Larry KIMANI

    We need to think of safer ( less abuse potential) meds than loperamide as we continuously work on eradicating the root cause of the diarrhea

  2. DeLinda McDaniel

    The dose listed in facts and comparisons is 20 tablets and has been known as a drug of abuse for over 20 years. It was once listed as a class IV narcotic. As was Lomotil.

  3. Leslee Ellsmere

    It isn’t new, it was being abused back when I was a pharmacy student over 25 years ago. It’s just making its rounds again. Opioids were becoming easier to get and inject so it fell out of favour but with the recent push to keep a lid on the opioids they are back to crushing and injecting loperamide.

  4. Shaikh Hussam Lateef

    Pharmacies should not dispense a patient more than the maximum daily dose 16 mg I think that is applicable.


    Lomotil has never been OTC. Loperamide is (Imodium). Confusion has always existed in the two names. Aspirin taken 10-100 times the usual dose is not too safe either. This is just a (cynical) case where a useful drug is abused and potentially (will be) restricted to the American public. This is similar to saying that a sugar substitute should be removed from the market because monkeys injected the equivalent of 350 cans of diet soda per day, developed bladder tumors. Sucaryl “bit the dust” in 1969. Although it was determined to be “safe” later, Sucaryl has yet to be remarketed even for diabetics.


    Unfortunately this useful drug will have FDA intervention due to abuse of an OTC drug.

  7. Sean Navin

    If there are to be any limits for this med, make it behind-the-counter like Sudafed.


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Written By Eric Christianson

July 3, 2016

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