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ALIMENTARY TRACT AND METABOLISM › ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS › ANTIPROPULSIVES › Antipropulsives
eluxadoline
A07DA06
Forms & Strengths
- Oral tablets: 75 mg
- Oral tablets: 100 mg
Adult Dosing
- Irritable bowel syndrome with diarrhea (IBS-D): 100 mg orally twice daily with food
- Reduced dose: 75 mg orally twice daily for patients who cannot tolerate the 100 mg dose, are receiving concomitant OATP1B1 inhibitors, have mild/moderate hepatic impairment, or are of advanced age unable to tolerate higher dose
Pediatric Dosing
- Safety and efficacy in pediatric patients below 18 years of age have not been established
Indications
- Treatment of irritable bowel syndrome with diarrhea (IBS-D) in adults
Mechanism of Action
- Mu-opioid receptor agonist and delta-opioid receptor antagonist, and a kappa-opioid receptor agonist
- Acts locally in the enteric nervous system to reduce bowel contractions and abdominal pain without significantly altering transit time
Contraindications
- Patients without a gallbladder or history of cholecystectomy
- Sphincter of Oddi disease or dysfunction
- History of pancreatitis or structural diseases of the pancreas
- Severe hepatic impairment (Child-Pugh Class C)
- History of chronic or severe alcoholism or alcohol abuse
- Known hypersensitivity to eluxadoline
Adverse Reactions
- Constipation
- Nausea
- Abdominal pain
- Vomiting
- Pancreatitis
- Sphincter of Oddi spasm
Drug Interactions
- OATP1B1 inhibitors (e.g., cyclosporine): increase systemic exposure of eluxadoline, dose reduction required
- Strong CYP inhibitors may affect metabolism
- Constipating agents (e.g., opioids, lotronex): concurrent use increases risk of severe constipation and related complications
- Alcohol: concurrent use increases the risk of pancreatitis and sphincter of Oddi spasm
Curated Content: Needs Vetting Before Put to Clinical Use