ursodeoxycholic acid




DCH Auriga
Full Prescribing Info
Ursodeoxycholic acid.
Ursodeoxycholic acid is a bile acid which is physiologically synthesized in the human liver and is also formed by bacteria in the large intestine. It is present in human bile making up 1.4-4% of the biliary bile acids. Ursodeoxycholic acid is an epimer of chenodeoxycholic acid; it differs from this bile acid only in the configuration of the hydroxyl group in the C7-position.
Pharmacology: Cholesterol gallstones are formed when there is an excess of cholesterol in the bile. Ursodeoxycholic acid inhibits the enzymatic synthesis of cholesterol in the liver, and this leads to a reduction of the cholesterol content in bile. The lithogenic index of bile is decreased. Due to the lower concentration of cholesterol in bile, cholesterol stones gradually dissolve. An additional advantage of this treatment is the disappearance of gastrointestinal symptoms within 2-4 weeks in many patients.
Pharmacokinetics: Ursodeoxycholic acid is absorbed by a purely passive, nonionic transport in the jejunum and in the upper part of the ileum. In the terminal ileum, ursodeoxycholic acid is absorbed actively. For absorption, ursodeoxycholic acid must be solubilized in micelles, as it has a low solubility at the pH present in the small intestinal lumen.
At a dosage of 350-1000 mg/day, the absorption rate amounts to 80-90%. Absorbed ursodeoxycholic acid is quickly conjugated in the liver with glycine or taurine and is then secreted into bile. The conjugates of ursodeoxycholic acid are reabsorbed from the intestine; hence during administration, it becomes the predominant biliary bile acid. In the intestinal tract, these conjugated bile were hydrolysed and metabolised.
Studies in mice and biliary fistula rats have shown that oral and IV administration of ursodeoxycholic acid mostly distributed in the liver, bile and gastrointestinal tract after instantaneous absorption. Ursodeoxycholic acid is scarcely detectable in the other tissues and organs. Most ursodeoxycholic acid is excreted in faeces as lithocholic acid.
Dissolution of cholesterol gallstones; stones must be radiolucent, and inspite of gallbladder stones, the gallbladder must be functioning.
As adjuvant medication for dissolution of gallstone fragments in conjunction with shock-wave lithotripsy treatment of patients with gallbladder stones.
Biliary reflux gastritis. Cholestatic liver diseases (eg, PBC).
Dosage/Direction for Use
Medical Dissolution of Gallstones: Daily Dose: 2-5 caps, depending on body weight (10 mg/kg body weight/day).
Dosage Recommendations: 2 caps/day (1 cap in the morning, 1 cap in the evening); 3 caps/day (1 cap in the morning, 2 caps in the evening); 4 caps/day (1 cap in the morning, 3 caps in the evening); 5 caps/day (2 caps in the morning, 3 caps in the evening).
The capsules must be taken regularly, otherwise therapy will not be successful. The duration of the dissolution of cholesterol gallstones requires usually 3 months to 2 years up to present knowledge. If there is no decrease of stone size after 18 months, further treatment seems not to be useful. The success of treatment should be controlled by gallbladder x-ray in intervals of 6 months.
Special Recommendations: Liver tests, SGOT, SGPT and γ-GT are recommended in the first 3 months all 4 weekly. Later, these tests are only necessary in a quarterly interval.
Adjuvant Medication in Conjunction With Shock-Wave Lithotripsy: Recommended Dose: 7-8 mg/kg body weight/day of Ursofalk and Chenofalk as a single daily dose to be taken in the evening. This adjuvant litholytic therapy is generally begun before the shock-wave treatment in order to reduce the saturation of the bile as far as possible. The therapy is continued for 3 months after the time that no more fragments are visible in the gallbladder. This regimen has the purpose of dissolving any extremely small residual fragments that can no longer be seen.
Cholestatic Liver Diseases: Same as Medical Dissolution of Gallstones.
Biliary Reflux Gastritis: 1 cap before retiring at night.
Inflammatory diseases of the bile duct, obstructive hepatobiliary diseases, acute cholecystitis. Parenchymal diseases of the liver (acute or chronic hepatitis); inflammatory bowel disease. Starvation diet.
Use in pregnancy: Pregnant women and fertile women who do not use contraceptive protection.
Use In Pregnancy & Lactation
Use in pregnancy: Pregnant women and fertile women who do not use contraceptive protection.
Side Effects
In a small percentage of patients, pulpy stools may occur. There is no reason to discontinue the therapy. Other side effects are not known up to date.
Drug Interactions
Simultaneous administration of cholestyramine, colestipol (colestid) or aluminum hydroxide-containing antacids together with Ursofalk is not appropriate since these drugs bind ursodeoxycholic acid and prevent its absorption.
MIMS Class
Cholagogues, Cholelitholytics & Hepatic Protectors
ATC Classification
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.
Cap 250 mg x 100's.
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