Actigall (ursodiol)

What is ursodiol, and how does it work (mechanism of action)?

Ursodiol is a naturally-occurring bile acid that is made by the liver in humans and is secreted in small quantities into 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. The FDA approved ursodiol in December 1987.

What brand names are available for ursodiol?

Actigall, Urso Forte, Urso 250

Do I need a prescription for ursodiol?

Yes

What are the side effects of ursodiol?

The most common side effects are:

• rash,
• itching,
• nausea,
• vomiting,
• stomach pain,
• back pain,
• constipation,
• diarrhea, and
• hair loss.

Serious allergic reactions and reduced concentration of white blood cells also have occurred.

What is the dosage for ursodiol?

The recommended dose for dissolving gallstones in adults is 8-10 mg/kg/day split into two or three doses (every 8 or 12 hours). Each dose should not exceed 300 mg. The maintenance dose is 250 mg at bedtime for six months.
For treating primary biliary cirrhosis, the recommended dose is 13-15 mg/kg/day split into 2 to 4 doses. Ursodiol should be taken with meals.

Which drugs or supplements interact with ursodiol?

Aluminum containing antacids, cholestyramine (Questran, Questran Light) and colestipol (Colestid) reduce the absorption of ursodiol and therefore reduce its action. Estrogens, oral contraceptives, clofibrate, and potentially other cholesterol reducing drugs may counteract the effects of ursodiol by increasing cholesterol secretion by the liver and the risk for gallstone formation.

Is ursodiol safe to take if I'm pregnant or breastfeeding?

The are no adequate studies in pregnant women.
It is not known whether ursodiol is secreted in breast milk.

What else should I know about ursodiol?

What preparations of ursodiol are available?

Capsules: 300 mg. Tablets: 250 and 500 mg

How should I keep ursodiol stored?

Ursodiol should be stored at room temperature, 15 C - 30 C (59 F - 86 F).

Summary

Ursodiol (Actigall, Urso Forte, Urso 250) is a medication prescribed to dissolve cholesterol gallstones and treating primary biliary cirrhosis. Side effects, drug interactions, and dosage information should be reviewed prior to taking this medication.