Actigall

Actigall (ursodiol) is a bile acid medication specifically formulated to dissolve certain types of gallstones in patients for whom surgery poses an unacceptable risk. It works by reducing the cholesterol saturation of bile, thereby promoting the gradual dissolution of radiolucent, non-calcified cholesterol stones in a functioning gallbladder. This oral therapy represents a non-surgical alternative for a carefully selected patient population, offering a targeted approach to managing symptomatic gallstone disease under expert medical supervision. Treatment requires patience and consistent adherence, with dissolution typically occurring over months of therapy, accompanied by regular monitoring via ultrasound to assess efficacy and stone recurrence.

Features

• Active ingredient: Ursodiol (ursodeoxycholic acid)
• Available in 300 mg capsules
• Gallstone dissolution via cholesterol desaturation of bile
• Indicated for radiolucent, non-calcified gallbladder stones ≤20 mm in diameter
• Requires functional gallbladder as confirmed by oral cholecystography
• Oral administration with twice-daily dosing
• Pregnancy Category B medication
• Requires prescription and specialist supervision

Benefits

• Provides a non-surgical alternative for gallstone dissolution in appropriate candidates
• Reduces biliary cholesterol saturation and lithogenicity
• May prevent stone recurrence in susceptible patients when used as maintenance therapy
• Avoids risks associated with cholecystectomy in high-risk surgical patients
• Enables management of symptomatic gallstones without abdominal surgery
• Supported by clinical evidence demonstrating dissolution efficacy in select stone types

Common use

Actigall is primarily indicated for the dissolution of radiolucent, non-calcified gallstones in patients with a functioning gallbladder who are poor candidates for surgery. The typical patient population includes those with significant comorbidities that increase surgical risk, elderly patients, or those who refuse cholecystectomy. Treatment is most effective for stones smaller than 15 mm in diameter, with optimal results seen in stones ≤5 mm. The medication is not appropriate for calcified stones, radiopaque stones, or stones located in the bile ducts. Patients must have patent cystic and common bile ducts as confirmed by appropriate imaging studies before initiation of therapy.

Dosage and direction

The recommended dosage for gallstone dissolution is 8-10 mg/kg/day administered in two or three divided doses with food. For most adults, this translates to:

• 300 mg twice daily for patients weighing approximately 60-80 kg
• 300 mg three times daily for patients weighing over 80 kg

Treatment should be continued for several months until gallstone dissolution is confirmed by ultrasound, typically at 6-month intervals. If partial dissolution occurs within 6 months, therapy may be continued. The medication should be taken with food to enhance absorption and bile concentration. Patients should not crush or chew capsules. Therapy is generally discontinued if no reduction in stone size is observed after 12 months of treatment.

Precautions

Liver function tests (ALT, AST, alkaline phosphatase) should be monitored every month for the first three months of therapy and periodically thereafter. Ultrasound examinations should be performed at 6-month intervals to assess stone dissolution and detect any potential stone recurrence. Patients should be advised that complete dissolution may require 6-24 months of continuous therapy. Women of childbearing potential should use effective contraception during treatment. Diarrhea or loose stools may occur initially but often resolve with continued therapy. Patients should report any signs of acute cholecystitis, cholangitis, biliary obstruction, or pancreatitis promptly.

Contraindications

Actigall is contraindicated in patients with:

• Radiopaque or calcified gallstones
• Non-functioning gallbladder or cystic duct occlusion
• Acute cholecystitis, cholangitis, biliary obstruction, or pancreatitis
• Known hypersensitivity to bile acids or any component of the formulation
• Chronic liver disease with decompensated hepatic function
• Inflammatory bowel disease affecting the terminal ileum
• Patients requiring emergency surgery for biliary complications

Possible side effect

Common side effects (≥1%) include:

• Diarrhea or loose stools (dose-related, often transient)
• Nausea
• Dyspepsia
• Flatulence
• Constipation
• Headache
• Dizziness

Less common side effects (<1%) may include:

• Elevated liver enzymes (usually transient)
• Pruritus
• Rash
• Back pain
• Metallic taste
• Hair thinning (usually reversible)
• Vomiting

Rare but serious adverse reactions include:

• Acute pancreatitis
• Biliary pain or colic
• Calcification of gallstones during therapy
• Severe allergic reactions

Drug interaction

Significant drug interactions include:

• Cholestyramine, colestipol, colesevelam: These bile acid sequestrants may reduce absorption and efficacy of Actigall. Administer at least 2 hours apart.
• Aluminum-based antacids: May decrease ursodiol absorption. Separate administration by at least 2 hours.
• Estrogens, oral contraceptives, clofibrate: These may increase biliary cholesterol secretion and reduce efficacy.
• Cyclosporine: Ursodiol may increase cyclosporine absorption, requiring monitoring of cyclosporine levels.
• Dapsone: Ursodiol may decrease dapsone absorption.
• Nitrendipine: Ursodiol may increase nitrendipine absorption.

Missed dose

If a dose is missed, take it as soon as remembered unless it is almost time for the next scheduled dose. Do not double the dose to make up for a missed dose. Maintain regular dosing schedule to ensure consistent bile concentration. If multiple doses are missed, contact the prescribing physician for guidance on resuming therapy.

Overdose

No specific antidote exists for ursodiol overdose. Symptoms may include severe diarrhea, gastrointestinal discomfort, and potential electrolyte imbalances. Treatment should be supportive and symptomatic. Dialysis is not effective due to high protein binding. In case of suspected overdose, contact a poison control center or seek immediate medical attention. Provide supportive care including fluid and electrolyte replacement if significant diarrhea occurs.

Storage

Store at controlled room temperature (20-25°C or 68-77°F). Excursions permitted to 15-30°C (59-86°F). Keep container tightly closed. Protect from light and moisture. Do not freeze. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Do not transfer capsules to other containers unless specifically designed for medication storage.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Actigall is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual response to therapy may vary. The complete prescribing information should be consulted before initiating treatment. Not all patients with gallstones are candidates for dissolution therapy. Surgical intervention may be required if complications develop or if dissolution therapy is unsuccessful. Stone recurrence may occur after successful dissolution in up to 50% of patients within 5 years.

Reviews

Clinical studies demonstrate that Actigall achieves complete gallstone dissolution in approximately 30-40% of appropriately selected patients after 6-24 months of therapy. Success rates are highest for small (<5 mm), floating, radiolucent stones in functioning gallbladders. Many gastroenterologists report satisfactory outcomes in patients who are poor surgical candidates, though emphasize the importance of proper patient selection and ongoing monitoring. Patients typically appreciate the non-surgical option but should be counseled about the extended treatment duration and possibility of stone recurrence. The medication is generally well-tolerated, with gastrointestinal side effects being the most common reason for discontinuation.