Products
Eluxadoline was approved in the form of film-coated tablets in the US in 2015, in the EU in 2016, and in many countries in 2018 (US: Viberzi, EU, CH: Truberzi).
Structure and properties
Eluxadoline (C32H35N5O5, Mr = 569.7 g/mol)
Effects
Eluxadoline (ATC A07DA06) has antidiarrheal and analgesic properties. It is an agonist at μ-opioid receptors, an antagonist at δ-opioid receptors, and an agonist at κ-opioid receptors. Binding to the opioid receptors normalizes intestinal motility and bowel movements. Antagonism at the δ-receptor is thought to result in less constipation as a side effect compared with pure μ-agonists such as loperamide. Eluxadoline is predominantly effective locally in the intestine due to low oral bioavailability.
Indications
For the treatment of irritable bowel syndrome with diarrhea (IBS-D / IBS-D).
Dosage
According to the SmPC. Tablets are taken in the morning and evening with food.
Abuse
Eluxadoline has a low potential for abuse.
Contraindications
For complete precautions, see the drug label.
Interactions
Eluxadoline is a substrate and inhibitor of OATP1B1 and has potential for inactivation of CYP3A4. Eluxadoline should not be combined with drugs that inhibit intestinal transit (eg, loperamide).
Adverse effects
The most common possible adverse effects include constipation, nausea, and abdominal pain. Rare cases of pancreatitis have been reported.
