Ursofalk (Ursodeoxycholic Acid / UDCA)
Bile acid therapy for gallstone dissolution and chronic liver disease
Quick Facts About Ursofalk
Key Takeaways About Ursofalk
- Naturally occurring bile acid: UDCA is a hydrophilic bile acid normally found in small amounts in human bile, making it well-tolerated by most patients
- Dual therapeutic role: Used both for dissolving cholesterol gallstones (6–24 months treatment) and as long-term therapy for primary biliary cholangitis
- Liver protection: Protects liver cells by replacing toxic bile acids, stabilizing cell membranes, and stimulating bile flow
- Regular monitoring required: Liver function tests should be performed during the first 3 months and periodically thereafter
- Contraception needed: Women of childbearing potential should use effective contraception; non-hormonal methods preferred for gallstone treatment
What Is Ursofalk and What Is It Used For?
Ursofalk contains ursodeoxycholic acid (UDCA), a naturally occurring bile acid that dissolves cholesterol gallstones and treats chronic liver diseases including primary biliary cholangitis (PBC). It works by reducing cholesterol saturation in bile, protecting liver cells from toxic bile acids, and stimulating bile secretion.
Ursodeoxycholic acid (UDCA), the active ingredient in Ursofalk, is a hydrophilic bile acid that naturally occurs in small quantities in human bile. Unlike the predominant bile acids in the body, which can be toxic to liver cells at high concentrations, UDCA has cytoprotective properties that make it valuable in treating a range of hepatobiliary conditions. It was first identified in bear bile and has been used therapeutically in traditional medicine for centuries, but modern pharmaceutical formulations have made it accessible as a standardized, prescription medication.
The primary approved indications for Ursofalk include the dissolution of small, radiolucent (non-calcified) cholesterol gallstones in patients with a functioning gallbladder, and the treatment of primary biliary cholangitis (PBC), previously known as primary biliary cirrhosis. In patients with gallstones, UDCA works by reducing the cholesterol saturation of bile, which gradually allows existing stones to dissolve over a period of 6 to 24 months. For PBC, it provides hepatoprotective effects that can slow disease progression, improve liver biochemistry, and enhance long-term transplant-free survival.
Ursofalk is additionally approved for the treatment of cystic fibrosis-associated liver disease (CFALD) in children and adolescents aged 6 to 18 years. Liver disease is the third leading cause of death in cystic fibrosis patients, and UDCA therapy aims to improve bile flow and reduce liver damage in this vulnerable population. The European Association for the Study of the Liver (EASL) and the American College of Gastroenterology (ACG) both recognize UDCA as a first-line treatment for PBC with strong evidence supporting its efficacy.
UDCA exerts its effects through multiple mechanisms: it replaces toxic hydrophobic bile acids in the bile acid pool (enriching it with a more hydrophilic composition), stabilizes hepatocyte cell membranes against bile acid-induced damage, stimulates choleresis (bile flow) through the liver and bile ducts, and modulates immune responses that contribute to liver inflammation. In gallstone dissolution, it specifically reduces biliary cholesterol secretion and promotes the formation of liquid crystals that facilitate stone dissolution.
What Should You Know Before Taking Ursofalk?
Ursofalk should not be used in patients with acute gallbladder inflammation, bile duct obstruction, frequent biliary colic, calcified gallstones, or impaired gallbladder function. Liver function monitoring is essential during the first three months of treatment, and women of childbearing potential must use effective contraception.
Contraindications
There are several important situations in which Ursofalk must not be used. Understanding these contraindications is essential for safe prescribing and patient awareness. Your healthcare provider will assess these factors before initiating treatment.
Do not take Ursofalk if you have any of the following conditions:
- Allergy to ursodeoxycholic acid or any other ingredient in the formulation (see the composition section below)
- Acute inflammation of the gallbladder (acute cholecystitis) or biliary tract inflammation (acute cholangitis)
- Obstruction of the common bile duct or the cystic duct (bile duct blockage)
- Frequent biliary colic — recurrent cramping pains in the upper abdomen associated with gallstone disease
- Calcified (radio-opaque) gallstones — UDCA only dissolves cholesterol stones, not calcified ones
- Impaired gallbladder contractility — the gallbladder must be functional for gallstone dissolution to occur
- Children with biliary atresia who have poor bile flow even after surgical correction (Kasai procedure)
Warnings and Precautions
During the first three months of Ursofalk therapy, your physician will monitor your liver function through blood tests (liver enzymes including ALT, AST, GGT, and alkaline phosphatase). These tests help ensure that treatment is effective and allow early detection of any adverse hepatic effects. In some patients, particularly those with PBC, monitoring may be required at more frequent intervals.
