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. As a hydrophilic secondary bile acid, it works by reducing the secretion of cholesterol from the liver and decreasing cholesterol absorption in the intestine, thereby desaturating bile and promoting the gradual dissolution of existing radiolucent stones. This oral therapy represents a non-surgical option for appropriately selected patients, requiring careful monitoring under specialist supervision to ensure efficacy and safety throughout the treatment course, which may extend over many months.

Features

• Active ingredient: Ursodiol 300 mg capsules
• Mechanism: Hydrophilic bile acid that reduces cholesterol saturation of bile
• Formulation: Oral capsule for systemic absorption
• FDA-approved for radiolucent, non-calcified gallbladder stones
• Requires functioning gallbladder for therapeutic effect
• Typically prescribed as long-term therapy (6-24 months)

Benefits

• Provides non-surgical alternative for gallstone dissolution in appropriate candidates
• Reduces cholesterol saturation of bile by up to 40-60%
• May prevent formation of new cholesterol stones during therapy
• Can alleviate biliary pain and complications associated with gallstones
• Avoids risks associated with cholecystectomy in high-risk surgical patients
• Well-tolerated profile with predominantly gastrointestinal side effects

Common use

Actigall is primarily indicated for the dissolution of radiolucent (non-calcified), cholesterol-rich gallstones in patients with a functioning gallbladder who are poor candidates for surgery. The medication is particularly valuable for elderly patients, those with significant comorbidities increasing surgical risk, or patients who refuse cholecystectomy. Treatment is typically reserved for stones smaller than 20 mm in diameter that are floating in bile, as these characteristics predict better dissolution rates. Beyond gallstone dissolution, Actigall is also used off-label for primary biliary cholangitis (PBC) to improve liver enzyme levels and slow disease progression, though different dosing regimens apply for this indication.

Dosage and direction

The standard dosage for gallstone dissolution is 8-10 mg/kg/day administered in two or three divided doses with food to enhance absorption and minimize gastrointestinal discomfort. Treatment should continue for at least 6 months, with many patients requiring 12-24 months of therapy for complete stone dissolution. Ultrasound monitoring is recommended at 6-month intervals to assess treatment response; therapy should be discontinued if partial stone dissolution isn’t evident after 12 months. For patients with rapid stone dissolution, treatment should continue for 3 months after confirmed dissolution and disappearance of stones on ultrasound. Capsules should be swallowed whole with water and not crushed or chewed.

Precautions

Liver function tests (ALT, AST, alkaline phosphatase) must be monitored every 3-6 months during therapy, as ursodiol may rarely cause hepatic dysfunction. Patients should be advised that calcification of stones may occur during treatment, rendering them insoluble and necessitating alternative management. Women of childbearing potential should use effective contraception, as safety during pregnancy hasn’t been definitively established despite ursodiol’s natural occurrence in bile. Diarrhea may occur initially but typically resolves with continued therapy; persistent diarrhea may require dosage adjustment. Patients should maintain a low-cholesterol diet during treatment to enhance therapeutic efficacy.

Contraindications

Actigall is contraindicated in patients with radio-opaque (calcified) gallstones that are unlikely to dissolve, those with non-functioning gallbladders, or individuals with chronic liver disease not associated with gallstones. The medication should not be used in patients with acute cholecystitis, cholangitis, biliary obstruction, or biliary-gastrointestinal fistula. Hypersensitivity to ursodiol or bile acids constitutes an absolute contraindication. Patients with frequent biliary colic requiring analgesics are generally poor candidates for dissolution therapy. Those with pigment stones or stones larger than 20 mm should not receive Actigall due to low dissolution probability.

Possible side effect

The most common adverse reactions are gastrointestinal, including diarrhea (occurring in approximately 10-20% of patients), nausea, vomiting, dyspepsia, and abdominal discomfort. These symptoms are typically mild and often resolve with continued therapy. Less frequently, patients may experience constipation, headache, dizziness, or hair thinning. Elevated liver enzymes (transaminases) occur in approximately 2-5% of patients and usually normalize with dosage reduction or discontinuation. Rare but serious side effects include acute pancreatitis, calcification of stones during treatment, and worsening of pre-existing liver disease. Allergic reactions including rash and urticaria have been reported in less than 1% of patients.

Drug interaction

Actigall may interact with several medications including aluminum-based antacids and bile acid sequestrants (cholestyramine, colestipol), which can reduce ursodiol absorption—administration should be separated by at least 2 hours. Estrogens, oral contraceptives, and clofibrate may counteract Actigall’s efficacy by increasing biliary cholesterol secretion. Concurrent use with cyclosporine may reduce cyclosporine absorption, potentially requiring dosage adjustment. Ursodiol may enhance the absorption of other lipophilic drugs. Proton pump inhibitors and H2 antagonists might theoretically reduce efficacy by altering biliary pH, though clinical significance remains uncertain.

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. Consistency in dosing is important for maintaining adequate bile acid concentrations, but occasional missed doses are unlikely to significantly impact overall treatment efficacy given the long-term nature of therapy. Patients should inform their physician if multiple doses are missed consecutively.

Overdose

No specific antidote exists for ursodiol overdose. Reported cases of overdose have been rare, with doses up to 20 times the recommended amount causing only diarrhea as the primary symptom. Management should be supportive and symptomatic, with attention to maintaining hydration and electrolyte balance if significant diarrhea occurs. Hemodialysis is not expected to be effective due to ursodiol’s high protein binding and extensive enterohepatic recirculation. Patients experiencing suspected overdose should seek medical attention for appropriate monitoring and supportive care.

Storage

Actigall capsules should be stored at controlled room temperature (20-25°C or 68-77°F) in their original container, protected from light and moisture. The medication should not be frozen. Keep out of reach of children and pets. Do not use capsules beyond the expiration date printed on the packaging. Once opened, the bottle should be tightly closed between uses to protect the capsules from humidity. Do not transfer capsules to other containers, as this may expose them to moisture and light that could degrade the medication.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional who can assess individual patient circumstances. The efficacy of Actigall varies among patients and is dependent upon appropriate patient selection based on stone characteristics and gallbladder function. Not all patients will experience complete stone dissolution, and some may require alternative therapies. The manufacturer’s prescribing information should be consulted for complete details regarding use, warnings, and precautions.

Reviews

Clinical studies demonstrate that approximately 30-40% of carefully selected patients achieve complete gallstone dissolution with Actigall therapy over 6-24 months. Success rates are highest in patients with small (<5 mm), floating, radiolucent stones and functioning gallbladders. In trials, stone recurrence rates after successful dissolution range from 30-50% within 5 years, though maintenance therapy may reduce this risk. Gastroenterologists generally regard Actigall as a valuable option for the minority of gallstone patients who meet strict selection criteria and cannot undergo surgery. Patient satisfaction is mixed, with some appreciating the non-surgical approach while others express frustration with the lengthy treatment duration and variable outcomes.