Ursodiol
ACTIGALL
What it isHydrophilic bile acid that displaces toxic bile acids; primary biliary cholangitis and cholesterol gallstones.
Why this oneIt is the only treatment that improves transplant-free survival in primary biliary cholangitis.
What limits itIt dissolves only small, non-calcified cholesterol stones, and slowly. Diarrhea; stones recur when it is stopped.
FDA-approved for
- primary biliary cholangitis (1997)
- gallstone dissolution
Off-label
- intrahepatic cholestasis of pregnancy
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Radiolucent gallbladder stone dissolution | Adults | 8–10 mg/kg/day in 2–3 divided doses | 8–10 mg/kg/day | 10 mg/kg/day |
| Gallstone prevention during rapid weight loss | Adults | 300 mg BID | 600 mg/day | 600 mg/day |
Renal Undefined
Hepatic Undefined
Instructions
- Obtain gallbladder ultrasound at 6-month intervals during the first year to monitor dissolution
- If stones appear dissolved, confirm with repeat ultrasound in 1–3 months
- If no partial dissolution by 12 months, success is unlikely
Contraindications
- Calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones (will not dissolve)
- Compelling reasons for cholecystectomy: unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-gastrointestinal fistula
Cautions
- Ineffective for calcified cholesterol, radiopaque, or bile pigment stones
Adverse reactions
- Diarrhea
- Abdominal pain
- Nausea, vomiting, dyspepsia, constipation
- Headache, dizziness
- Back pain, arthralgia
- Upper respiratory tract infection
Pregnancy Animal studies show no fetal harm at therapeutic multiples; not recommended during pregnancy
Lactation Undefined
NO BOXED WARNINGS
Principal riskDiarrhea
Cost, est. cash$5–$150/month
Generic entry2000
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Ursodiol ballicule
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