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Highlights

Ursodiol
Ursodiol is a naturally-occurring bile acid that is made by the liver in humans and is secreted in small quantities in bile. It is used to dissolve and prevent cholesterol gallstones and to treat primary biliary cirrhosis, a disease of the liver. Ursodiol blocks the enzyme in the liver that produces cholesterol and thereby decreases production of cholesterol by the liver and the amount of cholesterol in bile. It also reduces the absorption of cholesterol from the intestine. By decreasing the concentration of cholesterol in bile, ursodiol prevents the formation and promotes the dissolution of cholesterol-containing gallstones. The mechanism by which it acts in primary biliary cirrhosis is not clear. Ursodiol is used to prevent cholesterol gallstones from forming during rapid loss of weight. It also is used to dissolve cholesterol gallstones that do not contain calcium and are less than 2 cm in diameter. It does not dissolve gallstones that are composed of pigment rather than cholesterol. Ursodiol must be used for one or more years, and 50% of patients who have successful dissolution of their gallstones will have the gallstones return within five years. The likelihood of having successful dissolution of gallstones is low if partial dissolution is not seen within 12 months of starting treatment. Ursodiol also is used to treat primary biliary cirrhosis.

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