Generic Ursodiol

Introduction

Ursodiol is a bile-acid medication used primarily to dissolve cholesterol gallstones and to treat certain cholestatic liver disorders. It is supplied as oral tablets in strengths of 150 mg and 300 mg. Ursodiol belongs to the class of hydrophilic bile acids and is marketed under brand names such as Actigall and Urso. The drug’s therapeutic effects are based on its ability to modify the composition of bile, reducing cholesterol saturation and protecting liver cells from toxic bile acids. Off-label applications have been explored in conditions such as primary sclerosing cholangitis, but these uses are not approved by the FDA or EMA.

What is Ursodiol?

Ursodiol (also called ursodeoxycholic acid) is the generic formulation of a naturally occurring bile acid originally isolated from the bile of the Chinese black bear. It was later synthesized for pharmaceutical use and introduced in the United States in the early s. The medication is produced by several licensed manufacturers; common commercial preparations include Actigall (Allergan) and Urso (Vifor Pharma). Ursodiol tablets are available in 150 mg and 300 mg strengths for oral administration.

How Ursodiol Works

Ursodiol is a hydrophilic bile acid that competes with more hydrophobic, potentially toxic bile acids. By replacing these aggressive acids, it lowers the overall cholesterol concentration in bile, making the environment less likely to precipitate cholesterol crystals that form gallstones. In the liver, ursodiol stabilizes hepatocyte membranes and reduces the cytotoxic effect of accumulated bile acids, thereby improving cholestasis. The drug reaches peak plasma concentrations within 2-3 hours after an oral dose and is largely eliminated unchanged in the feces after hepatic uptake and biliary excretion.

Conditions Treated with Ursodiol

• Cholesterol Gallstone Dissolution - Ursodiol is indicated for patients with radiolucent, cholesterol-rich gallstones who are not candidates for surgery. It gradually reduces stone size, allowing natural passage.
• Primary Biliary Cholangitis (PBC) - The medication improves liver enzyme profiles and can delay disease progression in PBC, a chronic autoimmune cholestatic disorder.
• Intrahepatic Cholestasis of Pregnancy (ICP) - Ursodiol relieves pruritus and lowers serum bile acid levels, improving maternal comfort and reducing fetal risk in ICP.

The drug’s efficacy in these approved indications stems from its ability to alter bile composition, protect hepatocytes, and facilitate stone dissolution.

Off-Label and Investigational Uses of Ursodiol

• Primary Sclerosing Cholangitis (PSC): Small-scale studies suggest ursodiol may improve liver biochemistry, but larger trials have not confirmed a clear clinical benefit. It remains an off-label option that should only be considered under specialist supervision.
• Non-Alcoholic Fatty Liver Disease (NAFLD): Early research indicates ursodiol could reduce hepatic inflammation, yet definitive evidence is lacking.
• Cystic Fibrosis-Related Liver Disease: Some clinicians use ursodiol to manage cholestasis in cystic fibrosis, based on its hepatoprotective properties, but it is not an approved indication.

All off-label uses are not authorized by regulatory agencies. Patients should discuss potential risks and benefits with a qualified healthcare provider before initiating such therapy.

Is Ursodiol the Right Medication for You?

Ursodiol is most appropriate for adults who:

• Have documented cholesterol gallstones and are unsuitable for cholecystectomy.
• Have a confirmed diagnosis of primary biliary cholangitis.
• Experience intrahepatic cholestasis during pregnancy with elevated serum bile acids.

Contraindications include:

• Known hypersensitivity to ursodiol or any tablet excipients.
• Complete biliary obstruction (e.g., obstructive jaundice) where the drug cannot reach the bile ducts.

Patients with severe liver impairment or those taking certain medications that interfere with bile acid metabolism should be evaluated carefully before starting therapy.

Risks, Side Effects, and Interactions

Common

• Diarrhea - Usually mild and transient.
• Nausea or abdominal discomfort - Often improves with food.
• Flatulence - Can be managed by taking the tablet with meals.

Rare

• Skin rash or urticaria - May indicate an allergic response; discontinue if persistent.
• Elevated serum transaminases - Requires monitoring of liver function tests.

Serious

• Hepatic decompensation - Rare but reported in patients with advanced liver disease; immediate medical evaluation is essential.
• Severe hypersensitivity reactions - Anaphylaxis is extremely uncommon but possible.

Drug-Drug Interactions

• Anticholestatic agents (e.g., cholestyramine): May reduce ursodiol absorption; separate administration by at least 2 hours.
• Cyclosporine: Ursodiol can increase cyclosporine blood levels; monitor therapeutic concentrations.
• Oral contraceptives and hormone replacement therapy: No major interaction, but clinicians may monitor liver enzymes.

