ACTIGALL- ursodiol capsule
Actavis Pharma, Inc.
DESCRIPTION
Actigall is a bile acid available as 300 mg capsules suitable for oral administration.
Actigall is ursodiol, USP (ursodeoxycholic acid), a naturally occurring bile acid found in small quantities in normal human bile and in the biles of certain other mammals. It is a 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?,7?-Dihydroxy-5?-cholan-24-oic acid (C24 H40 O4 ). Ursodiol, USP has a molecular weight of 392.57
nactive Ingredients: Colloidal silicon dioxide, magnesium stearate, and starch (corn). Gelatin capsules contain ferric oxide, gelatin, and titanium dioxide. The capsules are printed with edible ink containing black iron oxide.
CLINICAL PHARMACOLOGY
About 90% of a therapeutic dose of Actigall is absorbed in the small bowel after oral administration. After absorption, ursodiol enters the portal vein and undergoes efficient extraction from portal blood by the liver (i.e., there is a large "first-pass" effect) where it is conjugated with either glycine or taurine and is then secreted into the hepatic bile ducts. Ursodiol in bile is concentrated in the gallbladder and expelled into the duodenum in gallbladder bile via the cystic and common ducts by gallbladder contractions provoked by physiologic responses to eating. Only small quantities of ursodiol appear in the systemic circulation and very small amounts are excreted into urine. The sites of the drug's therapeutic actions are in the liver, bile, and gut lumen.
Actigall 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.
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.
DOSAGE AND ADMINISTRATION
Gallstone Dissolution
The recommended dose for Actigall treatment of radiolucent gallbladder stones is 8 - 10 mg/kg/day given in 2 or 3 divided doses.
Ultrasound images of the gallbladder should be obtained at 6-month intervals for the first year of Actigall therapy to monitor gallstone response. If gallstones appear to have dissolved, Actigall therapy should be continued and dissolution confirmed on a repeat ultrasound examination within 1 to 3 months. Most patients who eventually achieve complete stone dissolution will show partial or complete dissolution at the first on-treatment reevaluation. If partial stone dissolution is not seen by 12 months of Actigall therapy, the likelihood of success is greatly reduced.
Gallstone Prevention
The recommended dosage of Actigall for gallstone prevention in patients undergoing rapid weight loss is 600 mg/day (300 mg b.i.d.).
HOW SUPPLIED
Actigall Capsules are opaque white and pink capsules imprinted "ACTIGALL" on one half and "300 mg" on the other half of the capsule in black.
Bottles of 100 are supplied with child-resistant closures.
(NDC 52544-930-01)
Store at 20-25�C (68-77�F). [See USP controlled room temperature.]
Dispense in a tight container (USP).
Keep out of reach of children.
Rx only