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Ursolit

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Ursolit

Ursolit_EN

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Ursolit

Quick Facts

Property Description
Active ingredient Ursodiol (Ursodeoxycholic Acid, UDCA)
Form Oral capsule or oral tablet
Pharmacological class Cholelitholytic agent, Hepatoprotective agent
General purpose Modulating bile composition and providing cell protection
Origin Naturally occurring compound, synthesized to pharmaceutical grade

What Type of Medicine is Ursolit, and What Is Its Active Ingredient?

Ursolit is a prescription medicine and a single-ingredient product classified primarily as a Cholelitholytic agent and a Hepatoprotective agent. Its sole active substance is Ursodiol, also known by its official chemical name Ursodeoxycholic Acid (UDCA), which is formulated for oral administration as solid oral capsules or oral tablets.

This dual pharmacological classification confirms its core function in modifying bile and protecting cells. Ursodiol is categorized as a Bile Acid, a classification recognized for its potential to alter the fundamental makeup of the bile.

Is Ursodiol a Natural or Synthetic Substance?

The active ingredient, Ursodiol, is a secondary bile acid and an endogenous compound that naturally occurs in small quantities in normal human bile. However, the medicine Ursolit utilizes a high-purity, synthetic/pharmaceutical grade form of Ursodiol to ensure consistent dosing and effectiveness.

Ursodiol belongs to the family of hydrophilic bile acids, a property that makes it less toxic to liver cells compared to other naturally occurring, more hydrophobic bile acids. As a secondary bile acid, Ursodiol protects liver cells from bile-acid induced damage. This protective quality supports its clinical use in conditions affecting the biliary system.

What Is the General Purpose of Ursolit?

The general purpose of Ursolit is to fundamentally modulate the bile composition and provide cytoprotection to the cells lining the liver and bile ducts, promoting a healthier internal biliary environment. Ursodiol achieves this by reducing the cholesterol saturation in bile and displacing more toxic hydrophobic bile acids within the system.

This unique physiological action is critical for conditions where the bile is unbalanced. For instance, its action of promoting the solubilization of cholesterol gallstones is a distinguishing feature, making it suitable for patients needing to regulate the solidity of bile components. This protective and bile-regulating effect defines its general application in conditions affecting bile flow and liver integrity.

Regulatory References

  1. National Institutes of Health (NIH)

What side effects are possible with Ursolit?

Possible Side Effects and Safety Information for Ursolit

Adverse Reactions Overview

Ursolit (ursodiol) is generally well-tolerated, but it is associated with several adverse reactions, primarily affecting the gastrointestinal and hepatobiliary systems. Common side effects reported during clinical studies include diarrhea and abdominal discomfort or pain. Headache, nausea, and dyspepsia have also been frequently noted.

Less common side effects documented include alopecia (hair loss), rash, and hypersensitivity reactions. In rare instances, patients may experience worsening of pre-existing jaundice or other signs of hepatic function deterioration. Post-marketing experience has identified serious hypersensitivity reactions, such as angioedema and laryngeal edema, where the frequency is not known.

Safety Considerations and Contraindications

Ursolit is contraindicated in patients with a complete and persistent obstruction of the bile ducts and in those with calcified cholesterol or radiopaque gallstones. It is also not indicated for patients who require urgent surgical intervention for complications like unremitting cholecystitis or biliary-gastrointestinal fistula.

Safety Monitoring

Due to the potential for the drug to affect liver function, official labeling requires routine safety monitoring. Liver function tests, including gamma-GT, alkaline phosphatase, AST, ALT, and bilirubin levels, must be checked every month for the first three months of therapy, and every six months thereafter. This ongoing monitoring is necessary for the early detection of a possible, clinically significant deterioration of hepatic function. Caution is advised for its use in patients with other underlying liver conditions. Limited data suggest no identified drug-associated risk in pregnant women, though use during lactation is typically approached with caution.