When Ursofalk is used for gallstone dissolution, imaging studies (typically ultrasound) are performed after 6 to 10 months to evaluate treatment progress. If there is no reduction in gallstone size after 12 months of continuous therapy, the treatment should be discontinued as further dissolution is unlikely. Patients should be aware that gallstones can recur after successful dissolution if the underlying metabolic factors (such as biliary cholesterol supersaturation) persist.
In PBC treatment, some patients may experience a temporary worsening of symptoms, particularly pruritus (itching), during the initial phase of therapy. This is generally a transient phenomenon. If it occurs, your doctor may temporarily reduce the daily dose and then gradually increase it back to the target dose over several weeks. If diarrhea develops during treatment, inform your physician as a dose adjustment may be necessary.
Women taking Ursofalk for gallstone dissolution should use only non-hormonal contraceptive methods, as hormonal contraceptives (including combined oral contraceptive pills) may increase biliary cholesterol secretion and promote gallstone formation, potentially counteracting the therapeutic effect of UDCA. For other indications, low-dose estrogen oral contraceptives may be used, but non-hormonal methods are still preferred.
Pregnancy and Breastfeeding
The safety of Ursofalk during pregnancy has not been fully established in humans. Animal studies have shown some evidence of reproductive toxicity at very high doses, although the relevance of these findings to human use is uncertain. As a precautionary measure, Ursofalk should not be used during pregnancy unless it is considered absolutely necessary by the treating physician and the potential benefits clearly outweigh the risks to the fetus.
It is not known whether ursodeoxycholic acid or its metabolites are excreted in human breast milk. Therefore, breastfeeding is not recommended during Ursofalk treatment unless the clinical necessity has been carefully evaluated. Before starting treatment, a pregnancy test should be performed to rule out pregnancy. Women of childbearing potential should use reliable contraception throughout the entire course of treatment.
It is worth noting that UDCA has been used off-label in some clinical settings for intrahepatic cholestasis of pregnancy (ICP), where it has shown benefits in reducing maternal pruritus and improving fetal outcomes. However, this use should only occur under close specialist supervision and is separate from the standard approved indications discussed here.
How Does Ursofalk Interact with Other Drugs?
Ursofalk can interact with bile acid sequestrants (cholestyramine, colestipol), aluminium-containing antacids, ciclosporin, ciprofloxacin, and hormonal contraceptives. These medications should be taken at least 2 hours apart from Ursofalk, and dose adjustments may be needed for some drugs.
Drug interactions with ursodeoxycholic acid can affect its absorption, efficacy, or the blood levels of co-administered medications. Understanding these interactions is important for maximizing therapeutic benefit and minimizing potential risks. Always inform your healthcare provider about all medications, supplements, and herbal products you are taking before starting Ursofalk.
Major Interactions
The most clinically significant interactions involve drugs that reduce UDCA absorption or whose levels are significantly affected by UDCA therapy. Bile acid sequestrants such as cholestyramine and colestipol bind UDCA in the intestinal lumen, dramatically reducing its absorption and rendering it ineffective. If concomitant use is unavoidable, the bile acid sequestrant should be taken at least 2 hours before or after Ursofalk, though ideally these combinations should be avoided altogether.
Ciclosporin (cyclosporine) absorption may be significantly increased by UDCA, potentially leading to elevated blood levels and increased toxicity risk. Patients taking both medications require close monitoring of ciclosporin blood levels, and dose adjustments may be necessary. This interaction is particularly relevant in transplant patients who may be taking both drugs concurrently.
Minor Interactions
Aluminium hydroxide-containing antacids can bind UDCA in the gastrointestinal tract, reducing its bioavailability. These should be taken at least 2 hours apart from Ursofalk. Several other medications have documented interactions of lesser clinical significance, including ciprofloxacin, nitrendipine, dapsone, and rosuvastatin, where UDCA may alter their absorption or metabolism to varying degrees.
