Obeliva 5 (Obeticholic Acid) Tablets

Obeliva 5 is manufactured in the form of film-coated tablets:

• Dosage Form and Packaging: 1 bottle contains 30 film-coated tablets. The bottle is packaged in a cardboard box with security features.
• Active Ingredient: Obeticholic Acid INN — 5 mg per tablet.
• Excipients: Microcrystalline cellulose, sodium starch glycolate, magnesium stearate, hypromellose, titanium dioxide, macrogol, protective film coating.

Pharmacodynamics: Obeticholic acid is a selective and potent agonist of the farnesoid X receptor (FXR), a nuclear receptor expressed in the liver and intestine. FXR activation suppresses bile acid synthesis from cholesterol by downregulating CYP7A1 enzyme expression, reduces bile acid concentration in hepatocytes, stimulates bile transport out of the liver, and exerts anti-inflammatory and antifibrotic actions.

Pharmacokinetics: Following oral administration, obeticholic acid is rapidly absorbed from the GI tract. Peak plasma concentration is reached within 1.5–2 hours. The drug is more than 99% bound to plasma proteins. It conjugates with glycine or taurine in the liver and is secreted into bile, participating in enterohepatic circulation. Excretion occurs primarily via feces (about 85%).

Obeliva 5 is prescribed by a physician for the following conditions:

• 🔹 Primary Biliary Cholangitis (PBC): Treatment of primary biliary cholangitis (formerly known as primary biliary cirrhosis) in combination with ursodeoxycholic acid (UDCA) in adults with an inadequate response to UDCA monotherapy.
• 🔹 PBC Monotherapy: Treatment of primary biliary cholangitis as monotherapy in adult patients who are intolerant to UDCA.
• 🔹 Other Cholestatic Conditions: As indicated by a specialist in specific cholestatic liver lesions (within clinical guidelines).

Obeliva 5 is intended exclusively for oral administration:

• 💊 Starting Dose: The recommended starting dose is 5 mg (1 tablet) once daily orally.
• ⏱️ Dose Titration: If an adequate reduction in ALP and bilirubin levels has not been achieved after 6 months of therapy and the drug is well tolerated, the dose may be increased to a maximum of 10 mg once daily.
• ⚠️ Administration Details: Tablets should be swallowed whole with water, with or without food. Patients with severe hepatic impairment require adjustment of the dosing regimen under medical supervision.

The use of Obeliva 5 is contraindicated in the following conditions:

• ❌ Hypersensitivity to obeticholic acid or to any of the excipients in the drug.
• ❌ Complete biliary tract obstruction (obstructive jaundice).
• ❌ Decompensated liver cirrhosis (Child-Pugh Class B and C) or a history of liver decompensation events.
• ❌ Severe hepatic failure without strict medical monitoring.
• ❌ Children and adolescents under 18 years of age (efficacy and safety have not been established).

When using Obeliva 5 concurrently with other medicinal products, consider the following factors:

• ⚠️ Bile Acid Binding Resins (cholestyramine, colestipol): Bind obeticholic acid in the GI tract and reduce its absorption. Obeliva 5 should be taken at least 4 hours before or 4 hours after taking bile acid sequestrants.
• ⚠️ CYP1A2 Substrates with Narrow Therapeutic Index (e.g., theophylline, tizanidine): Obeticholic acid may increase their plasma concentrations (monitoring required).
• ⚠️ Warfarin: A decrease in International Normalized Ratio (INR) may occur; regular INR monitoring is required during co-administration.

The use of Obeliva 5 during pregnancy is contraindicated or restricted due to a lack of sufficient clinical safety data for the fetus. Women of childbearing potential should use reliable contraceptive methods during therapy. Breastfeeding should be discontinued during treatment, as the excretion of obeticholic acid in human milk is unstudied.

Side effects of Obeliva 5 depend on dosage and individual susceptibility:

• 🧴 Dermatological Reactions (Very Common): Pruritus (skin itching) of varying severity, dry skin, rash.
• 🧠 General Symptoms (Common): Fatigue, weakness, dizziness, headache.
• 🍖 Digestive System: Abdominal pain, abdominal discomfort, diarrhea, constipation, or nausea.
• 🔬 Laboratory Parameters: Reduction in HDL-cholesterol levels (beneficial cholesterol), mild alterations in liver transaminase levels.

Symptoms of Overdose: Exacerbation of side effects, severe pruritus, elevation of liver enzymes, signs of hepatotoxicity.

Overdose Treatment: If overdose is suspected, immediately discontinue the drug. Gastric lavage, administration of activated charcoal or bile acid sequestrants, and symptomatic and supportive therapy should be performed under monitoring of liver function tests.

Rules for storing Obeliva 5:

• 🌡️ Temperature Regime: Store in a dry, light-protected place at temperatures between 15 °C and 30 °C.
• 💧 Moisture Protection: Keep in the original bottle with the cap tightly closed to protect from moisture and light.
• 👶 Safety: Keep safely out of reach of children and pets. Do not use after the expiration date.

To confirm the authenticity of Obeliva 5, pay attention to the following features:

• 🛡️ Packaging and Logo: The Everest company logo (stylized droplet with dots) is clearly printed on the box and bottle. The box is silver-gray with light blue and dark blue stripes.
• 🔍 Marking: The batch number (Batch No.), date of manufacture (Mfg Date), and expiration date (Exp Date) are embossed or printed on the side of the box and bottle label. A quality security emblem/hologram is present on the front.
• 📦 Protective Bottle: Plastic bottle features a child-resistant cap and tamper-evident seal (protective membrane under the cap). Film-coated tablets have a distinct uniform shape.