Clinical Information
Gen. Code and Des.
3095 ursodiol ORAL CAPSULE 300 MG
GCN and Des.
1070 ursodiol ORAL CAPSULE 300 MG
Strength
300MG
Dose Form
CAPSULE
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
56140000 CHOLELITHOLYTIC AGENTS
Active Ingredients
1212 ursodiol 128132
Inactive Ingredients
2549 gelatin 9000708
Actigall Capsules (ursodiol USP) Capsules Rx Only Prescribing info. SPECIAL NOTE Gallbladder stone dissolution with Actigall treatment requires months of therapy Complete dissolution does not occur in all patients and recurrence of stones within years has been observed in up to 50% of patients who do dissolve their stones on bile acid therapy Patients should be carefully selected for therapy with ursodiol, and alternative therapies should be considered DESCRIPTION Actigall is bile acid available as 300-mg capsules suitable for oral administration Actigall is ursodiol USP (ursodeoxycholic acid), naturally occurring bile acid found in small quantities in normal human bile and in larger quantities in the biles of certain species of bears It is bitter-tasting, white powder freely soluble in ethanol, methanol, and glacial acetic acid sparingly soluble in chloroform slightly soluble in ether and insoluble in water The chemical name for ursodiol is 3(alpha),7(beta)-dihydroxy-5(beta)-cholan-24-oic acid (C Za 40 4) INDICATIONS AND USAGE . Actigall is indicated for patients with radiolucent, noncalcified gallbladder stones 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 those patients who refuse surgery Safety of use of Actigall beyond 24 months is not established 2 Actigall is indicated for the prevention of gallstone formation in obese patients experiencing rapid weight loss CONTRAINDICATIONS Actigall will not dissolve calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones Hence, patients with such stones are not candidates for Actigall therapy Patients with compelling reasons for cholecystectomy including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-gastrointestinal fistula are not candidates for Actigall therapy Allergy to bile acids Drug Interactions Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Actigall by reducing its absorption Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with Actigall in the same manner as the bile acid sequestering agents Estrogens, oral contraceptives, and clofibrate (and perhaps other lipid- lowering drugs) increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of Actigall Carcinogenesis, Mutagenesis, Impairment of Fertility Ursodeoxycholic acid was tested in 2-year oral carcinogenicity studies in CD-1 mice and Sprague-Dawley rats at daily doses of 50, 250, and 1000 mg/kg/day It was not tumorigenic in mice In the rat study, it produced statistically significant dose-related increased incidences of pheochromocytomas of adrenal medulla in males (p=0 .014, Peto trend test) and females (p=0 .004, Peto trend test .) 78-week rat study employing intrarectal instillation of lithocholic acid and tauro-deoxycholic acid, metabolites of ursodiol and chenodiol, has been conducted These bile acids alone did not produce any tumors A tumor-promoting effect of both metabolites was observed when they were co-administered with carcinogenic agent Results of epidemiologic studies suggest that bile acids might be involved in the pathogenesis of human colon cancer in patients who had undergone cholecystectomy, but direct evidence is lacking Ursodiol is not mutagenic in the Ames test Dietary administration of lithocholic acid to chickens is reported to cause hepatic adenomatous hyperplasia Pregnancy Category B
