Loperamide as a Potential Drug of Abuse and Misuse: Fatal Overdoses at the Medical University of South Carolina

There have been increasing reports of misuse of a range of prescription and over-the-counter (OTC) drugs for recreational purposes. The use of psychoactive pharmaceuticals and 'pharming' are new, widespread phenomena involving the non-medical use of prescription and OTC drugs, which are recreationally used to achieve psychoactive effects either on their own or in combination with other substances. This article provides an overview of the topic, focusing on a range of medicines (e.g. prescription medicines such as quetiapine, gabapentinoids, Z-drugs, bupropion, venlafaxine, and over-thecounter medicines such as loperamide, dextromethorphan, benzydamine, promethazine, chlorphenamine, diphenhydramine and hyoscine butylbromide) that have emerged as misused and diverted, or already described through the literature, as well as recorded by drug users' online websites reporting new trends and experimentations of drug abuse. This rapidly changing drug scenario represents a challenge for pharmacy, psychiatry, public health and drug control policies. Moreover, possibly resulting from the COVID-19 pandemic, drug use-habits and availability have changed, causing a shift in behaviours relating to both prescription and OTC medicines. Healthcare professionals should be aware of potential prescription drugs diversion, recognise misuse cases, consider the possibility of polydrug misuse, and prevent it where possible. Pharmacists can play a key role in preventing and reducing drug abuse and should be involved in evidence-based actions to detect, understand and prevent drug diversion activities and the adverse effects of drug-misuse.

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“…It might be used to manage and cope with opioid withdrawal symptoms[7,40,[91][92]. Loperamide toxicity involves gastrointestinal (e.g.…”

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confidence: 99%

Misuse of prescription and over-the-counter drugs to obtain illicit highs: how pharmacists can prevent abuse

Chiappini¹,

Guirguis²,

Corkery³

et al. 2020

The Pharmaceutical Journal

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“…By 1988, loperamide was marketed as a nonprescription medication because of its low abuse potential relative to other medications within its class. 1…”

Section: Discussionmentioning

confidence: 99%

“…2 As a result, the FDA placed a black box warning for torsades de pointes, cardiac arrest, QT prolongation, and death. 1,3,8,9…”

Section: Discussionmentioning

confidence: 99%

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A Case Report of Loperamide-Induced Ventricular Storm

Vera

Kim

Sakr

2021

Journal of Investigative Medicine High Impact Case Reports

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Loperamide is an easily accessible antidiarrheal medication. Unlike other medications in its class, loperamide is unique in that it causes euphoria at supratherapeutic levels due to its effect on opioid receptors. Unfortunately, with its growing abuse potential also comes increasing reports of cardiotoxicity including prolonged QT, torsades de pointes, and sudden cardiac death. We report a case of a 29-year-old female who presented with unstable arrhythmia that further progressed into electrical storm in the setting of loperamide toxicity. Due to its growing popularity and availability, it is important for clinicians to understand loperamide’s mechanisms for causing toxicity as well as how to appropriately treat its complications.

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“…22,95 At recommended doses for a limited length of time, loperamide is an effective medication for the treatment of diarrhea. 9,[40][41][42][43][44]46,65 Additionally, it has increasingly been used for the treatment of opioid withdrawal symptoms. 44,65,67,96 Internet forum users insist loperamide may show a methadonelike effect for the treatment of substance use disorders at supratherapeutic doses.…”

Section: ■ History and Importance In Neurosciencementioning

confidence: 99%

DARK Classics in Chemical Neuroscience: Loperamide

Malinky

Lindsley

Han

2021

ACS Chem. Neurosci.

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Loperamide, a popular and inexpensive over-the-counter antidiarrheal medicine, is a potent μ-opioid receptor agonist approved by the U.S. Food and Drug Administration (FDA). It has been on the market since 1976 and is relatively safe with no central nervous system-related side effects when used for a short period of time at the recommended therapeutic dose (2−8 mg/day). In recent years, loperamide has become notoriously known as the "poor man's methadone" for people with substance dependence due to the increase in loperamide overdoses from self-administered medication to treat opioid withdrawal symptoms. As a result, in 2018, the FDA decided to limit the available packaged dose of loperamide to stop prominent abuse. This review provides the synthesis and chemical properties of loperamide as well as the pharmacology and adverse effects of its use and the social effects of such abuse.

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Loperamide as a Potential Drug of Abuse and Misuse: Fatal Overdoses at the Medical University of South Carolina

Cited by 16 publications

References 31 publications

Misuse of prescription and over-the-counter drugs to obtain illicit highs: how pharmacists can prevent abuse

Misuse of prescription and over-the-counter drugs to obtain illicit highs: how pharmacists can prevent abuse

A Case Report of Loperamide-Induced Ventricular Storm

DARK Classics in Chemical Neuroscience: Loperamide

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