obeticholic acid: clinical use

Prescribing considerations

• Confirm hepatic status before initiation and reassess the benefit–risk balance if liver function deteriorates.
• Treatment should be specialist supervised, with attention to biochemical response and tolerability.
• Severe pruritus may require symptomatic treatment, treatment modification or discontinuation.
• Interrupt treatment during severe intercurrent illness or clinically significant hepatic adverse reactions while liver function is evaluated.

Contraindications and cautions

• Hypersensitivity to obeticholic acid or an excipient
• Decompensated cirrhosis, including Child–Pugh class B or C
• Any previous hepatic decompensation event
• Complete biliary obstruction

Monitoring

• Clinical and laboratory evidence of PBC progression or hepatic adverse reactions
• Alkaline phosphatase, bilirubin and liver transaminases
• Features of portal hypertension or decompensation, including ascites, jaundice, variceal bleeding and encephalopathy
• Severity and tolerability of pruritus
• INR with concomitant warfarin
• Appropriate monitoring for narrow-therapeutic-index CYP1A2 substrates

Clinical pharmacology

A selective, potent FXR agonist that suppresses bile-acid synthesis, increases transport of bile acids from hepatocytes and promotes choleresis. It undergoes hepatic glycine and taurine conjugation with enterohepatic recirculation; elimination is mainly faecal.

Formulation and product differences

• The selected presentation is a yellow, round 5 mg film-coated tablet marked “INT” and “5”.
• The tablet is essentially sodium-free and may be taken with or without food.

Tablet

Route: Oral

Strengths: 5 mg, 10 mg