Ursodiol

A natural bile acid that is used to treat liver disease, particularly primary biliary cirrhosis.

Information about Ursodiol

Ursodeoxycholic acid or ursodiol is a naturally occurring bile acid that is used dissolve cholesterol gall stones and to treat cholestatic forms of liver diseases including primary biliary cirrhosis.

Liver safety of Ursodiol

Ursodiol has been linked to rare instances of transient and mild serum aminotransferase elevations during therapy and to rare instances of jaundice and worsening of liver disease in patients with preexisting cirrhosis.

Mechanism of action of Ursodiol

Ursodiol (ur" soe dye' ol) is a naturally occurring bile acid that is a minor fraction of the bile acid pool in humans, but a major fraction in bears and other hibernating animals. Ursodeoxycholic acid is more water soluble (hydrophilic) than cholic or chenodeoxycholic acid and is less inherently toxic to cells. When given orally, ursodeoxycholic acid becomes a major component of the bile acid pool, the proportion rising from <2% to as much as 65%. By replacing the hydrophobic or more toxic bile acids with ursodiol, the toxic effects of cholestasis are ameliorated. Unlike other primary bile acids, ursodiol has little agonist activity with FXR, the bile acid sensing nuclear receptor. As a consequence, ursodiol has little effect on cholesterol and lipid synthesis and is effective in reducing the cholesterol saturation of bile and in dissolving cholesterol gallstones. In addition, ursodiol has been shown to decrease serum enzyme elevations in a large number of cholestatic liver diseases including primary biliary cirrhosis, the cholestasis of pregnancy, and parenteral nutrition associated liver disease. In some situations, this improvement in liver enzyme levels has been accompanied by improvements in symptoms, liver histology and long term adverse outcomes of these diseases (cirrhosis, end stage liver disease).

FDA approval information for Ursodiol

Ursodiol was approved for dissolution of gallstones in 1987 and as a therapy of primary biliary cirrhosis in 1996. It is also used off label in other cholestatic liver conditions including sclerosing cholangitis, graft-vs-host disease, cholestasis of pregnancy and the liver disease of cystic fibrosis.

FDA approval information for Ursodiol

Ursodiol is available in tablets and capsules of 250 and 300 mg generically and under brand names such as Actigall and Urso. The typical initial dose for dissolution of gall stones is 8 to 10 mg/kg daily and for primary biliary cirrhosis is 13 to 15 mg daily in three divided doses with meals.

Side effects of Ursodiol

Ursodiol is generally well tolerated; uncommon side effects can include fatigue, nausea, headache and weight gain. Less common, but potentially severe adverse reactions include hypersensitivity reactions and depression.

• Chenodiol (Chenodeoxycholic Acid)
• Cholic Acid
• Obeticholic Acid
• Ursodiol (Ursodeoxycholic Acid)

• Dailymed label info on Ursodiol
• FDA Ursodiol

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