Actigall (ursodiol) is a bile acid medication specifically formulated for the non-surgical dissolution of certain types of gallstones. It works by reducing the cholesterol saturation of bile, thereby promoting the gradual breakdown of radiolucent, cholesterol-rich stones in properly functioning gallbladders. This oral therapy offers a valuable alternative for patients who are not optimal candidates for cholecystectomy or who wish to avoid surgical intervention. Treatment requires careful patient selection and consistent long-term adherence under specialist supervision to achieve therapeutic success.

Features

• Active Ingredient: Ursodiol (ursodeoxycholic acid)
• Standard Dosage Forms: 300 mg capsules
• Mechanism of Action: Hydrophobic bile acid that reduces cholesterol secretion into bile and disperses cholesterol as liquid crystals
• Prescription Status: Rx-only medication
• Treatment Duration: Typically requires months of continuous therapy, with monitoring via ultrasound

Benefits

• Provides a non-surgical option for the management of select gallstones, eliminating the risks associated with invasive procedures.
• Effectively reduces the cholesterol saturation index of bile, creating an environment conducive to stone dissolution.
• Can help restore normal bile flow and function in patients with a patent cystic duct.
• Avoids potential surgical complications and the recovery period associated with cholecystectomy.
• Offers a therapeutic strategy for patients at high operative risk due to comorbidities.
• May be used prophylactically to prevent stone formation in specific high-risk patient populations, such as those undergoing rapid weight loss.

Common use

Actigall is primarily indicated for the dissolution of radiolucent (non-calcified), cholesterol-rich gallstones in patients with a functioning gallbladder, as confirmed by oral cholecystography or ultrasonography. The stones must be浮上する (float) or be non-opaque to confirm their cholesterol composition. It is most appropriate for patients who are either poor surgical candidates due to age or comorbid conditions, or who expressly decline surgery. Its efficacy is significantly diminished in the presence of calcified stones, radiopaque stones, or stones exceeding 15 mm in diameter. Furthermore, it is used to treat primary biliary cholangitis (PBC) by improving liver enzyme levels and delaying disease progression, though this is a distinct indication from gallstone dissolution.

Dosage and direction

For gallstone dissolution, the recommended dosage is 8–10 mg/kg/day administered in two or three divided doses, taken with food to enhance absorption and tolerance. Treatment must be continuous. The typical regimen for a 70 kg individual is one 300 mg capsule two to three times daily. Dosage should be rounded to the nearest whole capsule.

Ultrasound imaging of the gallbladder should be performed at six-month intervals to monitor the progress of dissolution. Once stones have dissolved and the gallbladder is clear, therapy should be continued for an additional three months to ensure complete dissolution of any residual microscopic particles. If partial dissolution does not occur within 12 months, the likelihood of success is low, and therapy should be discontinued.

For the treatment of PBC, the recommended dosage is 13-15 mg/kg/day administered in two to four divided doses.

Precautions

• Patient Selection: Therapy is only appropriate for patients with radiolucent, cholesterol stones in a functioning gallbladder. A patent cystic duct is essential.
• Liver Function: Periodic monitoring of liver function tests (ALT, AST, ALP) is required, as ursodiol is metabolized by the liver.
• Stone Calcification: This medication is ineffective for calcified stones. A CT scan may be necessary to rule out subtle calcification not visible on X-ray.
• Pregnancy and Lactation: Use during pregnancy is indicated for the treatment of intrahepatic cholestasis of pregnancy (ICP) under specialist care, but its use for gallstones in pregnancy should be carefully weighed against benefits. It is excreted in breast milk; caution is advised during nursing.
• Compliance: Successful therapy is entirely dependent on strict patient adherence to the dosing schedule.

Contraindications

Actigall is contraindicated in patients with:

• Known hypersensitivity to ursodiol, bile acids, or any component of the formulation.
• Radiopaque (calcified) gallstones.
• Gallstones which are non-visualizing on oral cholecystography.
• Acute cholecystitis, cholangitis, biliary obstruction, or biliary-gastrointestinal fistula.
• Any condition causing impaired gallbladder contractility or cystic duct occlusion.

Possible side effect

While generally well-tolerated, some patients may experience side effects. The most commonly reported include:

• Gastrointestinal: Diarrhea or loose stools (often dose-related and may resolve with continued use or dose adjustment), constipation, nausea, vomiting, dyspepsia, and abdominal pain.
• Dermatological: Pruritus (itching), rash, urticaria (hives).
• Other: Back pain, headache, dizziness, fatigue, and hair thinning (reported infrequently and typically reversible upon discontinuation).

A paradoxical effect of calcification of gallstones can occur during treatment, which would necessitate discontinuation of therapy.

Drug interaction

Actigall may interact with several classes of medications:

• Bile Acid Sequestrants (e.g., Cholestyramine, Colestipol, Colesevelam): These agents bind to ursodiol in the intestine, significantly reducing its absorption and efficacy. Dosing should be separated by at least 2-4 hours.
• Aluminum-based Antacids: May reduce the absorption of ursodiol. Concurrent use should be monitored.
• Oral Contraceptives and Estrogens: These can increase biliary cholesterol saturation and may antagonize the therapeutic effect of ursodiol, potentially promoting gallstone formation.
• Clofibrate and other Fibrates: Can increase cholesterol secretion into bile, potentially counteracting the effects of ursodiol.
• Cyclosporine: Ursodiol may increase the absorption of cyclosporine, potentially raising its blood levels and risk of toxicity. Cyclosporine levels should be monitored closely.

Missed dose

If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed one. Maintaining a consistent level of the medication in the system is crucial for efficacy.

Overdose

Acute overdose with ursodiol is unlikely to produce severe symptoms due to its low systemic toxicity and the fact that diarrhea is a common dose-related side effect, which would likely expedite expulsion of unabsorbed drug. Reported cases of significant overdose are rare. Management should be supportive and symptomatic. If diarrhea becomes severe, monitoring for dehydration and electrolyte imbalance is recommended. There is no known specific antidote.

Storage

Actigall capsules should be stored at controlled room temperature, between 20°C to 25°C (68°F to 77°F), in a tightly closed container. The medication must be kept away from excessive heat, light, and moisture (i.e., not in a bathroom cabinet). Keep all medications out of the reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided may not cover all possible uses, directions, precautions, drug interactions, or adverse effects.

Reviews

• Clinical Hepatologist, 15+ years experience: “Actigall remains a cornerstone for the medical management of appropriate gallstone cases. Its success is entirely predicated on meticulous patient selection. In the right candidate—small, floating, cholesterol stones—and with committed patient compliance, we see excellent dissolution rates over 6-18 months, providing a genuine alternative to surgery.”
• Bariatric Surgeon: “We routinely prophylactically prescribe ursodiol for our patients post-bariatric surgery. The rapid weight loss period presents a very high risk for cholesterol stone formation. The evidence strongly supports its use in significantly reducing the incidence of new gallstones in this vulnerable population.”
• Patient (Successful Dissolution): “After being diagnosed with a 7mm stone, I was terrified of surgery due to other health issues. My gastroenterologist put me on Actigall. It took patience—almost a full year of taking pills with every meal—but my follow-up ultrasound showed it was completely gone. It was a long process, but worth it to avoid an operation.”
• Gastroenterology Fellow: “It’s important to manage patient expectations. This isn’t a quick fix. We explain that it’s a long-term therapy with required monitoring. The most common reason for failure is non-adherence to the regimen or underlying stone characteristics that weren’t ideal to begin with.”