Ursodiol, a naturally occurring hydrophilic bile acid, derived from cholesterol, is present as a minor fraction of the total human bile acid pool. Oral administration of ursodiol increases this fraction in a dose related manner, to become the major biliary acid, replacing/displacing toxic concentrations of endogenous hydrophobic bile acids that tend to accumulate in cholestatic liver disease. In addition to the replacement and displacement of toxic bile acids, other mechanisms of action include cytoprotection of the injured bile duct epithelial cells (cholangiocytes) against toxic effects of bile acids, inhibition of apoptosis of hepatocytes, immunomodulatory effects, and stimulation of bile secretion by hepatocytes and cholangiocytes.

URSO 250 and URSO Forte (ursodiol) tablets are bile acids indicated for the treatment of patients with primary biliary cholangitis.

• Recommended adult dosage: 13-15 mg/kg/day administered in two to four divided doses with food.
• Scored URSO Forte tablet: scored tablet can be broken in halves to provide recommended dosage.

Most common adverse reactions reported with the use of ursodiol during worldwide postmarketing and clinical experience (≥1%) are, in alphabetical order: abdominal discomfort, abdominal pain, alopecia, diarrhea, nausea, pruritus, and rash.

Patients with complete biliary obstruction and known hypersensitivity or intolerance to ursodiol or any of the components of the formulation.

Abnormal Liver Function Tests: Liver function tests (γ-GT, alkaline phosphatase, AST, ALT) and bilirubin level should be monitored. Treatment discontinuation should be considered if parameters increase to a level considered clinically significant in patients with stable historical liver function test levels. Caution should be exercised to maintain patients’ bile flow.
• Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis: Monitor for obstructive gastrointestinal symptoms; if symptoms occur, hold ursodiol until a clinical evaluation has been conducted.