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 radiolucent, non-calcified stones. This oral therapy represents a non-surgical alternative for appropriately selected patients, requiring careful patient selection, consistent dosing, and long-term monitoring under specialist supervision to achieve optimal therapeutic outcomes.

Features

• Active ingredient: Ursodiol (ursodeoxycholic acid) 300 mg capsules
• Mechanism: Hydrophilic bile acid that reduces cholesterol saturation of bile
• Formulation: Oral capsule for systemic absorption
• FDA-approved for gallstone dissolution in selected patients
• Requires radiolucent, functioning gallbladder confirmation
• Typically prescribed as long-term therapy (months to years)

Benefits

• Provides a non-surgical alternative for cholesterol gallstone dissolution
• Reduces cholesterol saturation of bile by up to 40-60%
• May prevent formation of new cholesterol stones during therapy
• Decreases hepatic secretion of cholesterol and intestinal cholesterol absorption
• Can improve biliary lipid composition and flow
• Offers viable option for high-risk surgical candidates

Common use

Actigall is primarily indicated for the dissolution of radiolucent cholesterol gallstones in patients with a functioning gallbladder who are not candidates for cholecystectomy due to increased surgical risk, patient preference, or other medical contraindications. The medication is specifically effective for stones that are non-calcified and visible on ultrasound but radiolucent on plain abdominal radiography. Treatment success is highest in patients with small stones (typically <15-20 mm in diameter) and those with patent cystic ducts. Beyond gallstone dissolution, Actigall is also used off-label for the treatment of primary biliary cholangitis (PBC) to improve liver enzyme levels and delay disease progression, as well as for cholesterol hepatolithiasis and certain cholestatic liver conditions.

Dosage and direction

The recommended dosage for gallstone dissolution is 8-10 mg/kg/day administered in two or three divided doses with food to enhance absorption and tolerance. Treatment typically begins with 300 mg twice daily, with adjustments based on patient weight and treatment response. For a 70 kg patient, this translates to approximately 600-700 mg daily. Administration should occur with meals to maximize bioavailability and minimize gastrointestinal discomfort. Therapy must be continuous, and patients should be advised that dissolution typically requires 6-24 months of treatment, with regular monitoring via ultrasound every 6 months to assess stone dissolution. Treatment should be discontinued if partial stone dissolution isn’t observed within 12 months or if calcification of stones occurs during therapy.

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 cautioned that complete dissolution occurs in approximately 30-40% of patients after 6-24 months of therapy, with stone recurrence rates of up to 50% within 5 years after discontinuation. Women of childbearing potential should use effective contraception, as safety during pregnancy, while generally favorable, requires careful risk-benefit assessment. Diarrhea or loose stools may occur initially but typically resolve with continued therapy. Patients should maintain a low-cholesterol diet during treatment to enhance therapeutic efficacy. Regular radiographic monitoring is essential to detect possible stone calcification, which would necessitate discontinuation of therapy.

Contraindications

Actigall is contraindicated in patients with radio-opaque (calcified) gallstones that are visible on plain abdominal radiography, as these stones are refractory to dissolution therapy. Additional contraindications include non-functioning gallbladder (confirmed by cholecystography), acute cholecystitis, cholangitis, biliary obstruction, biliary-gastrointestinal fistula, or hypersensitivity to bile acids or any component of the formulation. The medication is not recommended for patients with chronic liver disease severe enough to impair synthetic function (Child-Pugh class B or C), or those with inflammatory bowel diseases affecting bile acid metabolism. Patients with frequent biliary colic requiring analgesics are generally poor candidates for medical dissolution therapy.

Possible side effects

The most commonly reported adverse effects include diarrhea or loose stools (occurring in approximately 10-20% of patients), which are typically mild and often resolve with continued treatment. Less frequent side effects may include nausea, vomiting, dyspepsia, abdominal discomfort, constipation, and headache. Rare but potentially serious adverse reactions include urticaria, pruritus, rash, and hepatic enzyme elevations. Very rare cases of severe hepatotoxicity have been reported, necessitating immediate discontinuation and thorough hepatic evaluation. Patients may experience paradoxical worsening of biliary symptoms during initial therapy due to stone fragmentation and passage. Any signs of allergic reaction or worsening right upper quadrant pain should prompt immediate medical evaluation.

Drug interaction

Actigall may interact with several medication classes. 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 antagonize the cholesterol-desaturating effect of ursodiol by increasing biliary cholesterol secretion. Cyclosporine blood levels may be reduced through possible interference with absorption, requiring monitoring. Ursodiol may reduce the absorption of ciprofloxacin and other fluoroquinolones. The medication may alter the metabolism of drugs that undergo enterohepatic recirculation. Clinicians should review all concomitant medications, including over-the-counter products and herbal supplements, before initiating therapy.

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 necessary for effective cholesterol desaturation. If multiple doses are missed, patients should contact their healthcare provider for guidance on resuming therapy. Documentation of missed doses should be maintained, as inconsistent dosing may prolong the treatment duration required for stone dissolution.

Overdose

There are no well-documented cases of serious adverse events from ursodiol overdose. Based on its mechanism and pharmacokinetics, significant overdose would likely manifest as severe diarrhea, possibly leading to dehydration and electrolyte imbalances. Management should be supportive, including maintenance of hydration and electrolyte balance. Since ursodiol undergoes extensive enterohepatic circulation, activated charcoal may be considered if administered shortly after ingestion. Patients should be monitored for signs of dehydration and evaluated for electrolyte abnormalities. There is no specific antidote for ursodiol overdose. Symptomatic treatment and standard supportive care should be provided based on clinical presentation.

Storage

Actigall capsules should be stored at controlled room temperature between 20°C and 25°C (68°F and 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). The medication must be kept in its original container with the lid tightly closed to protect from moisture and light. Capsules should not be stored in bathroom cabinets or other areas subject to high humidity. Keep out of reach of children and pets. Do not use capsules that appear discolored, damaged, or beyond their expiration date. Proper storage ensures stability of the medication throughout the treatment period, which may extend for several years in some patients.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Actigall is a prescription medication that should be used only under the supervision of a qualified healthcare provider familiar with the patient’s complete medical history. Treatment decisions should be based on individual patient factors, including stone characteristics, gallbladder function, and overall health status. Patients should not initiate, adjust, or discontinue therapy without consulting their physician. The complete prescribing information should be reviewed before initiating treatment, including boxed warnings and latest safety information from the manufacturer.

Reviews

Clinical studies demonstrate that Actigall achieves complete gallstone dissolution in approximately 30-40% of carefully selected patients after 6-24 months of therapy. Success rates are highest in patients with small (<5 mm), floating cholesterol stones and functioning gallbladders. Gastroenterologists note that patient selection is critical—ideal candidates have radiolucent stones, patent cystic ducts, and willingness to commit to long-term therapy with regular monitoring. Many experts emphasize that while dissolution therapy avoids surgical risks, it requires patience and adherence, with stone recurrence remaining a significant consideration. Patients who successfully complete therapy often report satisfaction with avoiding surgery, though some express frustration with the lengthy treatment duration and need for ongoing monitoring.