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eluxadoline

MOR agonist; DOR antagonist; KOR agonist · Gastrointestinal motility agent

MOR agonist; DOR antagonist; KOR agonistGastrointestinal motility agentATC A07DA05
CDSCO approvedATC A07DA05
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • ArtesunateSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter
  • BexaroteneSevereDatabaseDDInter
  • CobicistatSevereDatabaseDDInter

Mechanism

Eluxadoline is a mixed mu opioid receptor (MOR) agonist, delta opioid receptor (DOR) antagonist, and kappa opioid receptor (KOR) agonist. It acts locally in the GI tract to reduce abdominal pain and diarrhea without causing significant constipation.

Indications

Diarrhea-predominant IBS (in adults)

Dosing

Adult
100 mg twice daily with food (for diarrhea-predominant IBS with a gallbladder). 75 mg twice daily (for patients without a gallbladder).

Pharmacokinetics

Peak effect
1.5 to 2 h
Half-life
3.7 to 6 h
Excretion
In feces (drug and metabolic products)

Contraindications

  • Known or suspected biliary duct obstruction
  • Sphincter of Oddi disease or dysfunction
  • History of pancreatitis
  • Structural diseases of the pancreas
  • Patients without a gallbladder (dosing adjustment required)

Side effects

Common
ConstipationNauseaAbdominal pain
Serious
  • Sphincter of Oddi spasm
  • Pancreatitis
  • Potential for addiction

Drug interactions

Artesunate
Severe
Database

Clinical effect not specified

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bexarotene
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cyclosporine
Severe
Database

Clinical effect not specified

Source: DDInter

Daclatasvir
Severe
Database

Clinical effect not specified

Source: DDInter

Darolutamide
Severe
Database

Clinical effect not specified

Source: DDInter

Eltrombopag
Severe
Database

Clinical effect not specified

Source: DDInter

Ethanol
Severe
Database

Clinical effect not specified

Source: DDInter

Gemfibrozil
Severe
Database

Clinical effect not specified

Source: DDInter

Grazoprevir
Severe
Database

Clinical effect not specified

Source: DDInter

Lapatinib
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about eluxadoline

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team