What is ursodiol?

From the Guidelines

Ursodiol is a bile acid medication used to treat certain liver and gallbladder conditions, primarily by dissolving gallstones and improving liver function. The typical adult dose is 300-600 mg daily, taken orally in divided doses with meals, as recommended by studies such as 1. Treatment duration varies depending on the condition but can range from several months to long-term use.

Key Points

• Ursodiol works by reducing cholesterol production in the liver and decreasing cholesterol absorption in the intestines, which helps prevent gallstone formation and can gradually dissolve existing gallstones, as explained in 1.
• It also has a protective effect on liver cells, making it useful in treating various liver diseases, as noted in 1.
• Common brand names include Ursodiol, Actigall, and Urso Forte.
• Side effects are generally mild but may include diarrhea, constipation, or stomach upset, as reported in 1.
• Patients should be aware that ursodiol may take several months to effectively dissolve gallstones, and it works best for smaller stones, as stated in 1.
• It's not suitable for everyone, particularly those with certain types of liver disease or gallbladder complications, so a thorough medical evaluation is necessary before starting treatment, as emphasized in 1.

Important Considerations

• The most recent and highest quality study, 1, recommends that UDCA is not used for the routine treatment of newly diagnosed PSC, due to lack of evidence of benefit and potential harm in high doses.
• For patients already established on UDCA therapy, there may be evidence of harm in patients taking high dose UDCA 28–30 mg/kg/day, as warned in 1.

From the FDA Drug Label

Ursodiol (ursodeoxycholic acid), is a naturally occurring bile acid found in small quantities in normal human bile and in the biles of certain other mammals The chemical name for ursodiol is 3α,7β-Dihydroxy-5β-cholan-24-oic acid (C24H40O4). Ursodiol is a bile acid available as 300 mg capsules suitable for oral administration. It is a naturally occurring substance found in small quantities in normal human bile. 2

From the Research

Definition and Mechanism of Ursodiol

• Ursodiol, also known as ursodeoxycholic acid, is a naturally occurring bile acid that constitutes about 1-2% of the bile acids in human bile 3.
• It is used to treat predominantly cholestatic liver disorders and has cytoprotective, anti-apoptotic, immunomodulatory, and choleretic effects 4, 5.
• Ursodiol works by displacing potentially hepatotoxic bile salts, interrupting the cycle of cholestatic injury, and exerting hepatoprotective membrane-stabilizing or immunomodulatory effects (or both) 6.

Therapeutic Applications of Ursodiol

• Ursodiol is effective in dissolving cholesterol gallstones, with a dissolution rate of 37% for patients treated with ursodiol at doses of more than 7 mg/kg per day or of more than 500 mg/d for at least 6 months 6.
• It is also used to treat chronic liver diseases, including primary biliary cirrhosis, primary sclerosing cholangitis, intrahepatic cholestasis of pregnancy, and cystic fibrosis 4, 5.
• Ursodiol has been shown to improve biochemical markers of cholestasis and inflammation, and may also exert anti-apoptotic and immunomodulatory effects 6, 4, 5.

Dosage and Efficacy of Ursodiol

• The dosage of ursodiol used to treat chronic liver disease is typically in the range of 10-15 mg/kg/day, which is higher than the dosage used for gallstone dissolution therapy 7.
• Studies have shown that ursodiol is effective at doses as low as 250 mg/day, with further improvements in serum enzyme levels seen at higher doses 7.
• The efficacy of ursodiol in preventing gallstone recurrence and improving survival in patients with chronic liver disease is still being studied 6, 3, 4, 5.