2016
DOI: 10.3109/15563650.2016.1159310
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Not your regular high: cardiac dysrhythmias caused by loperamide

Abstract: Loperamide produces both QRS and QT prolongation at supra-therapeutic dosing. A blood loperamide concentration of 210 ng/mL is among the highest concentrations reported. Supra-therapeutic dosing of loperamide is promoted on multiple drug-use websites and online forums as a treatment for opioid withdrawal, as well as for euphoric effects. With the current epidemic of prescription opioid abuse, toxicity related to loperamide, an opioid agonist that is readily available without a prescription is occurring more fr… Show more

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Cited by 41 publications
(30 citation statements)
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“…Because of this, the FDA released a warning in 2016 regarding its potential for negative cardiac side effects . Since the earliest case reports in 2014, several case reports have since described the various cardiac manifestations induced by loperamide abuse . While the exact mechanisms are not completely understood, the various cardiac manifestations are suspected to be due to lopermide's effects primarily on hERG/Ikr potassium channel and cardiac sodium channels, which mimic the effect of Vaughan–Williams Class III and Class IA antiarrhythmic agents, respectively .…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…Because of this, the FDA released a warning in 2016 regarding its potential for negative cardiac side effects . Since the earliest case reports in 2014, several case reports have since described the various cardiac manifestations induced by loperamide abuse . While the exact mechanisms are not completely understood, the various cardiac manifestations are suspected to be due to lopermide's effects primarily on hERG/Ikr potassium channel and cardiac sodium channels, which mimic the effect of Vaughan–Williams Class III and Class IA antiarrhythmic agents, respectively .…”
Section: Discussionmentioning
confidence: 99%
“…3 Since the earliest case reports in 2014, 1 several case reports have since described the various cardiac manifestations induced by loperamide abuse. [4][5][6][7][8][9][10] While the exact mechanisms are not completely understood, the various cardiac manifestations are suspected to be due to lopermide's effects primarily on hERG/Ikr potassium channel and cardiac sodium channels, which mimic the effect of Vaughan-Williams Class III and Class IA antiarrhythmic agents, respectively. 11,12 Patients with predominantly Class III manifestations exhibit the expected QT prolongation and torsades de pointes VT, whereas predominantly Class IA manifestations exhibit QRS widening due to delayed sodium channel upstroke and monomorphic ventricular tachycardia.…”
Section: Discussionmentioning
confidence: 99%
“…Loperamide overdose was not suspected initially in many cases, so a level was not sent, a barrier added to the need for sending to a reference laboratory. When obtained, the serum loperamide level was significantly above the upper therapeutic range of 3.1 ng/mL in most cases …”
Section: Methodsmentioning
confidence: 91%
“…Given the outliers in values, averages for loperamide dose, QRS duration, QTc interval, and days to clinical stability or resolution of ECG changes are presented as median (interquartile range). When the dose of loperamide ingested was a range in a given case, the median for that case was entered into the calculation for overall median dosage; for example, if the dose of loperamide was 40 to 160 mg per day, then 100 mg was the contributed value from that case to the sample median loperamide dose. If the dose or QTc duration was published as “greater than” or “at least” a given value, the given value was used; for example, Eggleston in 2015 presented a patient who ingested at least 400 mg of loperamide per day .…”
Section: Methodsmentioning
confidence: 99%
“…Although laboratory confirmation was only available in four cases, clinical features were consistent with previously reported cases (2-4). Optimal management of loperamide-associated cardiac toxicity is not yet clear; multiple interventions have been reported (2,4). Health care providers and public health officials should remain vigilant for loperamide abuse and report adverse events to the U.S. Food and Drug Administration's MedWatch reporting system (http://www.fda.gov/Safety/MedWatch).…”
Section: Notes From the Fieldmentioning
confidence: 99%