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Forensic Toxicology
Published in: Forensic Toxicology 2/2017

01-07-2017 | Review Article

“Poor man’s methadone” can kill the poor man. Extra-medical uses of loperamide: a review

Authors: Maria Katselou, Ioannis Papoutsis, Panagiota Nikolaou, Artemisia Dona, Chara Spiliopoulou, Sotiris Athanaselis

Published in: Forensic Toxicology | Issue 2/2017

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Abstract

Loperamide is a phenylpiperidine derivative and an opioid agonist that was launched by Janssen Pharmaceutica in 1973. It was initially classified in the United States as a Schedule II drug and was transferred to Schedule V in 1977; it has not been listed as a controlled substance since 1982. Loperamide is used for the symptomatic treatment of diarrhea and gastrointestinal inflammation. It has a low potential for central nervous system effects when administered in therapeutic doses. However, when used in supratherapeutic doses, either for self-treatment or drug abuse (opioid substitute), it can lead to life-threatening cardiac effects. The US Food and Drug Administration and the global community are concerned about these severe side effects, suggesting the need for control worldwide. This article reviews the existing knowledge on loperamide, including its chemistry, synthesis, pharmacology, toxicology, pharmacokinetics, biotransformation, its medicinal use, dependence potential, abuse of the drug, reported intoxications, fatalities, its determinations in biological samples, and its current legal status. All available information was gathered through a detailed search of PubMed and the World Wide Web.
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Metadata
Title
“Poor man’s methadone” can kill the poor man. Extra-medical uses of loperamide: a review
Authors
Maria Katselou
Ioannis Papoutsis
Panagiota Nikolaou
Artemisia Dona
Chara Spiliopoulou
Sotiris Athanaselis
Publication date
01-07-2017
Publisher
Springer Japan
Published in
Forensic Toxicology / Issue 2/2017
Print ISSN: 1860-8965
Electronic ISSN: 1860-8973
DOI
https://doi.org/10.1007/s11419-017-0365-x

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