Eluxadoline

Eluxadoline is a mu-opioid receptor agonist, kappa opioid receptor agonist and delta opioid receptor antagonist. It works directly in the intestine to reduce peristalsis and makes the nerves in the intestine less sensitive to stimulation. Used for IBS-D in adults. Recommended dose: 100 mg PO BID with food (75 mg BID in hepatic impairment). Discontinue if severe constipation >4 days. Contraindicated in patients without gallbladder, biliary obstruction, pancreatitis history, alcoholism and severe hepatic impairment. Common side effects include constipation, nausea, abdominal pain and dizziness.

• Diarrhea-predominant irritable bowel syndrome (IBS-D) in adult men and women

Eluxadoline is a mu-opioid receptor agonist, kappa opioid receptor agonist and delta opioid receptor antagonist. It works directly in the intestine to reduce peristalsis and makes the nerves in the intestine less sensitive to stimulation.

Eluxadoline reduces intestinal peristalsis and desensitizes intestinal nerves to relieve IBS-D symptoms.

Adult Dose: 100 mg PO BID with food. (Mild-moderate hepatic impairment: 75 mg PO BID).

Discontinue in patients who develop severe constipation lasting >4 days.

Hepatic Dose: Mild-moderate (Child-Pugh A or B): 75 mg BID; Severe (Child-Pugh C): Contraindicated.

Oral tablet. Take twice daily with food. Swallow whole.

If a dose is missed, take the next dose at the regular time and avoid taking two doses at a time.

Common Side Effects (1-10%):

• Constipation (7-8%)
• Nausea (7-8%)
• Abdominal pain (6-7%)
• URT infection (3-5%)
• Vomiting (4%)
• Nasopharyngitis (3-4%)
• Abdominal distention (3%)
• Bronchitis (3%)
• Dizziness (3%)
• Flatulence (3%)
• Rash (3%)
• Increased ALT (2-3%)
• Fatigue (2-3%)
• Viral gastroenteritis (1-3%)

Serious (<1%): Severe constipation

• Eluxadoline is a mu opioid receptor agonist; risk of sphincter of Oddi spasm leading to pancreatitis or hepatic enzyme elevation.
• Caution in patients without gallbladder.
• Evaluate alcohol intake prior to starting therapy; instruct patients to avoid chronic or acute excessive alcohol use.
• Monitor for new or worsening abdominal pain that may radiate to back or shoulder.
• Instruct patients to stop therapy and seek medical attention if symptoms of pancreatitis occur.

• Documented hypersensitivity to drug or components
• Patients who do not have a gallbladder
• Known or suspected gallbladder obstruction, biliary duct obstruction or sphincter of Oddi disease/dysfunction
• Alcoholism, alcohol abuse, alcohol addiction, or >3 alcoholic beverages/day
• History of pancreatitis, pancreatic duct obstruction, or structural diseases of pancreas
• Severe hepatic impairment (Child-Pugh C)

May interact with oral contraceptives, cyclosporine, probenecid, rosuvastatin.

No known food interactions. Take with food.

No studies in pregnant women. Animal reproduction studies showed no teratogenic effects. Use only if needed.

Unknown if distributed in human breast milk. Secreted in rat milk. Consider benefits and risks.

Safety and effectiveness in pediatric patients not established.

Limited information available regarding dose adjustment for elderly patients.

Renal impairment: Use with caution.

Hepatic impairment: Mild-moderate: 75 mg BID; Severe: Contraindicated.

Limited data on overdose. Do not exceed indicated dosing. Provide symptomatic treatment.

Store in a cool & dry place, protect from light. Keep out of reach of children.

Eluxadoline