Destone

Each uncoated tablet contains: Ursodeoxycholic Acid, USP 300 mg.

Pharmacology: Pharmacokinetics: Ursodeoxycholic acid is absorbed from the gastrointestinal tract and undergoes enterohepatic recycling. It is partly conjugated in the liver before being excreted into the bile. Under the influence of intestinal bacteria the free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid, some of which is excreted directly in the faeces and the rest absorbed and mainly conjugated and sulfated by the liver before excretion in the faeces. However, in comparison with chenodeoxycholic acid, less ursodeoxycholic acid undergoes such bacterial degradation.

Ursodeoxycholic acid is a naturally occurring bile acid present in small quantities in human bile. Ursodeoxycholic acid suppresses the synthesis and secretion of cholesterol by the liver and inhibits intestinal absorption of cholesterol. It is used for the dissolution of cholesterol-rich gallstones in patients with functioning gallbladders.

The licensed dose is 6 to 12 mg/kg daily as single bedtime dose or in 2 or 3 divided doses; obese patients may require up to 15 mg/kg daily. The daily dose may be divided unequally and the larger dose given before bedtime to counteract the increase in biliary cholesterol concentration seen overnight. The time required for dissolution of gallstones is likely to be between 6-24 months depending on stone size and composition. Treatment should be continued for 3 to 4 months after radiological disappearance of the stones.
A dose of 300 mg twice daily has been suggested for the prevention of gallstones in patients undergoing rapid weight loss. Ursodeoxycholic acid has also been given in reduced doses in combination with chenodeoxycholic acid.
Ursodeoxycholic acid is also used in primary biliary cirrhosis. The usual dose is 10 to 15 mg/kg daily in 2 to 4 divided doses. Ursodeoxycholic acid has been tried in the treatment of primary sclerosing cholangitis. The more hydrophilic derivative, tauroursodeoxycholic acid, has also been used.

Known hypersensitivity or intolerance to Ursodeoxycholic acid (Destone) or any of the components of the formulation.

Ursodeoxycholic acid should not be given to patients with intestinal and hepatic disorders that interfere with entero-hepatic circulation of bile salts. It is ineffective for the dissolution of calcified and pigment gallstones and is of no value in patients without a patent and functioning gallbladder. Licensed product information recommends that its use should be avoided in pregnancy.

Ursodeoxycholic acid may cause nausea, vomiting and other gastrointestinal disturbances; diarrhoea is reported to occur less frequently than with chenodeoxycholic acid. Increased liver enzyme values are also less likely. Pruritus may occur. Treatment with ursodeoxycholic acid may cause more calcification of cholesterol stones than chenodeoxycholic acid.

Ursodeoxycholic acid should not be used with drugs that increase bile cholesterol such as oestrogenic hormones and cholesterol-lowering drugs such as clofibrate. Use with bile-acid binding drugs including antacids, charcoal, and colestyramine should be avoided since this may reduce the effectiveness of therapy with ursodeoxycholic acid.

Store at temperatures not exceeding 30°C.

Cholagogues, Cholelitholytics & Hepatic Protectors

A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.

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