Ursodiol capsules are used for dissolution of gallstones in patients with radiolucent, noncalcified gallbladder stones less than 20 mm in greatest diameter who are not candidates for cholecystectomy because of systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or refusal of surgery; considered pharmacologic treatment of choice in these patients.
Dissolution of gallstones usually requires several months of ursodiol therapy. Complete dissolution of gallstones does not occur in all patients, and recurrence, which may occur within 5 years, is reported in up to 50% of patients who have achieved dissolution of the stones with the drug. Monitor for recurrence of stones.
(See Adequate Patient Monitoring under Cautions.)
Successful dissolution of gallstones with ursodiol occurs rarely in patients with calcified gallstones prior to treatment, those who develop stone calcification or gallbladder nonvisualization during treatment, and those with gallstones exceeding 20 mm in greatest diameter.
Successful dissolution is more likely in ursodiol-treated patients with floating or floatable stones (i.e., those with high cholesterol content) and dissolution is inversely related to stone size for stones less than 20 mm in greatest diameter.
Gallbladder nonvisualization prior to treatment is not a contraindication to ursodiol therapy; however, discontinue treatment in patients who develop gallbladder nonvisualization during therapy since this is predictive of failure for complete dissolution.
Prevention of Gallstones
Ursodiol capsules are used for prevention of gallstone formation in obese patients undergoing rapid weight loss.
Ursodiol reduces incidence of gallstone formation in obese patients experiencing rapid weight loss secondary to a very low calorie diet or following gastric bypass surgery.
Primary Biliary Cirrhosis
Ursodiol tablets are used for treatment of primary biliary cirrhosis.
Although optimal treatment for primary biliary cirrhosis remains to be established, many clinicians consider ursodiol the preferred initial treatment.
Substantial improvement in total bilirubin, AST, ALT, alkaline phosphatase, IgM concentrations, and histologic signs of disease has been reported in patients given ursodiol for primary biliary cirrhosis.
In controlled studies, improved biochemical markers (e.g., reduction in serum bilirubin) often were not accompanied by symptomatic improvement or prevention of complications of liver disease (e.g., ascites, GI bleeding). In addition, the impact of favorable changes in bilirubin concentrations on survival and need for liver transplantation has not been elucidated.
Ursodiol reduces the incidence of and delays time to treatment failure (defined as death; need for liver transplantation; histologic progression by 2 stages or to cirrhosis; development of varices, ascites, or encephalopathy; marked worsening of fatigue or pruritus; inability to tolerate the drug; a doubling of or an increase to 1.5 mg/dL or higher of serum bilirubin concentrations; voluntary withdrawal from study or discontinuance of study for any reason).
Ursodiol may delay progression of hepatic fibrosis in patients with early-stage disease; however, in majority of studies no improvement in fibrosis reported.
Ursodiol may delay development of esophageal varices and may improve pruritus.