BACKGROUND Loperamide is widely used in adults for acute diarrhea. However, its use in children has been discouraged by the World Health Organization and the American Academy of Pediatrics owing to concerns over safety and efficacy in young children. METHODS AND FINDINGS To assess the efficacy and adverse effects of loperamide compared with placebo for acute diarrhea in children, we reviewed ...

Background: Although the use of the antimicrobial, trimethoprim-sulfamethoxazole, in combination with the antisecretory and antimotility agent, loperamide, has been shown to be efficacious in the treatment of traveler's diarrhea, the use of fluoroquinolone antimicrobials in combination with loperamide has less support in the literature. The present study was designed to compare the efficacy of ...

3 Wuster M, Herz A. Opiate agonist action of antidiarrhoeal agents in vitro and in vivo-findings in support for selective action. Naunyn Schmiedebergs Arch Pharmacol 1978;301:187-94. 4 Niemegeers CJE, McGuire JL, Heykants JJP, Janssen PAJ. Dissociation between opiate-like and antidiarrheal activities of antidiarrheal drugs. J Pharmacol Exp Ther 1979;210:327-33. 5 Van Nueten JM, Janssen PAJ, Fon...

Verapamil has been shown to inhibit fentanyl uptake in vitro and is a potent P-glycoprotein inhibitor. Tissue partitioning of loperamide, a commercially available opioid, is closely controlled by the P-gp efflux transporter. The following studies were designed to evaluate the effect of opioids on verapamil partitioning in the lung and brain, in vivo. Opioid (fentanyl or loperamide) was administ...

To determine if loperamide is effective and safe in treating watery diarrhoea, we randomly assigned 50 adult expatriates in Bangladesh with more than three unformed stools in the previous 24 hours and illness of less than 72 hours to receive loperamide or a placebo. On entry into the five day study patients took two capsules (one loperamide capsule = 2 mg) and one after each unformed stool up t...

Loperamide, an effective antidiarrheal agent, was investigated in attempts to determine the site of action which underlies the antiperistaltic and other antidiarrheal actions. In in vitro studies, this compound applied in a dose over 10-8 g/ml, inhibited the release of both acetylcholine and prostaglandins during circumferential distension of the intestinal wall, in a dose dependent manner. The...

OBJECTIVE Loperamide, a non-prescription anti-diarrheal agent, is a peripheral mu-opioid receptor agonist that is excluded from the blood-brain barrier by p-glycoprotein at therapeutic doses. Overdoses of loperamide penetrate the central nervous system (CNS), leading to abuse. We report cardiac conduction abnormalities and dysrhythmias after ingestion of a recreational supra-therapeutic dose of...

Antimicrobial drug treatment of travelers' diarrhea is known to increase the risk for colonization with extended-spectrum β-lactamase-producing Enterobacteriaceae. Among 288 travelers with travelers' diarrhea, the colonization rate without medications was 21%. For treatment with loperamide only, the rate was 20%; with antimicrobial drugs alone, 40%; and with loperamide and antimicrobial drugs, ...

With increasing restrictions and safety protocols implemented in prescribing opioids, there has been an increased incidence of recreational abuse of over-thecounter medications, including loperamide. Loperamide is a peripherally-acting μ-opioid receptor agonist in the gastrointestinal tract which, if taken at high doses, can cross the blood-brain barrier to produce euphoria and analgesia effects.

Thirty-three Collies (14 male and 19 female) were used in a doseescalation study to determine the impact of ABCB1 genotype on loperamide pharmacokinetics (PK) and pharmacodynamics (PD). Loperamide was orally administered in four ascending doses (0.01, 0.05, 0.1, or 0.2 mg/kg) over a 4-wk period to fasted Collies. Comparisons were made within each dose to genotype, phenotype, and whether Collies...