ACTIGALL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACTIGALL (ACTIGALL).
Gallstone dissolution agent; reduces cholesterol saturation of bile by decreasing hepatic cholesterol secretion and increasing bile acid pool.
| Metabolism | Hepatic conjugation with glycine and taurine; undergoes enterohepatic circulation. |
| Excretion | Primarily fecal (biliary excretion of unchanged drug and metabolites); renal excretion is minimal (<1% of dose as unchanged drug). |
| Half-life | Terminal elimination half-life is approximately 3–5 days, reflecting enterohepatic circulation and slow turnover of the bile acid pool. |
| Protein binding | Extensive, >90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.1–0.2 L/kg, indicating distribution mainly in extracellular fluid and bile; limited tissue penetration. |
| Bioavailability | Oral bioavailability is approximately 30–60% due to incomplete absorption and first-pass hepatic extraction. |
| Onset of Action | Oral: Clinical effects (gallstone dissolution) observed after several weeks to months of continuous therapy; no parenteral formulation. |
| Duration of Action | Duration of action is prolonged due to enterohepatic circulation; continued therapy for up to 24 months may be required for gallstone dissolution. Effects persist as long as drug is present in bile salt pool. |
300 mg orally twice daily, or 8-10 mg/kg/day divided into 2-3 doses.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | Use with caution; no specific Child-Pugh based adjustments established. Avoid in severe hepatic disease. |
| Pediatric use | Not established; safety and efficacy not studied in pediatric patients. |
| Geriatric use | No specific dose adjustments; use standard adult dosing with monitoring for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACTIGALL (ACTIGALL).
| Breastfeeding | Ursodiol is excreted into human milk; M/P ratio not established. Caution is advised due to potential for adverse effects in nursing infants. |
| Teratogenic Risk | Pregnancy Category B. No evidence of fetal harm in animal studies; insufficient human data. Risk cannot be ruled out during first trimester; use only if clearly needed. |
| Fetal Monitoring | Monitor liver function tests, bilirubin, and gallbladder ultrasound in pregnancy. Assess fetal growth and well-being with serial ultrasound if prolonged therapy. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Calcified gallstones","Non-functioning gallbladder","Biliary tract obstruction","Chronic liver disease","Pregnancy"]
| Precautions | ["May cause gallstone calcification","Not effective for radiopaque or calcified stones","Diarrhea common","Monitor liver function tests"] |
| Food/Dietary | No specific food interactions reported. However, a low-cholesterol diet may support gallstone dissolution. Avoid excessive alcohol intake as it may impair liver function. |
| Clinical Pearls |
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| Fertility Effects | No known effect on human fertility. In animal studies, no impairment of fertility observed. |
| Ursodeoxycholic acid (Actigall) is a bile acid that reduces cholesterol saturation in bile and promotes dissolution of cholesterol gallstones. Use is limited to radiolucent, non-calcified gallstones <20 mm in diameter in patients with a functioning gallbladder. Therapy may take up to 24 months; assess stone dissolution by ultrasound every 6 months. Discontinue if stones enlarge, calcify, or no response after 12 months. Avoid in patients with chronic liver disease or biliary tract obstruction. Monitor liver enzymes periodically. |
| Patient Advice | Take Actigall exactly as prescribed, usually 2-3 times daily with or without food. · It may take several months to years for gallstones to dissolve completely; regular follow-up ultrasounds are needed. · Do not stop taking the medication without consulting your doctor, even if you feel well. · Report any new or worsening abdominal pain, jaundice, or clay-colored stools immediately. · This medication is not for rapid pain relief; acute gallstone attacks require prompt medical attention. · If you miss a dose, take it as soon as you remember unless it is almost time for your next dose; do not double the dose. · Store Actigall at room temperature away from moisture and heat. |