| Interacting Drug | Effect | Recommendation |
|---|---|---|
| Cholestyramine / Colestipol | Reduces UDCA absorption by binding in the gut | Take at least 2 hours apart; avoid if possible |
| Aluminium hydroxide antacids | Reduces UDCA absorption | Take at least 2 hours apart |
| Ciclosporin (Cyclosporine) | UDCA may increase ciclosporin blood levels | Monitor ciclosporin levels closely; adjust dose as needed |
| Ciprofloxacin | Possible altered absorption | Inform your doctor; monitoring may be required |
| Nitrendipine | Possible altered blood levels | Monitor blood pressure; dose adjustment may be needed |
| Dapsone | Possible altered absorption | Inform your doctor if taking concurrently |
| Hormonal contraceptives (estrogen-containing) | May increase biliary cholesterol, counteracting gallstone dissolution | Use non-hormonal contraception for gallstone treatment |
| Clofibrate | May increase biliary cholesterol secretion | Avoid concomitant use during gallstone dissolution |
| Rosuvastatin | UDCA may alter rosuvastatin levels | Monitor for statin-related side effects |
What Is the Correct Dosage of Ursofalk?
Ursofalk dosage depends on the condition being treated and the patient's body weight. For gallstone dissolution, the typical adult dose is 10–12 mg/kg/day in two divided doses. For primary biliary cholangitis, the dose is 12–16 mg/kg/day. For cystic fibrosis-associated liver disease in children, the dose is 20 mg/kg/day in 2–3 divided doses.
Always take Ursofalk exactly as prescribed by your doctor. The dosage is weight-based and varies depending on the indication. Do not change your dose or stop taking the medication without consulting your healthcare provider. Swallow the tablets whole without chewing or crushing, with a glass of water or other liquid. Regular and consistent dosing is essential for therapeutic success.
Adults
Gallstone Dissolution
Dose: 10–12 mg per kg body weight per day, divided into 2 doses (morning and evening).
Duration: Treatment typically lasts 6 to 24 months. Gallstone dissolution is monitored by ultrasound every 6 to 10 months. If no reduction in stone size is observed after 12 months, treatment should be discontinued.
Example: A 70 kg adult would take approximately 700–840 mg daily, equivalent to 1 tablet (500 mg) in the morning and half a tablet (250 mg) in the evening, or as directed by the physician.
Primary Biliary Cholangitis (PBC)
Dose: 12–16 mg per kg body weight per day.
Initial phase (first 3 months): The daily dose should be divided across the day (morning, midday, and evening) to improve tolerability.
Maintenance phase: Once liver values have improved, the entire daily dose may be taken as a single dose in the evening.
Duration: Treatment for PBC is generally continued indefinitely, as it is a chronic condition requiring long-term management.
Children (6–18 years) — Cystic Fibrosis-Associated Liver Disease
The recommended daily dose for children with cystic fibrosis-associated liver disease is 20 mg per kg body weight, divided into 2 to 3 doses. The doctor may increase the dose up to 30 mg/kg/day if clinically indicated. The following table provides dosing guidance based on body weight using 500 mg film-coated tablets.
| Body Weight (kg) | Daily Dose (mg/kg) | Morning | Midday | Evening |
|---|---|---|---|---|
| 20–29 kg | 17–25 mg/kg | ½ tablet | — | ½ tablet |
| 30–39 kg | 19–25 mg/kg | ½ tablet | ½ tablet | ½ tablet |
| 40–49 kg | 20–25 mg/kg | ½ tablet | ½ tablet | 1 tablet |
| 50–59 kg | 21–25 mg/kg | ½ tablet | 1 tablet | 1 tablet |
| 60–69 kg | 22–25 mg/kg | 1 tablet | 1 tablet | 1 tablet |
| 70–79 kg | 22–25 mg/kg | 1 tablet | 1 tablet | 1½ tablets |
| 80–89 kg | 22–25 mg/kg | 1 tablet | 1½ tablets | 1½ tablets |
| 90–99 kg | 23–25 mg/kg | 1½ tablets | 1½ tablets | 1½ tablets |
| 100–109 kg | 23–25 mg/kg | 1½ tablets | 1½ tablets | 2 tablets |
| >110 kg | — | 1½ tablets | 2 tablets | 2 tablets |
The tablets can be split in half along the score line. If only half a tablet is used, the remaining half can be stored for the next dose. For patients weighing less than 47 kg or those who cannot swallow tablets, Ursofalk oral solution may be a more suitable alternative.
Elderly
No specific dose adjustment is generally required for elderly patients. However, as with all medications in older adults, careful clinical monitoring is advisable, particularly regarding liver and kidney function. Elderly patients may be more susceptible to diarrhea, and dose reductions may be needed if gastrointestinal side effects occur. The prescribing physician will determine the appropriate dose based on the individual patient's clinical status, weight, and indication.
