Ursodiol Medicine - Information, Side effects and uses of Ursodiol

Orally administered ursodiol is indicated for dissolution of cholesterol gallstones in selected patients with uncomplicated radiolucent gallstone disease. However, alternative therapies should be considered since gallstone dissolution with ursodiol may require many months of treatment, complete dissolution does not occur in all patients, and recurrence of stones occurs within 5 years in about 50% of patients who have had stones dissolved by use of bile acid therapy.

Ursodiol therapy is more likely to be effective if the stones are small (< 20 mm) and of the floatable type. Ursodiol increases bile flow. In chronic cholestatic liver disease, ursodiol appears to reduce the detergent properties of the bile salts, thus reducing their cytotoxicity. Also, ursodiol may protect liver cells from the damaging activity of toxic bile acids (e.g., lithocholate, deoxycholate, and chenodeoxycholate), which increase in concentration in patients with chronic liver disease.

Anticholelithic - Although the exact mechanism of ursodiol's anticholelithic action is not completely understood, it is known that when administered orally ursodiol is concentrated in bile and decreases biliary cholesterol saturation by suppressing hepatic synthesis and secretion of cholesterol, and by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution.

Ursodiol is not indicated when there are calcified cholesterol stones, radiopaque stones (calcium-containing), or radiolucent bile pigment stones; when the gallbladder is not functioning ; or when surgery for gallstones is clearly indicated.

Precaution and Warning while taking Ursodiol

• Studies in rats with intrarectal instillation of lithocholic acid and other metabolites of ursodiol and chenodiol did not show evidence of tumorigenicity, except when these substances were administered in conjunction with a carcinogenic agent. Epidemiologic studies suggest that bile acids might be involved in the pathogenesis of human colon cancer in patients who have undergone a cholecystectomy; however, conclusive evidence is lacking.
• It is not known whether ursodiol is distributed into breast milk.
• Patients sensitive to other bile acid products may be sensitive to ursodiol also.
• Appropriate studies on the relationship of age to the effects of ursodiol when used as an anticholelithic have not been performed in the pediatric population. However, studies performed to date in children and infants with cholestatic liver disease and biliary atresia have not demonstrated pediatrics-specific problems that would limit the usefulness of ursodiol in children.
• Appropriate studies on the relationship of age to the effects of ursodiol have not been performed in the geriatric population. However, geriatrics-specific problems that would limit the usefulness of this medication in the elderly are not expected.