Ursodiol

ACTIGALL

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Pronunciation: ER-soe-dye-ol

Ursodiol ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Ursodiol ballicule

Ursodiol ACTIGALL mascot mnemonic cartoon — Visual mnemonic: Ursodiol mascot
**“Urso Active against gallstones”**

What it isHydrophilic bile acid that displaces toxic bile acids; primary biliary cholangitis and cholesterol gallstones.

Why this oneThe 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.

Ursodiol molecular structure (skeletal formula) — Molecular structure: Ursodiol

FDA-approved for

primary biliary cholangitis (1997)
gallstone dissolution

Off-label

intrahepatic cholestasis of pregnancy

Principal riskDiarrhea

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

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.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
Radiolucent noncalcified gallbladder stones <20 mm (dissolution; surgery high-risk or refused)	Adults	8-10 mg/kg/day in 2 or 3 divided doses	8-10 mg/kg/day	Undefined (safety beyond 24 months not established)
Gallstone prevention in obese patients with rapid weight loss	Adults	300 mg BID	600 mg/day (300 mg BID)	Undefined

Renal Undefined

Hepatic Undefined

Dissolution: gallbladder ultrasound every 6 months in year 1; confirm dissolution with repeat ultrasound within 1 to 3 months; success unlikely if no partial dissolution by 12 months. AST/ALT at initiation

Available strengths

cap 150, 200, 300, 400 mg
tab 250, 500 mg

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
Allergy to bile acids

Cautions

Enteroliths (bezoars) in patients at risk for intestinal stenosis or stasis
Liver tests (AST/ALT at initiation)
Bile acid sequestrants/aluminum antacids reduce effect; estrogens, OCs, clofibrate may counteract

Adverse reactions

Abdominal pain
Diarrhea
Constipation
Nausea
Vomiting
Dyspepsia
Headache
Dizziness
Back pain
Upper respiratory tract infection
Viral infection
Fatigue

Pregnancy No fetal harm in animal studies at 20- to 100-fold human dose; no adequate human studies; not recommended during pregnancy

Lactation Unknown if excreted in human milk; use caution in nursing mothers

Cost

Ursodiol (ACTIGALL)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/unit	CostPlus
150 mg	cap	per unit		not offered
200 mg	cap	per unit		not offered
300 mg	cap	per unit	$0.43/ea	offered
400 mg	cap	per unit		not offered

Generic entry2000

Open Ursodiol in the interactive console ↗

Self-check

How does ursodiol change the bile-acid pool?
Displaces toxic bile acids.
Which stones can ursodiol dissolve?
Small, non-calcified cholesterol stones.