Overdose and Emergency Response

Overdose and When to Seek Help

The official regulatory documents for Ursolit (Ursodiol) confirm that there have been no reports of accidental or intentional human overdosage documented in the prescribing information. This absence of reports contributes to the classification of the medication as having a low acute toxicity profile.

Documented Manifestations and Emergency Actions

The most likely and documented clinical manifestation of a severe overdose is diarrhea. This is supported by regulatory context explaining that absorption of Ursodiol naturally decreases with increasing dosage, leading to greater amounts of the substance being excreted. This physiological self-limitation is cited by authorities as the reason why other severe systemic symptoms are generally considered unlikely.

Manifestation and Action Regulatory Statement
Most Likely Sign Diarrhea, which requires symptomatic management.
Urgent Action Required Individuals must seek immediate medical attention or contact a poison control center if an overdose is suspected, as mandated by official guidance.
Supportive Measure In cases of persistent overdose-related diarrhea, the officially mandated actions include dose reduction or discontinuation of therapy. Supportive care may involve the use of ion-exchange resins to limit further bile acid absorption.

Monitoring Requirements

While severe outcomes are not reported, official monitoring requirements are mandated in the overdose context. It is officially referenced that liver function should be monitored following a suspected overdose, ensuring appropriate clinical oversight as directed by prescribing information.

Therapeutic Uses of Ursolit

What Ursolit Treats: Main Uses and Benefits

Ursolit is a medication that may be used to address symptoms related to specific digestive and liver conditions. Its use is associated with alleviating discomfort and aiding in the management of these conditions. The medicine is commonly utilized to address specific indications, including cholesterol gallstone dissolution, primary biliary cholangitis (PBC), and certain forms of intrahepatic cholestasis (impaired bile flow within the liver).

The potential benefit for patients includes the management of challenging symptoms like pruritus (itching) that can be associated with PBC, and the therapeutic effect on cholesterol stones. This medication is intended to support the management of symptoms and liver health.

Quick Fact: Relief for Pruritus Ursolit may assist in the management of the intense itching (pruritus) that can occur with Primary Biliary Cholangitis (PBC).

Eligibility and Restrictions for Use

Official Eligibility Rules for Ursolit (Ursodiol)

Eligibility for Ursolit is strictly defined by regulatory authorities based on pre-existing patient conditions, particularly those affecting the biliary system.

Populations Who Must Not Use Ursolit (Contraindications)

Ursolit is contraindicated and must not be used by individuals with:

  • Complete biliary obstruction (blockage of the bile ducts).
  • Acute inflammation of the gallbladder or biliary tract.
  • Radio-opaque calcified gallstones. The medicine is indicated only for radiolucent (non-calcified) stones.
  • Known hypersensitivity to the active ingredient, ursodiol, or bile acids.
  • Impaired gallbladder function or frequent biliary colic.

Age-Related and Conditional Eligibility

Age Group Regulatory Status
Adults Established for all approved indications.
Pediatric (General) Safety and effectiveness are not established for gallstone or PBC indications.
Pediatric (Specific) Established for children 6–18 years with cystic fibrosis-related hepatobiliary disorders.

Pregnancy and Lactation: Use during pregnancy is not recommended unless clearly necessary. Caution should be exercised, and use is generally not recommended during breastfeeding. Furthermore, women of childbearing potential taking Ursolit for gallstone dissolution are required to use effective non-hormonal contraception.

What should I know about interactions with other medicines?

