Generic

Ursodeoxycholic Acid

Indications

This drug is indicated for the dissolution of small to medium sized radiolucent, cholesterol rich gall-stones in functioning gall bladders. This drug is also indicated for the treatment of primary biliary cirrhosis.

Pharmacology

Ursodeoxycholic acid is a natural bile acid used to treat different liver and gallbladder diseases. The activity of ursodeoxycholic acid is achieved by reducing the secretion of cholesterol in the bile. Ursodeoxycholic acid achieves this through several mechanisms: it reduces the absorption of cholesterol, inhibits the synthesis of cholesterol in the liver, and does not inhibit the synthesis of bile acids.

Therefore, it changes the composition of bile from supersaturated to unsaturated. Ursodeoxycholic acid also promotes the formation of liquid cholesterol crystal complexes, thereby enhancing the excretion of cholesterol from the gallbladder to the intestine. Ursodeoxycholic acid improves cholestatic liver disease

Protects bile duct cells from the cytotoxicity of hydrophobic bile acids
Stimulates hepatobiliary secretion. Protects liver cells from bile acid-induced apoptosis

Ursodeoxycholic acid in the intestine The upper part is completely absorbed. The time to reach peak serum concentration ranges from 30 to 150 minutes. The absorption rate is between 60% and 80%. Ursodeoxycholic acid enters the portal vein after absorption, and is extracted from the portal vein blood through the liver, combined with amino acids, which can be glycine or taurine, and then secreted into the hepatobiliary ducts. A small amount of ursodeoxycholic acid appears in the circulation, and a very small amount is excreted in the urine. The biological half-life of ursodeoxycholic acid is 3.55.8 days.

Dosage & Administration

Dissolution of Gall stones: 8-12 mg/kg/day either as single night time dose or in divided doses.

Primary Billiary Cirrhosis: 10-15 mg/kg/day in 2-4 divided doses.

Acute Viral Hepatitis: 600 mg/day.

Alcoholic Fatty Liver: 300 mg/day.

Primary Sclerosing Cholangitis: 25-30 mg/kg/day.

Dissolution of Gallstones and Non-Alcoholic Steato Hepatitis: 13-15 mg/kg/day.

Interaction

This drug should not be administered with oral contraceptives, oestrogenic hormones and other drugs which reduce the blood cholesterol level and increase the bile cholesterol level.
Concomitant administration with bile acid-binding drugs including antacids, charcoal and cholestyramine should be avoided, since this may reduce the effectiveness of therapy with Ursodeoxycholic acid.

Contraindications

This medicine is contraindicated to radio-opaque calcified gall-stones, non-functioning gall bladder, inflammatory diseases and other conditions of the small intestine, colon and liver which interfere with the enterohepatic circulation of bile salts.

Side Effects

This drug may give rise to nausea, vomiting, diarrhea, gallstone calcification and pruritus.

Pregnancy and Lactation

Pregnancy Category B by FDA.

Precautions & Warnings

Excessive dietary intake of calories and cholesterol should be avoided. Patients with rare hereditary problems of galactose intolerance, Lap lactose deficiency or glucosegalactose malabsorption should not take this medicine.

Therapeutic Class

Anti-gallstones drugs: Bile Acids

Storage Conditions

Store below 25° C. Protected from light and moisture. Keep the medicine out of the reach of children.

Pharmaceutical Name

Drug International Ltd.