Ursodeoxycholic Acid (Ursofalk, Cholurso)
Comprehensive guide to ursodeoxycholic acid uses, dosage, side effects, and precautions for liver and gallstone conditions.
Ursodeoxycholic acid (UDCA), marketed as Ursofalk or Cholurso, is a bile acid medication primarily used to treat primary biliary cholangitis (PBC), dissolve certain gallstones, and manage hepatobiliary disorders in conditions like cystic fibrosis.
UDCA occurs naturally in small amounts in human bile and works by improving bile flow, reducing cholesterol saturation in bile, and protecting liver cells from toxic bile acids.
About Ursodeoxycholic Acid
Ursodeoxycholic acid is a hydrophilic bile acid that helps regulate cholesterol in bile and protects the liver from damage caused by hydrophobic (toxic) bile acids. It stimulates hepatobiliary secretion, making it a choleretic agent, and has anti-inflammatory effects on gastrointestinal epithelial cells.
In the body, primary bile acids produced by the liver are metabolized into secondary bile acids by gut bacteria. UDCA reduces intestinal cholesterol absorption, breaks up cholesterol micelles, and promotes the dissolution of cholesterol-rich gallstones.
UDCA has been used for over a century, initially as a liver tonic in traditional Chinese medicine, and is now a standard therapy for cholestatic liver diseases.
Key Uses
UDCA is indicated for several liver and biliary conditions:
- Primary Biliary Cholangitis (PBC): Improves liver biomarkers, delays fibrosis progression, and enhances transplant-free survival. It is the only FDA-approved drug for PBC.
- Gallstone Dissolution: Dissolves radiolucent, cholesterol-rich gallstones in patients unsuitable for surgery, with success rates of 30-60% but high recurrence.
- Hepatobiliary Disorders in Cystic Fibrosis: Treats associated cholestasis.
- Intrahepatic Cholestasis of Pregnancy (ICP): First-line therapy at 20-25 mg/kg/day to improve liver tests and pruritus, though perinatal outcomes may not improve.
- Other: Biliary sludge post-bariatric surgery, bile reflux gastritis; limited efficacy in primary sclerosing cholangitis (PSC), non-alcoholic fatty liver disease, or biliary atresia.
In PBC, meta-analyses show survival benefits with long-term use (>2 years), reducing the risk of death or transplantation by 32%. For PSC, high doses (>28 mg/kg/day) increase mortality risk and are not recommended.
How Ursodeoxycholic Acid Works
UDCA exerts multiple protective effects:
- Choleretic Effect: Stimulates bile acid secretion via calcium signaling, enhancing canalicular membrane transport and vesicular exocytosis.
- Bile Acid Pool Alteration: Increases hydrophilic bile acids, diluting toxic hydrophobic ones that damage cholangiocytes and hepatocytes.
- Anti-Apoptotic: Stabilizes cell membranes, inhibits mitochondrial damage, and reduces bile acid-induced apoptosis.
- Anti-Inflammatory: Regulates cytokines, antimicrobial peptides, and wound healing in epithelial cells.
These mechanisms reduce alkaline phosphatase and bilirubin levels, improve liver histology, and slow fibrosis in cholestatic diseases.
Dosage Information
Dosage varies by condition and is typically weight-based. Take with food to improve absorption.
| Condition | Recommended Dose | Duration |
|---|---|---|
| Primary Biliary Cholangitis (PBC) | 13-15 mg/kg/day, divided doses | Long-term |
| Gallstone Dissolution | 8-10 mg/kg/day | 6-24 months |
| Intrahepatic Cholestasis of Pregnancy | 20-25 mg/kg/day | Until delivery |
| Cystic Fibrosis Hepatobiliary Disorders | 20-30 mg/kg/day | Long-term |
Available as 250 mg capsules, 500 mg tablets, or oral suspension. For PBC, divide into 2-3 doses; monitor liver function every 4 weeks initially, then quarterly.
Cautions
- Do not use in acute gallbladder inflammation, radio-opaque stones, or non-functioning gallbladder.