Interaction Map: Interactions with other medicines and products — official regulatory information for Ursolit

Category Official Regulatory Statement
Medicinal product categories with documented interactions Bile Acid Sequestering Agents; Aluminum-based Antacids; Estrogens; Oral Contraceptives; Lipid-lowering agents (e.g., Fibrates).
Specific interacting medicines (if explicitly listed) Cholestyramine, Colestipol; Clofibrate; Ciclosporin; Nitrendipine; Dapsone.
Mechanistic basis of interactions (only if stated in label) Inhibition of Ursodiol absorption (via binding in the gut); Counteraction of therapeutic effect (via increased hepatic cholesterol secretion); Alteration of other drug's blood levels (e.g., increased Ciclosporin absorption).
Timing-based interaction rules (if applicable) Mandatory Separation: Binding agents must be taken at least 2 hours before or after Ursolit.
Population-specific interaction notes (if applicable) None explicitly stated where the severity of a drug-drug interaction is altered in a specific patient population.
Interaction-related restrictions Substances that increase cholesterol secretion should be avoided because they may counteract the effect of Ursolit.

Interaction Classifications (High-Level)

Classification Official Regulatory Statement
Interaction severity classification Reduced Effectiveness/Exposure; Altered Exposure of Co-administered Drug.
Regulatory basis Information derived from government-approved prescribing information (FDA and EMA).
Interaction-context constraints Interaction must be managed by separation of administration timing or by avoidance of the interacting medicine.

Resulting Interaction Structure

Official Interaction Statements:

  • Bile Acid Sequestering Agents and Aluminum-based Antacids interfere with the absorption of Ursolit by binding bile acids in the intestine, officially reducing the exposure of Ursolit.
  • Co-administration of Ursolit may increase the blood concentrations of Ciclosporin by affecting its absorption from the gut.
  • Substances that increase hepatic cholesterol secretion, specifically Estrogens, Oral Contraceptives, and lipid-lowering agents, should be avoided because they counteract the therapeutic effectiveness of Ursolit.
  • Interactions with certain drugs (e.g., Nitrendipine, Dapsone) have been noted to potentially alter their concentrations.

Connection to the overall interaction profile:

The official regulatory documents define the product's interaction structure predominantly around reducing the absorption and efficacy of Ursolit by other medicinal products, requiring management through mandated timing separation or avoidance. A secondary component of the official profile identifies the potential for Ursolit to increase the systemic exposure of certain co-administered drugs, specifically noted for Ciclosporin. The majority of documented interactions are classified as clinically significant due to their direct interference with the intended pharmacological action of the medicine.

Mechanism of Action

How Ursolit Works

The mechanism of action for Ursodiol is defined by its role as a highly hydrophilic bile acid that performs three distinct, simultaneous actions involving the modulation of bile chemistry and the stabilization of cellular membranes.

Modulating Bile Composition and Solubilization

Ursodiol fundamentally alters the chemical composition of the bile acid pool. It acts by displacing toxic hydrophobic bile acids and inhibiting both the intestinal absorption of cholesterol and its secretion from the liver. This cascade results in a reduction of the cholesterol saturation of bile, creating a chemical environment that favors the physicochemical transition of cholesterol from solid to soluble phase.

Direct Cellular Stabilization (Cytoprotection)

The drug provides direct cellular stabilization by incorporating itself into the membranes of hepatocytes and cholangiocytes. This action physically stabilizes the mitochondrial membrane, effectively inhibiting the intrinsic apoptotic pathway that can be triggered by toxic bile acid buildup. This mechanism limits the cell-damaging effects of hydrophobic bile acids, influencing the structural stability of hepatic and biliary cells.

Enhancing Biliary Secretion (Choleretic Action)

Ursodiol engages in a choleretic action by actively upregulating specific membrane transport proteins on liver cells, such as the Chloride-Bicarbonate Anion Exchanger (AE2). This enhances the secretion of water and bicarbonate into the bile, resulting in an increased volume and fluidity of bile. This physiological change produces an increased hydrostatic effect and bile flow, which facilitates the transport of accumulated bile acids and debris out of the ducts.

Dosage and Administration Information

Official Administration Guidelines

Ursolit is administered by the oral route as a capsule, tablet, or suspension. The administration protocol is weight-dependent; the total daily dose is calculated based on body weight and is typically divided into multiple administrations taken throughout the day.

