FXR 5mg Tablet 10pcs

Uses of FXR 5mg Tablet

Primary biliary cirrhosis

How does FXR 5mg Tablet work?

Obeticholic Acid works by decreasing the production of bile in the liver and promoting the removal of bile from your liver. 

Side Effects of FXR 5mg Tablet

• Common side effects include pruritus (itching), fatigue, abdominal pain, reduced high-density lipoprotein cholesterol (HDL-C), and discomfort.
• Severe pruritus, rash, and oropharyngeal pain can occur in some patients.

Quick Suggestions:

• Obeticholic Acid can be taken with or without food.
• Avoid taking more or less than the recommended dose.
• Do not stop taking the medication without talking to your doctor. Your doctor may suggest tests to monitor your liver function and bilirubin levels periodically while you are taking this medicine.
• Eat a healthy balanced diet low in fat and exercise regularly to prevent gallstone formation.

Primary biliary cholangitis:

Primary biliary cholangitis (PBC), formerly known as primary biliary cirrhosis, is an autoimmune liver disease characterized by progressive damage to the small bile ducts in the liver. These tiny tubes, known as bile ducts, are responsible for transporting bile, a digestive fluid produced by the liver, to the small intestine. Bile plays a crucial role in the digestion and absorption of dietary fats.

In PBC, the body's immune system mistakenly targets and damages the bile ducts, leading to their inflammation and destruction. As a result, bile accumulates in the liver, causing a range of problems, including liver damage and scarring (fibrosis) over time. This continuous damage to the liver can eventually lead to cirrhosis, which is characterized by extensive scarring and impaired liver function.

PBC is considered an autoimmune disease because the immune system's attack on the bile ducts is an abnormal immune response. The exact cause of PBC is not fully understood, but genetic, environmental, and immunological factors likely play a role in its development.

Patients with PBC may experience various symptoms, including fatigue, itching (pruritus), dry eyes and mouth (Sjögren's syndrome), and, in more advanced stages, complications of liver cirrhosis. Early diagnosis and treatment are crucial to manage the condition and prevent further liver damage.

The primary treatment for PBC is ursodeoxycholic acid (UDCA), which helps manage symptoms and slow disease progression. Obeticholic acid, as described earlier, is another medication that may be used in combination with UDCA or as monotherapy in cases where UDCA is not effective or tolerated.

Regular monitoring and management of PBC are essential to maintain liver health and improve the quality of life for affected individuals.

Pharmacology

Obeticholic acid's mechanism of action involves activating the Farnesoid X receptor (FXR), which is a nuclear receptor found in the liver and gut. FXR plays a vital role in regulating various pathways, including those related to bile acids, inflammation, fibrosis, and metabolism. When obeticholic acid activates FXR, it triggers several changes in the body:

• Reducing Intracellular Bile Acids: FXR activation leads to a reduction in the concentrations of bile acids within the hepatocytes (liver cells). This is achieved by limiting the production of de novo cholesterol, a precursor to bile acids. By reducing the synthesis of new bile acids, obeticholic acid helps lower the overall bile acid levels inside the liver.
• Enhancing Bile Acid Transport: FXR activation also promotes the transport of bile acids out of the hepatocytes and into the bile ducts. This process facilitates the removal of bile acids from the liver, preventing their accumulation within liver cells.
• Reducing Hepatic Bile Acid Exposure: The combined effects of lowering intracellular bile acids and increasing their transport out of hepatocytes help reduce the exposure of the liver to excessive bile acids. This is important because elevated bile acid levels can lead to liver damage.
• Increasing Choleretic Activity: Choleretic activity refers to the production and flow of bile. By increasing choleretic activity, obeticholic acid assists in the release of bile acids from the liver into the bile ducts, which is essential for the digestion and absorption of dietary fats.

Dosage & Administration

Adult Dose:

• The recommended starting dose of Obeticholic Acid depends on the patient's condition.
• For noncirrhotic or compensated Child-Pugh class A patients, the starting dose is 5 mg once daily. If needed, it can be titrated to 10 mg once daily.
• For Child-Pugh class B or C patients, or those with a prior decompensation event, the starting dose is 5 mg once weekly. It can be titrated to 5 mg twice weekly and, if required, to 10 mg twice weekly.

Administration:

• Obeticholic Acid can be taken with or without food.
• If you are taking a concomitant bile-acid binding resin, ensure to separate the dose of Obeticholic Acid by at least 4 hours.

Interaction

• Bile-acid binding resins may reduce the absorption and efficacy of Obeticholic Acid.
• Co-administration with warfarin can decrease the INR; monitor INR and adjust the warfarin dose accordingly.
• Obeticholic Acid may increase exposure to CYP1A2 substrates, so monitor these substrates with a narrow therapeutic index.
• Avoid concomitant use of inhibitors of the bile salt efflux pump (BSEP), such as cyclosporine, as they may exacerbate the accumulation of conjugated bile salts in the liver.

Contraindications

Obeticholic Acid is contraindicated in patients with complete biliary obstruction.

Pregnancy & Lactation

There is insufficient human data on the use of Obeticholic Acid during pregnancy to establish the risk associated with the drug. There is no information on the presence of Obeticholic Acid in human milk, its effects on breastfed infants, or its impact on milk production.

Precautions & Warnings

• Obeticholic Acid should be used with caution in patients with hepatic decompensation, particularly in Child-Pugh Class B or C hepatic impairment.
• Monitor patients for elevations in liver enzymes and risks for hepatic decompensation.
• There is a dose-response relationship for liver-related adverse reactions.
• The safety of Obeticholic Acid during lactation is unknown; consider the potential benefits of breastfeeding along with the mother's clinical need for the drug.

Storage Conditions

Store between 15°C and 30°C in a dry, light-protected place. Keep it out of reach of children.