Ocaliva

Ocaliva regulates bile acid metabolism, inflammatory response and fibrosis pathways by activating FXR receptors in the liver and intestines.

1. Drug name

1. Common name: Obeticholic Acid (ObeticholicAcid)

2. Trade name: OCALIVA®

2. Indications

1. For the treatment of primary biliary cholangitis (PBC) in adults:

Patients without cirrhosis;

Patients with compensated cirrhosis but no evidence of portal hypertension.

2. It can be used in combination with ursodeoxycholic acid (UDCA) (when UDCA response is insufficient), or as a monotherapy for patients with UDCA intolerance.

3. Specifications and properties

5mg, tablet.

IV. Main ingredient

1. Active ingredient: obeticholic acid.

2. Excipients: microcrystalline cellulose, sodium starch glycolate, magnesium stearate, etc.

5. Usage and dosage

1. Initial dose of : 5mg once a day, orally for 3 months.

2. Dose adjustment : If the efficacy is insufficient after 3 months and the drug is well tolerated, it can be increased to 10 mg once a day (maximum dose).

3. Missed dose/vomiting : No need to make up the dose, just take the next dose as originally planned.

4. Medication time : before or after meals, but the interval between taking the drug and the bile acid-binding resin must be at least 4 hours.

VI. Dose adjustment

1. Intolerance to itching : the dose can be reduced to 5 mg once every other day or suspended for 2 weeks and then restarted.

2. Deterioration of liver function : Permanent discontinuation of the drug is required when portal hypertension or hepatic decompensation occurs.

7. Medication Precautions

1. Contraindicated use of in combination: Contraindicated in patients with complete biliary obstruction, decompensated cirrhosis (Child-Pugh B/C grade) or portal hypertension.

2. Monitoring requirements : Regularly check liver function, blood lipids (HDL-C may decrease) and INR (when combined with warfarin).

3. Special storage : There is no clear requirement. It is recommended to store it at room temperature and away from light.

8. Medication for special groups

1. Pregnant women : There is no risk in animal experiments, but there is insufficient human data.

2. U200c during lactation: The safety is unknown, and the pros and cons need to be weighed.

3. Children/elderly : No safety data has been established.

4. Liver damage : Patients with moderate to severe liver damage require close monitoring.

9. Adverse reactions

1. Common (≥5%): itching (70%), fatigue, abdominal pain, rash, joint pain, dizziness, constipation, etc.

2. Serious risks: liver failure, portal hypertension, reduced HDL-C.

10. Contraindications

1. Decompensated cirrhosis or previous decompensated events.

2. Compensated cirrhosis accompanied by portal hypertension.

Complete biliary obstruction.

11. Drug interactions

1. Bile acid binding resin : Take it 4 hours apart.

2. Warfarin : It may reduce INR, and the dose needs to be monitored and adjusted.

3. CYP1A2 substrate (such as theophylline): may increase exposure and needs to be monitored.

4. BSEP inhibitor (such as cyclosporine): avoid combined use.