Dosage ranges vary by the intended use. For Primary Biliary Cholangitis (PBC), the established regimen is 13–15 mg/kg per day. The typical regimen for the dissolution of cholesterol gallstones is 8–10 mg/kg per day. All scheduled doses are generally administered with food. While 500 mg tablets may be scored for flexible dosing, they are intended to be swallowed whole with water and not chewed.

The duration of use depends on the condition. For gallstone dissolution, use may span up to two years and is often continued for an additional three months after the stones are confirmed to be removed. For chronic conditions such as PBC, the protocol includes routine monitoring of serum liver enzymes at scheduled intervals. Weight-based dosing rules for pediatric patients are also established for specific indications.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Ursolit

Evidence for Use in Primary Biliary Cholangitis (PBC)

This section will summarize the core research base for Ursodiol in PBC, detailing the types of randomized controlled trials (RCTs) and observational studies that exist and what key clinical and biochemical markers they were designed to measure.

Ursodiol was studied for its use in managing Primary Biliary Cholangitis (PBC), a long-term liver condition. Research has explored this use through multiple study designs, including randomized controlled trials (RCTs) and long-term observational studies were also conducted to monitor patient patterns. Researchers examined outcomes related to systemic or functional imbalance, such as changes in liver enzyme levels like Alkaline Phosphatase (ALP) and bilirubin. They also monitored whether treatment was associated with a delay in disease progression or the need for a liver transplant. Studies explored how symptoms evolved in the observed populations, particularly for pruritus (itching).

Research describes patterns where individuals who received Ursodiol exhibited alterations in these biochemical markers when compared to those who received a placebo. Studies monitored the elapsed time before patients reached certain long-term clinical events, and described patterns of observed change, although not all studies reported identical patterns.

Evidence for Use in Cholesterol Gallstone Management

This section will review the evidence regarding the use of Ursodiol for the dissolution and prevention of specific types of gallstones, focusing on the outcomes examined in controlled trials, such as rates of stone disappearance and recurrence.

Ursodiol was evaluated in controlled trials for two distinct purposes: dissolving existing non-calcified cholesterol gallstones and preventing new ones from forming. Research examined outcomes reflecting the physical disappearance of the stones, verified by follow-up imaging, and the incidence of new stone formation in high-risk groups. Research describes patterns of reduced frequency of new stone formation in these at-risk populations. The studies conducted in this area apply only to the populations studied—specifically, those with cholesterol gallstones that are not calcified.

Gaps in Evidence and Areas of Uncertainty

The reliance on surrogate endpoints in some trials means long-term effects are not fully established regarding ultimate survival for all subgroups. Furthermore, studies monitored recurrence rates, which suggest gallstones may re-form after treatment is discontinued. The core research limitation is that studies focused only on one specific type of gallstone (non-calcified cholesterol). Overall, the evidence quality varies across studies, and research is ongoing to further clarify long-term outcomes.

Key Studies & References

  1. Ursodeoxycholic Acid: LiverTox Clinical and Research Information

Frequently Asked Questions (FAQ)

Common questions about Ursolit (FAQ)

Q: Is Ursolit safe to use during pregnancy?

A: Official documents describe that use is generally not recommended unless a healthcare professional considers it clearly necessary. Animal studies have shown potential risks to the developing fetus. Regulatory information notes that women of childbearing potential taking the medicine for gallstone dissolution are required to use effective non-hormonal contraception.

Q: Can Ursolit be used while breastfeeding?

A: Official guidance states that use during lactation is generally not recommended, and regulatory documents describe that caution is typically applied in such situations. Research examining the composition of breast milk suggests that the amount of the active substance transferred to the infant is considered very small.

Q: Does Ursolit interact with birth control pills?

A: Official interaction information states that Oral Contraceptives containing estrogen may counteract the intended therapeutic effect of the medicine. This happens because these hormonal substances can increase the secretion of cholesterol from the liver.

