Brand name: Ursophar®
Composition: Ursodeoxycholic Acid
Dosage form: Oral Capsule
Strength: 300 mg
Category: Gallstone solubilizing
For 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 caused by systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for those patients who refuse surgery. Safety for use of ursodiol beyond 24 months is not established. For the prevention of gallstone formation in obese patients experiencing rapid weight loss.
Administration and Dosage:
Gallstone dissolution- The recommended dose for ursodiol capsule treatment of radiolucent gallbladder stones is 8 to 10 mg/kg/day given in 2 or 3 divided doses. Obtain ultrasound images of the gallbladder at 6-month intervals for the first year of ursodiol therapy to monitor gallstone response. If gallstones appear to have dissolved, continue ursodiol therapy and confirm dissolution 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 ursodiol therapy, the likelihood of success is greatly reduced.
Gallstone prevention- The recommended dosage of ursodiol capsules for gallstone prevention in patients undergoing rapid weight Joss is 600 mg/ day (300 mg twice daily).
Hypersensitivity or intolerance to ursodiol or any of the components of the formulations.
Ursodiol will not dissolve calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones. Hence, patients with such stones are not candidates for ursodiol therapy.
Patients with compelling reasons for cholecystectomy including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-GI fistula are not candidates for ursodiol therapy. Allergy to bile acids.
Hepatic effects: Ursodiol therapy has not been associated with liver damage. Lithocholic acid, a naturally occurring bile acid, is known to be a liver-toxic metabolite. This bile acid is formed in the gut from ursodiol less efficiently and in smaller amounts than that seen from chenodiol. Lithocholic acid is detoxified in the liver by sulfation and, although man appears to be an efficient sulfater, it is possible that some patients may have a congenital or acquired deficiency in sulfation, thereby predisposing them to Lithocholate-induced liver damage.
Pregnancy: Category B. There have been no adequate and well controlled studies of the use of ursodiol in pregnant women, but inadvertent exposure of 4 women to therapeutic doses of the drug in the first trimester of pregnancy during the ursodiol trials led to no evidence of effects on the fetus or newborn baby. Although it seems unlikely, the possibility that ursodiol can cause fetal harm cannot be ruled out; hence, the drug is not recommended for use during pregnancy.
Lactation: It is not known whether ursodiol is excreted in human milk. Because many drugs are excreted in human milk, exercise caution when ursodiol is administered to a breastfeeding mother.
Children: The safety and effectiveness of ursodiol in pediatric patients have not been established.
Elderly: Small differences in efficacy and greater sensitivity of some elderly individuals taking ursodiol cannot be ruled out. Therefore, it is recommended that dosing proceed with caution in this population.
Monitoring: Abnormalities in liver enzymes have not been associated with ursodiol therapy and, in fact, ursodiol has been shown to decrease liver enzyme levels in liver disease. However, patients given ursodiol should have AST and ALT measured at the initiation of therapy and thereafter as indicated by the particular clinical circumstances. Patients with variceal bleeding, hepatic encephalopathy, ascites, or in need of an urgent liver transplant should receive appropriate specific treatment.
Antacids: Aluminum-based antacids adsorb bile acids in vitro and interfere with the action of ursodiol by reducing its absorption.
Bile acid sequestrants: Cholestyramine and colestipol may interfere with the action of ursodiol by reducing its absorption.
Clofibrate Estrogens Oral Contraceptives: These agents (and perhaps other lipid-lowering drugs) increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of ursodiol.
CNS: Fatigue; Headache; Insomnia
GI: Abdominal pain; Cholecystitis; Constipation; Diarrhea; Dyspepsia; Flatulence; GI disorder; Nausea; Vomiting
GU: Urinary tract infection
Musculoskeletal: Arthralgia; Arthritis; Back pain; Myalgia
Respiratory: Bronchitis; Coughing; Pharyngitis; Rhinitis; Sinusitis; Upper respiratory; tract infection
Miscellaneous: Allergy; Chest pain; Infection, viral
Symptoms: Neither accidental nor intentional overdosage with ursodiol has been reported. Doses of ursodiol in the range of 16 to 20 mg/kg/day have been tolerated by 7 patients for 6 to 37 months without symptoms. The LD50 for ursodiol in rats is over 5,000 mg/kg given over 7 to 10 days and over 7,500 mg/kg for mice. Single oral doses of ursodiol at 10, 5, and 10 g/kg in mice, rats, and dogs, respectively, were not lethal. A single oral dose of ursodiol at 1.5 g/kg was lethal in hamsters. Symptoms of acute toxicity were salivation and vomiting in dogs, and ataxia, dyspnea, ptosis, agonal convulsions, and coma in hamsters.
Treatment: The most likely manifestation of severe overdose with ursodiol would likely be diarrhea, which should be treated symptomatically.
Store at 25°C (77 °F); excursions permitted to 15°C to 30°C (59°to 86°F). Dispense in a tight container.
Package: Box of 30 capsules
Manufacturer: Koushanpharmed Co., Iran