Actigall (ursodiol) Side Effects, Warnings, and Drug Interactions

Actigall (ursodiol) is a naturally-occurring bile acid made by the liver in humans and is secreted in small quantities into bile and is used to dissolve and prevent cholesterol gallstones and to treat primary biliary cirrhosis, a disease of the liver.

Actigall 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, Actigall prevents the formation and promotes the dissolution of cholesterol-containing gallstones. The mechanism by which it acts in primary biliary cirrhosis is not clear. 

Common side effects of Actigall include:

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

Serious side effects of Actigall include serious allergic reactions and reduced concentration of white blood cells.

Drug interactions of Actigall include aluminum containing antacids, which reduce the absorption of Actigall and therefore reduce its action, such as:

• cholestyramine and
• colestipol.

The following drugs may counteract the effects of Actigall by increasing cholesterol secretion by the liver and the risk for gallstone formation:

• estrogens,
• oral contraceptives,
• clofibrate, and
• potentially other cholesterol-reducing drugs. 

There are no adequate studies of Actigall in pregnant women. It is unknown if Actigall is secreted in breast milk. Consult your doctor before breastfeeding.

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.

The nature and frequency of adverse experiences were similar across all groups.

The following tables provide comprehensive listings of the adverse experiences reported that occurred with a 5% incidence level:

GALLSTONE DISSOLUTION

Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Actigall by reducing its absorption. Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with Actigall in the same manner as the bile acid sequestering agents. Estrogens, oral contraceptives, and clofibrate (and perhaps other lipid-lowering drugs) increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of Actigall.