Loperamide Trends in Abuse and Misuse Over 13 Years: 2002–2015

Abstract

Our data suggest that loperamide may be increasing in popularity as a drug of abuse and for treatment of opioid withdrawal symptoms. Given the potential for significant toxicity with loperamide exposure, including life-threatening cardiac dysrhythmias, clinicians should consider obtaining a screening electrocardiogram for patients presenting after acute or chronic high-dose ingestions of loperamide. In addition, increased control over the availability of loperamide may be warranted.

Ventricular fibrillation due to overdose of loperamide, the “poor man’s methadone”

“…Loperamide exhibits predominantly peripheral activity, low bioavailability, and poor blood-brain barrier penetration at the FDA-approved doses. When ingested in massive doses (40–100 times the usual dose), it can cross the blood-brain barrier and exert CNS activity similar to that of other opioids [3]. The patient in our vignette was a daily, long-term loperamide-abuser.…”

“…Since dissemination of its opioid properties in online recreational drug use forums, poison control centers have noticed a doubling in referrals for loperamide overdose since 2014 [3,4]. Loperamide has peripheral mu receptor agonistic properties in the gastrointestinal tract, and accidental and deliberate overdosage has been associated with opioid-like euphoria [5,6].…”

“…Due to its ability to control diarrhea, the same drug forums advocated for its use to control the diarrheal symptoms of opioid withdrawal, and it has been increasingly utilized in this manner [3,6]. However, with increasing abuse, there has been a concomitant increase in the number of reports of cardiotoxicity, particular dysrhythmias during the post-marketing drug safety surveillance [2,3] These reports led to a 2016 FDA warning on potential arrhythmias from usage [7]. Herein, we report prolonged cardiotoxicity in a patient abusing loperamide to manage her heroin withdrawal and review the complexities of managing this presentation.…”

Loperamide abuse and cardiotoxicity

“…Loperamide, an over-the-counter antidiarrheal agent, has seen a steady rise in recreational abuse for its opioid-like effects [1,2]. First reported on web-based forums in 2005, the USA has seen an increase in abuse over the last decade [2], doubling from 2013 to 2015 [1].…”

“…First reported on web-based forums in 2005, the USA has seen an increase in abuse over the last decade [2], doubling from 2013 to 2015 [1]. Recreational abusers report taking doses up to 400 mg/day [1].…”