Ursodiol (4 brand names, 2 dosage forms, 1 route)
Available dosage forms: CAPSULE, TABLET.
Routes of administration: ORAL.
Brand Names
- ACTIGALL
- URSO 250
- URSO FORTE
- URSODIOL
Indications and Usage
Ursodiol tablets are indicated for the treatment of patients with primary biliary cholangitis (PBC).
Contraindications
Patients with complete biliary obstruction and known hypersensitivity or intolerance to ursodiol or any of the components of the formulation.
Mechanism of Action
Ursodiol, 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 apoptosis of hepatocytes, immunomodulatory effects, and stimulation of bile secretion by hepatocytes and cholangiocytes.
Overdosage
There have been no reports of accidental or intentional overdosage with ursodiol. Single oral doses of ursodiol at 10 g/kg in mice and dogs, and 5 g/kg in rats 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.