Used in the treatment of dissolution of cholesterol-rich gallstones.
Mode of Action
USOLIV, a naturally occurring hydrophilic bile acid, derived from cholesterol, is present as a minor fraction of the total human bile acid pool. Oral administration of ursodiol increases this fraction in a dose related manner, to become the major biliary acid, replacing/displacing toxic concentrations of endogenous hydrophobic bile acids that tend to accumulate in cholestatic liver disease. In addition to the replacement and displacement of toxic bile acids, other mechanisms of action include cytoprotection of the injured bile duct epithelial cells (cholangiocytes) against toxic effects of bile acids, inhibition of apotosis of hepatocytes, immunomodulatory effects, and stimulation of bile secretion by hepatocytes and cholangiocytes.
The majority of ursodiol is absorbed by passive diffusion and its absorption is incomplete. At least 70% of ursodiol (unconjugated) is bound to plasma protein. Once absorbed, ursodiol undergoes hepatic extraction to the extent of about 50% in the absence of liver disease. In the liver, ursodiol is conjugated with glycine or taurine, and then secreted into bile. Ursodiol is excreted primarily in the feces.
Dosage and Recommendation
Dissolution of cholesterol gall stone: 6-12 mg/kg/day as a single dose at bedtime or 2-3 divided doses for 3-4 months after radiological disappearance of stones. Primary Billiary Cirrhosis: 10-15 mg/kg/day administered in two to four divided doses with food.
Packing and Presentation
USOLIV 150 (Ursodeoxycholic acid 150 mg): 10 x 10s USOLIV 300 (Ursodeoxycholic acid 300 mg): 10 x10s