Missed Dose
If you forget to take a dose of Ursofalk, take it as soon as you remember, unless it is almost time for your next scheduled dose. In that case, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a forgotten one. Consistency is important for effective treatment, particularly in gallstone dissolution where interruptions may slow progress.
Overdose
In the event of an overdose, diarrhea is the most likely symptom. If significant overdose occurs, or if a child accidentally ingests the medication, seek medical attention immediately or contact your local poison control center. There is no specific antidote for ursodeoxycholic acid overdose; treatment is symptomatic and supportive. Electrolyte balance should be monitored and corrected if necessary, particularly if diarrhea is severe or prolonged.
What Are the Side Effects of Ursofalk?
The most common side effect of Ursofalk is diarrhea, occurring in up to 1 in 10 patients. Pale stools may also occur. Serious side effects are very rare and include severe upper abdominal pain and worsening liver function in PBC patients. Nausea, vomiting, itching, and urticaria have been reported at unknown frequency.
Like all medicines, Ursofalk can cause side effects, although not everyone experiences them. Most side effects are mild and related to the gastrointestinal system, which is expected given the drug's mechanism of action on bile acid metabolism. The following frequency grid categorizes known adverse reactions based on their reported incidence in clinical trials and post-marketing surveillance.
Common
- Diarrhea or loose stools
- Pale-colored (light) stools
Very Rare
- Severe pain in the right upper abdomen (during PBC treatment)
- Worsening liver function during PBC treatment (reversible upon discontinuation)
- Calcification of gallstones (detected on imaging; usually asymptomatic)
- Urticaria (hives)
Frequency Not Known
- Pruritus (itching), particularly during initial treatment of PBC
- Nausea
- Vomiting
The diarrhea associated with Ursofalk treatment is typically dose-related and may improve with dose reduction. If you experience persistent diarrhea, contact your healthcare provider as a dose adjustment may resolve the issue. Pale stools are a pharmacological effect related to changes in bile composition and are not generally a cause for concern.
In patients being treated for PBC, a temporary worsening of symptoms — especially itching — may occur in the early weeks of treatment. This is usually self-limiting and resolves as the body adjusts to the medication. However, if symptoms become severe or persistent, your doctor may temporarily reduce the dose before gradually escalating it back to the target level.
Contact your doctor promptly if you experience severe or persistent abdominal pain (especially in the upper right quadrant), signs of jaundice (yellowing of the skin or eyes), severe or worsening diarrhea, or any signs of an allergic reaction such as widespread hives, swelling of the face or throat, or difficulty breathing.
How Should You Store Ursofalk?
Store Ursofalk at room temperature, in its original packaging, out of reach and sight of children. No special storage conditions are required. Do not use the medication after the expiry date printed on the packaging.
Ursofalk film-coated tablets do not require any special storage conditions. Store them at room temperature, away from excessive heat and moisture. Keep the medication in its original blister packaging to protect it from environmental factors. As with all medications, store Ursofalk out of the sight and reach of children to prevent accidental ingestion.
Check the expiry date (marked as "EXP" on the packaging) before taking the medication. The expiry date refers to the last day of the stated month. Do not use Ursofalk after this date. Unused or expired medications should not be disposed of via household waste or flushed down the toilet. Return them to a pharmacy for safe disposal to protect the environment.
What Does Ursofalk Contain?
Each Ursofalk 500 mg film-coated tablet contains 500 mg of ursodeoxycholic acid as the active ingredient, along with inactive excipients including magnesium stearate, povidone K 25, microcrystalline cellulose, and a hypromellose-based film coating.
The active substance in each film-coated tablet is 500 mg ursodeoxycholic acid (UDCA). This is a white, crystalline substance that is poorly soluble in water but soluble in ethanol and glacial acetic acid. The pharmaceutical form is a white, oval, biconvex film-coated tablet with a score line on both sides, allowing it to be divided into two equal halves for flexible dosing.
The inactive ingredients (excipients) serve various pharmaceutical functions:
- Magnesium stearate — lubricant to prevent the tablet from sticking to manufacturing equipment
- Polysorbate 80 — wetting agent to improve drug dissolution
- Povidone K 25 — binding agent to hold the tablet together
- Microcrystalline cellulose — filler and disintegrant
- Colloidal anhydrous silica — flow agent for uniform tablet content
- Crospovidone (Type A) — superdisintegrant for rapid tablet break-up
- Talc — glidant and anti-tack agent
- Hypromellos — film-coating polymer
- Macrogol 6000 — plasticizer in the film coating
Ursofalk 500 mg tablets are available in packs of 50 or 100 film-coated tablets. Not all pack sizes may be marketed in every country. The manufacturer is Dr. Falk Pharma GmbH, based in Freiburg, Germany, a pharmaceutical company specializing in gastroenterology and hepatology medications.