- Avoid high doses in PSC due to increased death/transplant risk.
- Monitor for gallstone calcification (ultrasound every 6 months).
- Not for complete bile duct obstruction.
Side Effects
UDCA is generally well-tolerated. Common side effects include:
- Diarrhea (most frequent, dose-related).
- Abdominal pain, nausea, pruritus.
- Rare: Liver enzyme elevation, allergic reactions, headache.
Serious effects are uncommon; discontinue if severe diarrhea or worsening liver tests occur. In pregnancy, benefits outweigh risks for ICP.
Before Taking Ursodeoxycholic Acid
Inform your doctor if you have:
- Allergies to bile acids.
- Active peptic ulcer, inflammatory bowel disease, or recent biliary surgery.
- Pregnancy/breastfeeding (use only if essential).
Liver function tests and ultrasound are required before starting. Regular monitoring is essential for efficacy and safety.
How to Take Ursodeoxycholic Acid
Swallow whole with water, preferably with meals. Do not crush/chew tablets. For suspension, shake well. Consistent timing aids absorption.
If a dose is missed, take as soon as remembered unless near next dose. Adherence is crucial for gallstone dissolution and PBC benefits.
Additional Precautions
- Interactions: Antacids, cholestyramine, or estrogen may reduce efficacy; separate by 4 hours.
- Driving/Operating Machinery: No effect.
- Storage: Room temperature, away from moisture.
- Overdose: Diarrhea; seek medical help.
Pregnancy and Breastfeeding
UDCA is category B in pregnancy; used safely for ICP with no increased perinatal risks in trials like PITCHES. Limited data in breastfeeding; consult physician.
Frequently Asked Questions (FAQs)
Q: What is ursodeoxycholic acid used for?
A: Primarily for PBC, gallstone dissolution, and cholestasis in pregnancy or cystic fibrosis.
Q: How long does it take for UDCA to dissolve gallstones?
A: 6-24 months; success in 30-60% of suitable cases, with high recurrence post-treatment.
Q: Does UDCA cure PBC?
A: No, but it slows progression, improves liver tests, and delays transplantation.
Q: Can UDCA cause diarrhea?
A: Yes, the most common side effect; reduce dose if severe.
Q: Is UDCA safe in pregnancy?
A: Yes, first-line for ICP; improves symptoms without proven perinatal harm.
Monitoring and Follow-Up
Liver enzymes (ALT, AST, ALP, bilirubin) should be checked monthly for 3 months, then every 3-6 months. Ultrasound for gallstones every 6 months. Adjust dose based on response; combine with obeticholic acid if incomplete PBC response.
UDCA improves Mayo risk score and histology in PBC, with 76% fibrosis-free at 4 years.
References
- Ursofalk: Dr. Falk Pharma UK & Ireland — Dr. Falk Pharma. 2023. https://uk.drfalkpharma.com/en/products/ursofalk/
- Ursodeoxycholic acid – Wikipedia — Wikipedia Contributors. 2024-01-10. https://en.wikipedia.org/wiki/Ursodeoxycholic_acid
- Information for the user Ursofalk® 500mg film-coated tablets — Medicines.org.uk. 2023. https://www.medicines.org.uk/emc/files/pil.2980.pdf
- Why do we use ursodeoxycholic acid (UDCA) in cholestatic liver diseases? — American Association for the Study of Liver Diseases (AASLD). 2024. https://www.aasld.org/liver-fellow-network/core-series/why-series/why-do-we-use-ursodeoxycholic-acid-udca-cholestatic
- Ursodeoxycholic Acid – StatPearls — NCBI Bookshelf. 2023-07-17. https://www.ncbi.nlm.nih.gov/books/NBK545303/
- Ursodiol (oral route) – Mayo Clinic — Mayo Clinic. 2024. https://www.mayoclinic.org/drugs-supplements/ursodiol-oral-route/description/drg-20066618
- Ursodiol: Uses & Side Effects – Cleveland Clinic — Cleveland Clinic. 2023. https://my.clevelandclinic.org/health/drugs/20178-ursodiol-capsules-or-tablets
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