ER-soe-dye-ole

Therapeutic Classification:

• Gallbladder stone dissolution and prevention.
• Primary biliary cirrhosis.

Unlabeled Uses:

• Biliary atresia.
• TPN-induced cholestasis.

• ↓cholesterol content of bile and bile stones by suppressing cholesterol synthesis and secretion from the liver and inhibits intestinal absorption of cholesterol.

• Gallstone dissolution and reduction in gallstone formation.
• ↓progression of liver disease and improvement in liver function tests.

Absorption: 90% absorbed following oral administration.

Distribution: Only small quantities are found in the systemic circulation; sites of action include the liver, bile, and gut lumen.

Metabolism/Excretion: Undergoes extensive enterohepatic recycling; excreted in feces via bile.

Half-life: 100 hr.

Contraindicated in:

• Patients requiring cholecystectomy
• Calcified cholesterol stones, radiopaque stones, bile pigment stones, or stones >20 mm
• Complete biliary obstruction.

Use Cautiously in:

• Chronic liver disease
• Surgical enteroanastomoses or Crohn's disease (↑ risk of bezoar formation).

Derm: hair thinning, pruritus, rash.

EENT: rhinitis.

GI: abdominal/biliary pain, bezoar formation, constipation, diarrhea, flatulence, ↑ liver enzymes, jaundice, nausea, stomatitis, vomiting.

MS: arthralgia, myalgia.

Neuro: anxiety, depression, fatigue, headache, sleep disorder.

Resp: cough.

Drug-Drug:

• Cholestyramine, colestipol, and aluminum-containing antacids may ↓ absorption.
• Estrogens may ↓ its effectiveness.

• PO (Adults): Gallstone dissolution: Initial 8–10 mg/kg/day in 2–3 divided doses; maintenance: 250 mg/day at bedtime for 6 mo–1 yr; Gallstone prevention: 300 mg twice daily; Primary biliary cirrhosis: 13–15 mg/kg/day in 2–4 divided doses.
• PO (Children and Infants): TPN-induced cholestasis: 30 mg/kg/day in 2–3 divided doses.
• PO (Infants): Biliary atresia: 10–15 mg/kg/day.

(Generic available)

• Capsules: 200 mg; 300 mg; 400 mg;
• Tablets: 250 mg; 500 mg;

• Monitor abdominal pain prior to and periodically during therapy. If GI obstructive symptoms present, hold therapy until clinical evaluation complete.
• Monitor ultrasonograms at 6 mo intervals during the first yr of therapy.

• Monitor liver function tests (GGT, alkaline phosphatase, AST, ALT) and bilirubin levels every mo for 3 mo and every 6 mo thereafter. If increase to clinically significant levels, consider discontinuation of therapy.

• Administer with food. Tablets may be broken in half and swallowed with water. To minimize the bitter taste, advise patient to swallow the half-tablet quickly without chewing. Half-tablets should be stored separately for up to 28 days.

• Instruct patient to take ursodiol as directed.
• Advise patient to avoid aluminum-containing antacids during therapy; may impair absorption.

• Dissolution and reduction in formation of gallstones. May take several mo of therapy and complete dissolution may not occur. Stone recurrence may occur after dissolution.
• ↓progression of liver disease and improvement in liver function tests.

Actigall, Reltone, Urso 250, Urso Forte

Urso DS