Frequently Asked Questions About Ursofalk
Ursofalk (ursodeoxycholic acid / UDCA) is used primarily for two conditions: dissolving small, non-calcified cholesterol gallstones in patients with a functioning gallbladder, and treating primary biliary cholangitis (PBC), a chronic autoimmune liver disease. It is also used for cystic fibrosis-associated liver disease in children aged 6 to 18 years. UDCA works by reducing the cholesterol content of bile, protecting liver cells, and stimulating bile flow.
Gallstone dissolution with Ursofalk typically takes 6 to 24 months. The treatment is most effective for small, radiolucent (non-calcified) cholesterol gallstones in patients with a functioning gallbladder. Progress is evaluated by ultrasound after 6 to 10 months. If no reduction in stone size is observed after 12 months of continuous treatment, the therapy should generally be discontinued.
The most common side effect is diarrhea, occurring in up to 1 in 10 patients. Pale-colored stools are also frequently reported. These effects are related to the drug's action on bile acid metabolism and are usually dose-dependent. Very rare side effects include severe upper abdominal pain during PBC treatment, temporary worsening of liver function, gallstone calcification, and urticaria (hives). Nausea, vomiting, and itching have also been reported.
Ursofalk should generally not be used during pregnancy unless considered absolutely necessary by the treating physician. The effects on the fetus have not been fully established. Women of childbearing potential must use effective contraception while taking Ursofalk. For gallstone dissolution treatment, non-hormonal contraceptives are specifically recommended, as hormonal contraceptives may increase gallstone formation.
Yes, for primary biliary cholangitis (PBC), Ursofalk is typically taken indefinitely as long-term maintenance therapy. PBC is a chronic condition, and ongoing UDCA treatment has been shown to slow disease progression, improve liver biochemistry, and enhance transplant-free survival. Regular monitoring of liver function tests is essential throughout treatment. For gallstone dissolution, treatment is time-limited (usually 6–24 months) and discontinued once stones have dissolved or if no progress is seen after 12 months.
No, Ursofalk has no known effect, or a negligible effect, on the ability to drive or operate machinery. It does not cause drowsiness, dizziness, or impaired concentration at therapeutic doses. You can continue your normal daily activities, including driving, while taking this medication.
References
This article is based on the following peer-reviewed sources and international medical guidelines:
- European Association for the Study of the Liver (EASL). EASL Clinical Practice Guidelines: The diagnosis and management of patients with primary biliary cholangitis. Journal of Hepatology, 2017; 67(1): 145–172. Updated 2023.
- Lindor KD, Bowlus CL, Boyer J, et al. Primary Biliary Cholangitis: 2018 Practice Guidance from the American Association for the Study of Liver Diseases. Hepatology, 2019; 69(1): 394–419.
- European Medicines Agency (EMA). Ursodeoxycholic acid — Summary of Product Characteristics. EMA Product Information Database.
- National Institute for Health and Care Excellence (NICE). Gallstone disease: diagnosis and management. Clinical guideline CG188, 2014 (updated 2023).
- Poupon RE, Lindor KD, Cauch-Dudek K, et al. Combined analysis of randomized controlled trials of ursodeoxycholic acid in primary biliary cirrhosis. Gastroenterology, 1997; 113(3): 884–890.
- Colombo C, Battezzati PM, Crosignani A, et al. Liver disease in cystic fibrosis: A prospective study on incidence, risk factors, and outcome. Hepatology, 2002; 36(6): 1374–1382.
- World Health Organization (WHO). WHO Model List of Essential Medicines. 23rd List, 2023. Geneva: WHO.
- Portincasa P, Di Ciaula A, Bonfrate L, Wang DQ. Therapy of gallstone disease: What it was, what it is, what it will be. World Journal of Gastrointestinal Pharmacology and Therapeutics, 2012; 3(2): 7–20.
About the Medical Editorial Team
This article has been written and reviewed by the iMedic Medical Editorial Team, a group of licensed specialist physicians with expertise in gastroenterology, hepatology, and clinical pharmacology. Our editorial process follows the GRADE evidence framework and adheres to guidelines from international organizations including EASL, ACG, and WHO.
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