Ursodiol
Ursodiol (Actigall)
Ursodiol
(ur-so- DYE-ohl)
Pregnancy Category: B Actigall Urso Ursofalk (Rx)

Classification: Gall stone solubilizer

Action/Kinetics: Naturally occurring bile acid that inhibits the hepatic synthesis and secretion of cholesterol; it also inhibits intestinal absorption of cholesterol. Acts to solubilize cholesterol in micelles and to cause dispersion of cholesterol as liquid crystals in aqueous media. Undergoes a significant first-pass effect where it is conjugated with either glycine or taurine and then secreted into hepatic bile ducts.

Uses: Dissolution of gallstones in clients with radiolucent, noncalcified gallstones ( <20 mm) in whom elective surgery would be risky (i.e., systemic disease, advanced age, idiosyncratic reactions to general anesthesia) or in those who refuse surgery. Prevent gallstones in obese clients undergoing rapid weight loss. Primary biliary cirrhosis (Urso).

Contraindications: Clients with calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones. Acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, biliary-gastrointestinal fistula, allergy to bile acids, chronic liver disease. Provide appropriate specifc treatment in those with variceal bleeding, hepatic encephalopathy, ascites, or in need of an urgent liver transplant.

Special Concerns: Use with caution during lactation. Safety and efficacy have not been determined in children. Safety for use beyond 24 months is not known.

Side Effects: GI: N&V;, dyspepsia, metallic taste, abdominal pain, biliary pain, cholecystitis, constipation, stomatitis, flatulence, diarrhea. Skin: Pruritus, rash, dry skin, urticaria. CNS: Headache, fatigue, anxiety, depression, sleep disorders. Other: Sweating, thinning of hair, back pain, arthralgia, myalgia, rhinitis, cough.

Overdose Management: Symptoms: Diarrhea. Treatment: Treat with supportive measures.

Drug Interactions: Antacids, aluminum-containing / Ursodiol effect R/T GI tract absorption Cholestyramine / Ursodiol effect R/T GI tract absorption Clofibrate / Ursodiol effect R/T hepatic cholesterol secretion Colestipol / Ursodiol effect R/T GI tract absorption Contraceptives, oral / Ursodiol effect R/T hepatic cholesterol secretion Estrogens / Ursodiol effect R/T hepatic cholesterol secretion

How Supplied: Capsule: 300 mg; Tablet: 250 mg

Dosage
?Capsules Gallstones.
Adults: 8-10 mg/kg/day in two or three divided doses, usually with meals.
Prevent gallstones in rapid weight loss in obesity.
Adults: 300 mg b.i.d. during period of weight loss.
?Tablets Primary biliary cirrhosis.
Adults: 13-15 mg/kg/day given in 4 divided doses with food.