How Do Gallstone Solubilizing Agents Work?

Gallstone solubilizing agents are a class of medications used to dissolve small noncalcified gallstones (made up of cholesterol) in adults who do not want to or cannot have gallbladder surgery, to prevent gallstones in overweight or obese patients undergoing rapid weight loss and to treat primary biliary cirrhosis (PBC-an autoimmune liver disease). These agents are naturally occurring bile acids. Bile acids are hydroxylated steroids synthesized in the liver from cholesterol and secreted in small quantities into bile (a digestive fluid produced by the liver and stored in the gallbladder).

Gallstone solubilizing agents are administered orally in the form of capsules or tablets. They are usually taken two or three times a day with or without food to treat gallstones and two times a day to prevent gallstones in people who are losing weight quickly. For PBC, they are usually taken two or four times a day with food. 

Gallstone solubilizing agents work in the following ways:

• These bile acid agents decrease the amount of cholesterol produced by the liver and its secretion in the bile by blocking an enzyme in the liver that is responsible for producing cholesterol (inhibition of hepatic cholesterol synthesis and secretion).
• They also decrease the amount of cholesterol absorbed by the intestines.
• They help in dissolving or breaking down the cholesterol in bile to prevent stone formation and promote the dissolution of cholesterol-containing gallstones.
• In addition, they decrease the toxic levels of bile acids that accumulate in the liver in patients suffering from PBC.

Gallstone solubilizing agents are used in conditions such as:

• Gallstone dissolution
• Gallstone prevention
• PBC (a chronic disease in which the bile ducts in the liver are slowly destroyed)
• Cystic fibrosis liver disease (mucus builds up and blocks bile ducts in the liver)
• Niemann-Pick disease (a rare, inherited disease that affects the body's ability to metabolize fat [cholesterol and lipids] within cells)
• Xanthomatosis (papules or nodules of the skin or mucous membranes that contain lipids)

Common side effects include:

• Headache
• Dizziness (feeling faint, weak, or unsteady)
• Diarrhea
• Dyspepsia (persistent or recurrent pain or discomfort in the upper abdomen)
• Nausea/vomiting
• Back pain
• Upper respiratory tract infection
• Hair loss
• Itching
• Mild abdominal pain
• Cough/runny or stuffy nose

Other rare side effects include:

• Rash
• Frequent urination or pain when you urinate
• Leukopenia (reduced number of white blood cells)
• Thrombocytopenia (low blood platelet count)
• Peripheral edema (swelling of lower legs or hands)
• Symptoms of liver damage
• Yellowing of eyes/skin
• Dark urine
• Unusual/extreme tiredness
• Severe abdominal pain
• Persistent nausea/vomiting

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Genetic and brand names of gallstone solubilizing agents include:

• Actigall
• Chenodal
• Chenodiol
• Urso Forte
• Ursodiol