Trade Names:Actigall- Capsules 300 mg
Trade Names:URSO 250- Tablets 250 mg
Trade Names:URSO Forte- Tablets 500 mgPMS-Ursodiol C (Canada)URSO DS (Canada)
Suppresses hepatic synthesis and cholesterol secretion and inhibits intestinal absorption of cholesterol.
About 90% absorbed in the small bowel.
Extracted from portal blood in the liver where it is conjugated with glycine or taurine and then secreted into the hepatic bile ducts. These conjugates are absorbed in the small intestine. The conjugates is deconjugated in the ileum, leading to formation of free ursodiol that can be reabsorbed and reconjugated in the liver. Some ursodiol is epimerized to chenodiol, which may undergo 7-hydroxylation to lithocholic acid.
Various metabolites (including chenodiol, lithocholic acid, and sulfated lithocholic acid conjugates) are excreted in the feces.
Dissolution of gallstones in patients with radiolucent, noncalcified, gallbladder stones less than 20 mm in greatest diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk due to systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for patients refusing surgery (capsules only); prevention of gallstone formation in obese patients experiencing rapid weight loss (capsules only); treatment of patients with primary biliary cirrhosis (tablets only).
Cholestasis-associated pruritus; primary sclerosing cholangitis.
Hypersensitivity to any component of product.Capsule only
Presence of calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones; patients with compelling reasons for cholecystectomy, including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-GI fistula; allergy to bile acids.
PO 8 to 10 mg/kg/day in 2 or 3 divided doses.Gallstone PreventionAdults
PO 300 mg twice daily.Primary Biliary CirrhosisAdults
PO 13 to 15 mg/kg/day in 2 to 4 divided doses with food.
Store tablets at controlled room temperature (68° to 77°F). Store capsules at controlled room temperature (59° to 86°F).
May decrease ursodiol absorption.Clofibrate, estrogens, oral contraceptives
May decrease the efficacy of ursodiol by increasing hepatic cholesterol secretion and encouraging cholesterol gallstone formation.
None well documented.
The following adverse reactions occurred at an incidence rate of 5% or more.
Asthenia; dizziness; fatigue; headache; insomnia.
Abdominal pain; cholecystitis; constipation; diarrhea; dyspepsia; flatulence; GI disorder; nausea; vomiting.
Arthralgia; arthritis; back pain; musculoskeletal pain; myalgia.
Bronchitis; coughing; sinusitis; upper respiratory tract infection.
Allergy; chest pain; influenza-like symptoms; peripheral edema; viral infection.
Category B .
Safety and efficacy not established.
Studies suggest bile acids might be involved in pathogenesis of human colon cancer in patients undergoing a cholecystectomy; however, direct evidence is lacking.
Gallbladder nonvisualization developing during treatment predicts failure of complete stone dissolution and treatment should be discontinued.
May recur within 2 yr in 30% of patients and within 5 yr in 50% of patients.
The lithocholic acid metabolite of ursodiol is hepatotoxic; therefore, monitor AST and ALT.
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