loperamide (Imodium)
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Introduction
Tradename: Imodium.
Indications
- adjunctive therapy for management of diarrhea
Contraindications
- diarrhea secondary to infection
- bloody diarrhea
- temperature > 101 F
Dosage
- 4 mg PO initially, then 2 mg PRN, max 16 mg/day
- pediatrics:
- if clinical improvement is not noted in 48 hours, discontinue use
Tabs: 2 mg.
Pharmacokinetics
- 40% absorbed after oral administration
- elimination 1/2life is approximately 11 hours
- 25% of the drug is eliminated unchanged in the feces
- does not cross blood brain barrier
elimination via liver
Adverse effects
- uncommon (< 1%)
- 2 cases of fatal misuse of loperamide
- both cases involved men with substance use disorder managed with buprenorphine who were using loperamide to self-treat opioid withdrawal[5]
- cardiac arrhythmias with misuse & abuse[6][8]
- QT interval prolongation, torsades de pointes or other ventricular arrhythmias, syncope, & cardiac arrest[8]
- increasing reports of abuse[7]
Laboratory
Mechanism of action
- slows intestinal motility
- affects water & electrolyte movement through the bowel
- inhibits peristalsis by directly effecting circular & longitudinal muscles of the intestinal wall
- acts on opioid receptors[5]
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Deprecated Reference
- ↑ 5.0 5.1 5.2 Orciari Herman A, Sadoughi S, Saitz R OTC Diarrhea Drug Increasingly Being Misused for Opioid Effects. Physician's First Watch, May 12, 2016 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org
Eggleston W et al Loperamide Abuse Associated With Cardiac Dysrhythmia and Death. Ann Emerg Med. 2016 Apr 26. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27140747 <Internet> http://www.annemergmed.com/article/S0196-0644%2816%2930052-X/pdf - ↑ 6.0 6.1 FDA Saftey Communication. June 7, 2016 Loperamide (Imodium): Drug Safety Communication - Serious Heart Problems With High Doses From Abuse and Misuse. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm505303.htm
- ↑ 7.0 7.1 7.2 Pallin DJ Increasing Reports of Loperamide Abuse. NEJM Journal Watch. Nov 10, 2016 Massachusetts Medical Society (subscription needed) http://www.jwatch.org
Vakkalanka JP et al. Epidemiologic trends in loperamide abuse and misuse. Ann Emerg Med 2016 Nov 4 PMID: https://www.ncbi.nlm.nih.gov/pubmed/27823872 - ↑ 8.0 8.1 8.2 Brooks M. FDA Acts to Stem Misuse, Abuse of Antidiarrheal Loperamide. Medscape - Jan 30, 2018. https://www.medscape.com/viewarticle/891968
FDA Safety Alert. Jan 30, 2018 Imodium (loperamide) for Over-the-Counter Use: Drug Safety Communication - FDA Limits Packaging To Encourage Safe Use. https://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm594403.htm