Q: Are there any specific supplements or vitamins that should be avoided with Ursolit?

A: The official regulatory interaction map identifies specific classes of medications, such as certain antacids and cholesterol-lowering agents, that should be avoided. Regulatory information notes that all supplements, vitamins, and over-the-counter products are intended to be discussed with a healthcare provider.

Q: What does official guidance say about taking Ursolit with grapefruit?

A: Official regulatory documents do not contain a specific warning or statement regarding an interaction between this medicine and grapefruit or grapefruit juice.

Q: Are there any foods or drinks that make Ursolit less effective?

A: Official information states that the medicine should be taken with food but does not list any specific everyday foods or common beverages that interfere with its effectiveness. The primary known substances that interfere are certain medications, such as binding agents.

Q: What are the major research themes discussed in regulatory documents for Ursolit?

A: Research reviewed in regulatory documentation focuses primarily on two major themes. One theme is monitoring biochemical markers and observing clinical outcomes for its use in Primary Biliary Cholangitis (PBC). The second theme evaluates the physical dissolution and prevention of non-calcified cholesterol gallstones.

Q: Why do some people need to take Ursolit for a long time?

A: The required duration of use is strictly defined by the condition being addressed. For the dissolution of gallstones, use may be required for up to two years, continuing for a period after the stones are confirmed to be removed. For conditions like Primary Biliary Cholangitis (PBC), the treatment protocol is defined as long-term or chronic use.

Q: Can Ursolit be crushed or split?

A: Official instructions describe that the medicine is intended to be swallowed whole with water and is not intended to be chewed. While some tablets are scored for flexible dosing, the patient information leaflet provides specific instructions on the handling and storage of split tablets.

Q: Is Ursolit used to treat conditions other than what is listed?

A: Regulatory approval for the medicine is currently established for specific conditions, notably Primary Biliary Cholangitis (PBC) and the dissolution/prevention of non-calcified cholesterol gallstones. Any discussion of other uses falls outside of the authorized product information reviewed by regulatory agencies.

Q: Will Ursolit change the way I feel right away?

A: The desired therapeutic effect of the medicine, such as the dissolution of gallstones, is not immediate. Official pharmacology information describes the initial response for gallstone dissolution occurring over a period of 3 to 6 months of continuous treatment.

Q: How long does it usually take to notice any changes after starting Ursolit?

A: The desired therapeutic effect of the medicine, such as the dissolution of gallstones, is not immediate. Official pharmacology information describes the initial response for gallstone dissolution occurring over a period of 3 to 6 months of continuous treatment.

Q: Is Ursolit a type of steroid?

A: The medicine is chemically classified as a bile acid, which is a naturally occurring compound that is synthesized for pharmaceutical use. Pharmacologically, it is classified as a cholelitholytic agent and hepatoprotective agent, and is not classified as a steroid medicine.

Q: Does Ursolit affect hormone levels?

A: Official interaction information notes that substances containing Estrogens (such as certain oral contraceptives) should be avoided because they may interfere with the medicine’s effectiveness. This is due to these hormones increasing the secretion of cholesterol from the liver.

Q: Is it normal to feel tired when first taking Ursolit?

A: Fatigue (tiredness) has been reported in the adverse reactions section of clinical studies. However, the reported rate was similar to or lower than the rate observed in patients taking a placebo.

Q: Can I drink alcohol while taking Ursolit?

A: Regulatory safety information advises against the consumption of alcohol while taking the medicine. This is because alcohol may increase the risk of certain side effects, such as drowsiness, and potential liver effects.

Q: Does Ursolit interact with common over-the-counter pain relievers?

A: Official interaction documentation mentions that co-administration with Acetylsalicylic acid (a common pain reliever) may increase the risk or severity of adverse effects. Regulatory information notes that all over-the-counter medicines are intended to be discussed with a healthcare provider.

Q: Is Ursolit suitable for people with kidney problems?

