Obeticholic Acid
Generic Details
Generic Name
Obeticholic Acid
Other Names
- Ocaliva
Drug Class
- Farnesoid X receptor agonist
Chemical Formula
C26H44O4
Molecular Weight
420.63 g/mol
Mechanism of Action
- Activates the farnesoid X receptor (FXR) to regulate bile acid synthesis and transport
Indications
- Primary biliary cholangitis (PBC)
- Nonalcoholic steatohepatitis (NASH)
Common Dosage Forms
- Tablet
Typical Dosage
- 5 mg to 10 mg once daily
Pediatric Dosage
- Safety and efficacy not established in children
Geriatric Dosage
- Dosage adjustment may be needed based on renal function
Side Effects
- Pruritus
- Fatigue
- Abdominal pain
- Headache
- Nausea
- Hyperlipidemia
Contraindications
- Complete biliary obstruction
- Liver decompensation
- Hypersensitivity to obeticholic acid
Pregnancy Category
- Not recommended for use during pregnancy
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Bile acid sequestrants
- Cyclosporine
- Warfarin
Overdose Symptoms
- No specific antidote available
Antidote for Overdose
- Supportive care and symptomatic treatment
Storage Conditions
- Store at room temperature away from moisture and heat
Pharmacokinetics
- Absorption: Well absorbed after oral administration
- Distribution: Highly bound to plasma proteins
- Metabolism: Undergoes extensive hepatic metabolism
- Excretion: Excreted in feces (75%) and urine (20%)
Precautions
- Monitor liver function tests regularly
- Risk of liver decompensation in certain patient populations
Warnings
- May increase the risk of liver-related complications
- May cause exacerbation of liver impairment in certain patients
Others
- Regular monitoring is essential during treatment with obeticholic acid