Obexa 10 | Farnesoid X Receptor (FXR) Agonists
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Home Medicines Liver Obexa 10mg Tablet 1 Strip

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Obexa 10mg Tablet 1 Strip

Generic: Obeticholic Acid

Type: Tablet

Pack Size: 10 Pcs

Obexa is prescribed for adults diagnosed with Primary Biliary Cholangitis (PBC) who either:

  • Do not have cirrhosis, or
  • Have compensated cirrhosis without signs of portal hypertension.
  • It can be used:
  • In combination with ursodeoxycholic acid (UDCA) when the response to UDCA alone is insufficient, or
  • As monotherapy in patients intolerant to UDCA.

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✅ Description:

Obeticholic acid activates the Farnesoid X Receptor (FXR) found in the liver and intestines. FXR plays a crucial role in controlling bile acid levels, inflammation, fibrosis, and metabolism. Its activation reduces bile acid build-up in liver cells by:

  • Suppressing bile acid synthesis from cholesterol
  • Enhancing their excretion from hepatocytes
  • This action reduces the circulating bile acid pool and encourages bile flow, lowering hepatic bile acid exposure.

Pharmacodynamics:
Daily dosing with 10 mg obeticholic acid led to a 173% rise in FGF-19, a bile-regulating hormone, over 12 months. It also reduced levels of cholic acid and chenodeoxycholic acid. The clinical implications of these changes remain unclear.

Cardiac Safety:
No significant QT interval prolongation was observed at doses up to 10 times the recommended level.

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✔️ Dosage & Administration

Pre-treatment Assessment:
Before starting therapy, assess for:

Decompensated cirrhosis (Child-Pugh Class B/C)

Previous hepatic decompensation

Portal hypertension (e.g., ascites, varices, low platelets)

Obexa is contraindicated in such cases.

Recommended Dosage:

Start at 5 mg once daily for 3 months.

If necessary and tolerated, increase to 10 mg once daily based on liver function tests (ALP and bilirubin).

  • Pediatrics: Not established for children.
  • Elderly (65+ years): No major safety differences noted, but increased sensitivity is possible.
  • Hepatic Impairment: Contraindicated in decompensated liver disease or portal hypertension due tothe risk of serious hepatic side effects.
✔️ Managing Severe Pruritus:

Consider adding antihistamines or bile acid sequestrants.

Modify dose:
• 5 mg every other day (if 5 mg daily is not tolerated)
• 5 mg daily (if 10 mg daily is intolerable)

Interrupt therapy temporarily (up to 2 weeks) and resume at a lower dose if needed.

✔️ Monitoring:
  • Regularly monitor liver biochemistry and signs of worsening PBC.
  • Patients with cirrhosis or concurrent liver disease should be watched closely for portal hypertension or hepatic decompensation.
  • Discontinue if evidence of liver failure, biliary obstruction, or severe hepatic events arises.
✔️ Side Effects

Common adverse effects include:

Itching (pruritus)

Fatigue

Abdominal discomfort

Others: rash, joint pain, throat irritation, dizziness, constipation, thyroid irregularities, and skin inflammation (eczema)

✔️ Drug Interactions
  • Bile Acid Binding Agents (e.g., cholestyramine) may interfere with Obexa absorption. Space doses by at least 4 hours.
  • Warfarin May reduce INR. Monitor and adjust warfarin dose.
  • CYP1A2 Substrates (e.g., theophylline): Obexa may elevate their blood levels. Therapeutic drug monitoring is advised.
  • BSEP Inhibitors (e.g., cyclosporine): Concomitant use may raise hepatic bile salt accumulation. Use with caution and monitor liver function.
✔️ Contraindications

Decompensated cirrhosis or history of liver decompensation

Portal hypertension in compensated cirrhosis

Complete bile duct obstruction

✔️ Use in Pregnancy and Lactation

Pregnancy:
Limited human data. Animal studies show no harm at high doses. Use only if needed.

Lactation:
Unknown if excreted in breast milk. Weigh the benefits of breastfeeding against the mother's treatment needs and potential risk to the infant.

✔️ Precautions & Warnings

Liver Complications in Cirrhosis:
Liver failure and decompensation, some fatal or requiring transplant, have occurred, especially in cirrhotic patients. Risk increases with higher doses or pre-existing liver issues. Monitor liver function closely.

Severe Itching:
Occurs in up to 23% of patients at the 10 mg dose. It can severely affect daily life. Consider dose adjustment, symptomatic treatment, or interruption of therapy.

HDL-C Reduction:
Obexa may lower HDL (good cholesterol). Monitor lipid levels, particularly in long-term use or when treatment response is poor.

✔️ Overdose

Higher-than-recommended doses (25–50 mg) have led to liver-related side effects. If overdose occurs, provide supportive treatment and monitor liver function closely.

✔️ Storage

Store below 30°C, in a dry, dark place. Keep away from the child

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