A: Regulatory documents indicate that caution is generally applied when the medicine is used in people with existing kidney impairment. Regulatory information notes that a dose adjustment may be required in such cases.

Q: Can Ursolit be used by children?

A: The safety and effectiveness of the medicine for its primary approved uses (gallstone dissolution and PBC) have not been established in children. However, regulatory documents confirm its use is established for children aged 6–18 years for a specific condition (cystic fibrosis-related hepatobiliary disorders).

Q: What happens if I miss a dose of Ursolit?

A: Patient information leaflets state that specific guidance for a missed dose is typically provided by a healthcare professional or pharmacist, as instructions may vary based on the prescribed regimen.

Q: What should I do if I experience an allergic reaction to Ursolit?

A: Official regulatory patient information describes that in the event of an allergic reaction, the medicine is intended to be immediately stopped and urgent medical attention should be sought, such as by contacting a healthcare professional or visiting an emergency department.

Q: How does Ursolit affect cholesterol levels?

A: The medicine affects cholesterol levels by reducing the secretion of cholesterol from the liver and by decreasing its intestinal absorption. This action ultimately helps lower the saturation of cholesterol in the bile.

Q: Is there a generic version of Ursolit available?

A: The active ingredient, ursodiol (ursodeoxycholic acid), is available in both the branded form and as a generic medicine.

Q: Can Ursolit affect my sleep?

A: Insomnia (difficulty sleeping) has been reported as an adverse reaction in clinical studies documented in regulatory product information.

Q: What is the recommended storage temperature for Ursolit?

A: The product should be stored at a Controlled Room Temperature, defined in regulatory documents as 20 C to 25 C (68 F to 77 F). It must also be protected from freezing, excessive heat, light, and moisture.

Q: Do any official drug documents mention the possibility of hair loss with Ursolit?

A: Yes, official product information documents list alopecia (hair loss) as one of the documented adverse reactions that have been reported.

Q: Can Ursolit cause dry mouth?

A: Dry mouth is not generally reported or listed among the common adverse reactions documented in official product information.

Q: Is it normal to feel a bit dizzy after starting Ursolit?

A: Dizziness has been reported in clinical studies and is included in the list of adverse reactions described in official product information.

Q: Does Ursolit affect fertility in men or women?

A: Official regulatory information requires women of childbearing potential to use effective non-hormonal contraception while taking the medicine for gallstone dissolution. The effects of the medicine on fertility are not fully established in human studies.

Q: What is the purpose of the different strengths of Ursolit available?

A: Different strengths of the medicine are available to allow for accurate and flexible dosing. The required daily dose is often calculated based on the patient's body weight and varies depending on the specific condition being addressed.

Q: Is Ursolit considered a controlled substance?

A: The medicine is classified as a Bile Acid and a Cholelitholytic agent and is not designated as a controlled substance by the US Drug Enforcement Administration (DEA) or similar regulatory bodies.

Q: Can Ursolit be taken with herbal teas?

A: Official regulatory documents do not contain specific warnings or statements regarding interactions with herbal teas. However, all herbal products and supplements are intended to be discussed with a healthcare provider.

How should Ursolit be stored and disposed of?

Storage and Disposal of Ursolit

Ursolit (Ursodiol) must be stored strictly according to official regulatory conditions to maintain product integrity.

Storage Conditions

  • Temperature: Store at Controlled Room Temperature, defined as 20 C to 25 C (68 F to 77 F). The product must be kept from freezing and excessive heat.
  • Protection: Keep the medicine in its original, closed container, and protect it from light and moisture.
  • Stability: If a scored tablet is broken, the resulting half-tablets have a limited shelf-life of up to 28 days when stored in the bottle.
  • Child Safety: The medication must be kept out of the sight and reach of children.

️ Disposal Instructions

Do not keep outdated or unused medicine. Patients must ask a healthcare professional how any unused medicine should be disposed of before discarding it. Ursodiol is not on the list of medicines recommended for flushing.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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