Actigall (ursodiol) is a bile acid medication specifically formulated to dissolve certain types of cholesterol gallstones in patients for whom surgery poses an unacceptable risk. It works by reducing the secretion of cholesterol from the liver and decreasing the cholesterol saturation of bile, thereby promoting the gradual dissolution of existing radiolucent, non-calcified gallstones. This oral therapy represents a non-surgical option for a carefully selected patient population, offering a targeted approach to managing symptomatic gallbladder disease when cholecystectomy is contraindicated.

Features

• Active ingredient: Ursodiol (ursodeoxycholic acid) 300 mg capsules
• Mechanism: Hydrophilic bile acid that reduces cholesterol saturation index
• Formulation: Gelatin capsules for oral administration
• FDA-approved for gallstone dissolution therapy
• Requires specific patient selection criteria for optimal efficacy
• Typically prescribed as long-term therapy (months to years)

Benefits

• Provides a non-surgical alternative for gallstone management in appropriate candidates
• Reduces cholesterol saturation of bile, addressing the underlying pathophysiology
• May prevent formation of new cholesterol stones during treatment
• Can alleviate symptoms associated with gallstones when surgery is not feasible
• Well-tolerated profile with minimal systemic absorption
• May improve biliary lipid composition long-term

Common use

Actigall is primarily indicated for the dissolution of radiolucent, non-calcified gallstones less than 20 mm in diameter in patients with functioning gallbladders who are appropriate candidates for non-surgical therapy. It is particularly valuable for elderly patients, those with significant comorbidities that increase surgical risk, or patients who refuse cholecystectomy. The medication is also used off-label for primary biliary cholangitis (PBC) treatment and for preventing gallstone formation in patients undergoing rapid weight loss.

Dosage and direction

The recommended dosage for gallstone dissolution is 8-10 mg/kg/day administered in two or three divided doses with food. Treatment typically continues for several months until gallstones dissolve and for three months thereafter as confirmed by ultrasound. Patients should be instructed to take capsules with meals to enhance bioavailability and consistent absorption. Regular monitoring with ultrasound every 6 months is essential to assess treatment efficacy and determine when therapy may be discontinued.

Precautions

Liver function tests should be monitored periodically during treatment, as Actigall may cause hepatic impairment in some patients. Use with caution in patients with non-visualizing gallbladders, calcified gallstones, or chronic liver disease. Women of childbearing potential should use effective contraception during treatment, as safety in pregnancy hasn’t been established. Patients should be advised that stone recurrence may occur after successful dissolution therapy, particularly if underlying risk factors persist.

Contraindications

Actigall is contraindicated in patients with radio-opaque (calcified) gallstones, non-functioning gallbladders, or known hypersensitivity to ursodiol or any component of the formulation. It should not be used in patients with acute cholecystitis, cholangitis, biliary obstruction, or biliary-gastrointestinal fistula. The medication is also contraindicated in patients with chronic liver disease not associated with gallstone formation unless specifically indicated for PBC treatment under specialist supervision.

Possible side effects

Common side effects (occurring in >1% of patients) include diarrhea, constipation, nausea, vomiting, dyspepsia, and abdominal pain. Less frequently reported effects include headache, dizziness, fatigue, alopecia, pruritus, and rash. Hepatic reactions including elevated liver enzymes, hepatitis, and jaundice have been reported rarely. Most adverse effects are mild and transient, often resolving with continued therapy or dose adjustment.

Drug interactions

Actigall may reduce the absorption of cyclosporine, requiring dosage adjustment and therapeutic monitoring. Bile acid sequestrants (cholestyramine, colestipol) and aluminum-based antacids may decrease ursodiol absorption and should be administered at least 2 hours apart. Estrogens, oral contraceptives, and clofibrate may counteract the effectiveness of Actigall by increasing biliary cholesterol secretion. Close monitoring is recommended when co-administering with these medications.

Missed dose

If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent dosing is important for maintaining therapeutic bile acid concentrations and optimal gallstone dissolution efficacy.

Overdose

There are no reported cases of acute overdose with Actigall. Based on its mechanism of action and pharmacokinetics, diarrhea would be the most likely manifestation of excessive dosing. Treatment should be supportive and symptomatic. Given the medication’s extensive hepatic metabolism and biliary excretion, dialysis is unlikely to be effective. Patients experiencing suspected overdose should seek medical attention for appropriate monitoring and management.

Storage

Actigall capsules should be stored at controlled room temperature (20-25°C or 68-77°F) in their original container with the lid tightly closed. Protect from light, moisture, and excessive heat. Keep out of reach of children and pets. Do not use capsules that appear discolored, damaged, or beyond the expiration date printed on the packaging. Proper storage ensures medication stability and efficacy throughout the treatment period.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Actigall should be used only under the supervision of a qualified healthcare professional who can assess individual patient suitability and monitor treatment response. Patients should not initiate or discontinue therapy without consulting their physician. The prescribing information provided here may not include all possible uses, directions, precautions, or interactions.

Reviews

Clinical studies demonstrate that Actigall achieves complete gallstone dissolution in approximately 30-40% of carefully selected patients after 6-24 months of therapy. Gastroenterologists report that appropriate patient selection is critical for success, with best results seen in patients with small (<5 mm), floating, radiolucent stones in functioning gallbladders. Many experts note that while dissolution therapy requires patience and compliance, it provides a valuable option for high-risk surgical candidates. Long-term follow-up indicates stone recurrence rates of approximately 10% per year for the first several years after successful dissolution, emphasizing the need for ongoing monitoring and management of underlying risk factors.