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?

Written By Eric Christianson

July 3, 2016

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