Generic
Obeticholic Acid
29 brands available in the market
At a glance
Obeticholic Acid is a Farnesoid X Receptor (FXR) agonist used for primary biliary cholangitis (PBC). It activates FXR to reduce bile acid synthesis and increase bile acid transport out of hepatocytes, reducing hepatic bile acid exposure.
Description
Obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine. FXR activation decreases intracellular hepatocyte bile acid concentrations by suppressing de novo synthesis from cholesterol and increasing transport of bile acids out of hepatocytes.
Indications
- Primary biliary cholangitis (PBC) — in patients without cirrhosis or with compensated cirrhosis who do not have evidence of portal hypertension
- In combination with UDCA in patients with inadequate response or as monotherapy in patients unable to tolerate UDCA
Therapeutic class
Farnesoid X Receptor Agonists
Pharmacological class
FXR Agonist
Pharmacology
Obeticholic acid activates FXR to suppress de novo bile acid synthesis in the liver and increase transport of bile acids out of hepatocytes, reducing hepatic bile acid exposure and limiting the circulating bile acid pool.
Mechanism of action
Treats PBC by reducing hepatic bile acid concentration.
Dosage
Adult Dose (Oral):
- Noncirrhotic or compensated Child-Pugh A: 5 mg/day for first 3 months; increase to 10 mg/day if adequate response not achieved and tolerated
- Child-Pugh B or C, or prior decompensation: 5 mg once weekly; increase to 5 mg twice weekly (at least 3 days apart) if adequate response not achieved and tolerated; may titrate to 10 mg twice weekly based on response and tolerability
Administration
- May take with or without food
- Separate from bile-acid binding resins by at least 4 hours
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects (>10%):
- Pruritus (56-70%)
- Fatigue (19-25%)
- Severe pruritus (19-23%)
- Reduced HDL-C (9-20%)
- Abdominal pain and discomfort (10-19%)
Uncommon (1-10%):
- Rash, oropharyngeal pain, dizziness, constipation, peripheral edema, palpitations, pyrexia, thyroid function abnormality, eczema
Precautions & warnings
- Hepatic decompensation and failure reported in patients with decompensated cirrhosis (Child-Pugh B/C) or prior decompensation event
- Contraindicated in compensated cirrhosis with evidence of portal hypertension (ascites, gastroesophageal varices, persistent thrombocytopenia)
- Monitor for elevations in liver enzymes and risks for hepatic decompensation
- Monitor HDL-C
Contraindications
- Decompensated cirrhosis (Child-Pugh B or C) or prior decompensation event
- Compensated cirrhosis with evidence of portal hypertension (ascites, gastroesophageal varices, persistent thrombocytopenia)
- Complete biliary obstruction
Drug interactions
- Bile-acid binding resins may reduce absorption and systemic exposure; separate by at least 4 hours
- May decrease INR with warfarin; monitor INR and adjust warfarin dose
- May increase exposure of CYP1A2 substrates (theophylline, tizanidine)
- Avoid concomitant use of BSEP inhibitors (cyclosporine)
Food interactions
May be taken with or without food.
Use in pregnancy
Use in Pregnancy: Limited human data on use during pregnancy; no developmental abnormalities observed in animal studies.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No information on presence in human milk; consider benefits and risks of breastfeeding.
Pediatric use
Safety and effectiveness not established in pediatric patients.
Geriatric use
No overall differences in safety or effectiveness between elderly and younger patients.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed.
Hepatic Impairment: Contraindicated in decompensated cirrhosis or portal hypertension; caution.
Overdose effects
Overdose: Dose-dependent hepatic adverse reactions (liver enzyme elevations, ascites, jaundice, portal hypertension); monitoring and supportive care.
Storage conditions
Store below 30°C in a dry place, protect from light; keep out of reach of children.
Chemical structure
Obeticholic Acid