Bile acid preparations
ATC code: A05AA02 (Ursodeoxycholic acid)
Brand names
Actigall
Hydrophilic tertiary bile acid representing less than 5 % of the human bile acid pool. Reduces biliary cholesterol saturation, promotes dissolution of cholesterol stones, and stabilizes hepatocyte membranes. Competitively displaces toxic hydrophobic bile acids and exerts immunomodulatory and antiapoptotic effects in biliary epithelium. Therapeutic dose 13–15 mg/kg/day.
First line
First-line disease-modifying therapy for primary biliary cholangitis per 2017 and 2018. Dose 13–15 mg/kg/day in 1–4 divided doses. Lowers alkaline phosphatase and bilirubin, slows fibrosis progression, and improves transplant-free survival. Biochemical response is assessed at 12 months. Non-responders may receive obeticholic acid or fibrates per EASL.
Individual decision
Medical litholysis is reserved for a narrow group of patients with symptomatic cholesterol stones and contraindications to surgery. Conditions: radiolucent stones smaller than 10 mm occupying less than half the gallbladder, with preserved gallbladder function. Dose 10–15 mg/kg at bedtime for 6–24 months. Complete dissolution in 30–60 %, with 5-year recurrence of 30–50 %. Cholecystectomy remains standard for symptomatic stones.
First line
Per 2022 and SOGC 2014, ursodeoxycholic acid reduces pruritus and improves maternal biochemistry in intrahepatic cholestasis of pregnancy. Effect on fetal outcomes (stillbirth, preterm birth) is debated — the PITCHES trial (NEJM 2019, over 600 patients) showed no reduction in the composite endpoint. Use is justified symptomatically for pronounced pruritus and significant bile acid elevation.
Not recommended
In metabolic dysfunction-associated steatotic liver disease (MASLD, formerly NAFLD), ursodeoxycholic acid monotherapy has not demonstrated efficacy per 2024 and 2023. Biochemical improvements occur but do not translate into histological or clinical outcomes (fibrosis, cirrhosis, cardiovascular mortality). Use in this niche is unjustified. MASLD management rests on 7–10 % weight loss, physical activity, GLP-1 agonists in coexisting T2D, and resmetirom in MASH with fibrosis.
Not recommended
— Liver 'detox' and cleansing: Cyclic «liver cleansing» with ursodeoxycholic acid in people without established disease is marketing-driven and lacks an evidence base. The liver does not require pharmacological «cleansing». Elevated ALT/AST warrants differential workup (viral hepatitis, MASLD, alcohol, drug-induced injury, autoimmune disease) — the cause is treated.
FDA categories were retired in 2015. Use in the second and third trimesters for intrahepatic cholestasis of pregnancy is common, with reassuring fetal safety in observational data. First-trimester use is restricted to clear indications.
Excreted into breast milk in minimal amounts. Compatible with breastfeeding per LactMed.
ursodeoxycholic acid is evaluated for the following indications with varying evidence strength: Primary biliary cholangitis (evidence tier A), Gallstone disease (cholesterol stones) (evidence tier B), Intrahepatic cholestasis of pregnancy (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of ursodeoxycholic acid (≥ 1 in 100): Diarrhea, dyspepsia, Pruritus (paradoxical, early in therapy), Nausea. See the Safety section for uncommon and serious reactions.
FDA categories were retired in 2015. Use in the second and third trimesters for intrahepatic cholestasis of pregnancy is common, with reassuring fetal safety in observational data. First-trimester use is restricted to clear indications.
Excreted into breast milk in minimal amounts. Compatible with breastfeeding per LactMed.
ursodeoxycholic acid is contraindicated in: Acute cholecystitis, cholangitis; Biliary obstruction; Calcified (radiopaque) stones; Non-functioning gallbladder (for medical litholysis); Severe hepatic or renal impairment. Full list in the Safety section.