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| http://dx.doi.org/10.1080/20009666.2017.1361294 | DOI Listing |
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Peripherally mediated opioid combination therapy in mouse and pig.
J Pain
November 2024
Department of Neuroscience, University of Minnesota Medical School, USA; Department of Pharmacology, University of Minnesota Medical School, USA; Department of Dermatology, University of Minnesota Medical School, USA.
The concomitant epidemics of chronic pain and opioid misuse in the United States have led to a call for novel analgesics with limited abuse potential. Previously, we have shown that co-delivery of a novel combination targeting both μ- and δ-opioid receptors in the peripheral and central nervous systems can produce synergistic analgesia. Loperamide, a peripherally restricted μ-opioid agonist, and oxymorphindole, a δ-opioid receptor partial agonist, synergize in multiple mouse models of hyperalgesia.
View Article and Find Full Text PDFLoperamide-Induced Torsades de Pointes.
Cureus
July 2024
Cardiology, University of Pittsburgh Medical Center (UPMC) Harrisburg, Harrisburg, USA.
Loperamide is a readily available, over-the-counter medication used to treat diarrhea. At therapeutic doses, loperamide exerts its effects mainly on the intestinal opioid receptors with minimal psychoactive effects; however, at supratherapeutic doses, it reaches central opioid receptors. With tighter regulations on opioid prescriptions, loperamide has emerged as a popular drug of abuse among opioid users.
View Article and Find Full Text PDFLoperamide positive deaths in Sweden 2012-2022 and Finland 2017-2022: Fatal loperamide intoxication exclusively for Sweden.
Forensic Sci Int
August 2024
Department of Forensic Genetics and Forensic Toxicology, National Board of Forensic Medicine, Linköping 587 58, Sweden; Division of Clinical Chemistry and Pharmacology, Department of Biomedical and Clinical Sciences, Linköping University, Linköping 581 83, Sweden.
Loperamide, a potent μ-opioid receptor agonist used as an antidiarrheal drug, exhibits increased bioavailability at supratherapeutic doses, causing potential central nervous system effects. Its misuse for opioid withdrawal relief and euphoria can lead to dangerously elevated blood levels, causing severe cardiac dysrhythmias and death. This study aimed to compare loperamide positive autopsy cases in Sweden and Finland after the introduction of postmortem toxicological analysis of loperamide, focusing on loperamide's role in fatalities and identifying common characteristics among those affected.
View Article and Find Full Text PDFOver-the-counter medications encountered in the postmortem pediatric population from 2010-2020.
J Anal Toxicol
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Toxicological Services, NMS Labs, 200 Welsh Rd, Horsham, PA 19044, USA.
In forensic toxicology, the pediatric population requires special focus when evaluating positive findings because of the many toxicokinetic and toxicodynamic differences (e.g., metabolic capabilities, body size, etc.
View Article and Find Full Text PDFManagement of loperamide-related opioid use disorder with buprenorphine within an Australian context: A case report.
Drug Alcohol Rev
September 2024
Illawarra Drug & Alcohol Service, Illawarra Shoalhaven Local Health District, Wollongong, Australia.
Loperamide is an over-the-counter peripheral mu-opioid agonist commonly used to manage diarrhoea. When taken in an excessive dose, loperamide's penetration of the central nervous system increases, leading to euphoria, respiratory depression and other opioid effects. A health warning was released in the United States in 2016 with increased reports of excessive loperamide use leading to cardiac conduction abnormalities such as ventricular tachycardia, prolonged QTc and Torsades des Pointes.
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