Drug-Food Interactions

• Ursodiol is best taken with a meal or a snack to enhance absorption and reduce gastrointestinal upset. High-fat meals do not significantly alter its bioavailability.

Use: Dosing, Missed Dose, Overdose

• Standard dosing for gallstone dissolution: 8-10 mg/kg/day divided into two doses; typical adult regimens use two 300 mg tablets daily.
• Primary biliary cholangitis: Starting dose of 13-15 mg/kg/day, often three tablets of 300 mg split throughout the day.
• Intrahepatic cholestasis of pregnancy: 10-15 mg/kg/day in divided doses; safety data support continuation throughout pregnancy.

Missed dose: Take the missed tablet as soon as remembered unless it is near the time of the next scheduled dose; do not double the dose.

Overdose: Symptoms may include severe diarrhea and abdominal cramps. If an overdose is suspected, seek immediate medical assistance; supportive care is the mainstay of treatment.

Practical precautions:

• Swallow tablets whole with water; do not crush or chew.
• Avoid excessive alcohol while on therapy, as it can worsen liver injury.
• Caution when operating machinery until individual tolerance to possible gastrointestinal effects is known.

FAQ

• How should I store Ursodiol tablets? Store at room temperature, away from moisture and direct sunlight. Do not refrigerate or freeze; keep the bottle tightly closed.

• Can I travel internationally with Ursodiol? Yes, but carry the medication in its original labeled container and bring a copy of the prescription or a physician’s letter if required by customs.

• What inactive ingredients are in the 300 mg tablets? Common excipients include microcrystalline cellulose, lactose monohydrate, magnesium stearate, and silicon dioxide. Patients with lactose intolerance should verify with the manufacturer.

• Is Ursodiol safe for people with a gluten allergy? The tablets are formulated without gluten-containing ingredients, but patients with celiac disease should confirm the source batch.

• Does taking Ursodiol affect laboratory tests? Ursodiol can modestly lower serum cholesterol and bilirubin levels, potentially altering liver function panels. Inform the laboratory if you are on therapy.

• Can I take Ursodiol while breastfeeding? Limited data exist; the drug does appear in breast milk in small amounts. Discuss risks and benefits with a qualified health professional before use.

• Why does my doctor recommend a split dose rather than a single daily dose? Dividing the dose maintains steadier bile-acid concentrations throughout the day, improving efficacy and reducing gastrointestinal side effects.

• What is the difference between Ursodiol and other bile-acid drugs like chenodiol? Ursodiol is hydrophilic and hepatoprotective, whereas chenodiol (chenodeoxycholic acid) is more hydrophobic and can be hepatotoxic at higher doses.

• Will Ursodiol interact with over-the-counter supplements such as milk thistle? No well-documented interaction exists, but both affect liver metabolism; monitor liver function if used together.

• How long does it typically take to dissolve gallstones with Ursodiol? Therapeutic response varies; many patients experience stone reduction within 6-12 months, with complete dissolution possible after 18-24 months of continuous therapy.

Glossary

Hydrophilic bile acid

A water-soluble bile acid that reduces the toxicity of bile by diluting more hydrophobic, damaging acids.

Cholestasis

A condition where bile flow from the liver is impaired, leading to accumulation of bile acids in the bloodstream.

Radiolucent gallstones

Gallstones composed mainly of cholesterol that appear dark on X-ray imaging, making them amenable to dissolution therapy.

Hepatoprotection

The process of preventing damage to liver cells, often by reducing oxidative stress or toxic bile-acid exposure.

Buying Ursodiol from Our Online Pharmacy

Ursodiol can be obtained conveniently through our online pharmacy. By sourcing directly from licensed international suppliers, we provide a cost-effective alternative that often aligns closely with manufacturer pricing. Every batch is verified for authenticity and quality, ensuring that you receive a medication that meets stringent regulatory standards.

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Choosing our online pharmacy means you benefit from reliable, affordable access without compromising safety or confidentiality.

Disclaimer

The details presented about Ursodiol are intended for informational purposes only and do not replace professional medical advice. Treatment choices, including any off-label applications, should be made under the guidance of a qualified health professional. Readers are presumed to be responsible adults capable of making informed health decisions. Our online pharmacy supplies Ursodiol to individuals who may face limited availability through conventional pharmacies or insurance programs, or who seek a cost-effective generic option. Always discuss any medication changes with your health care provider before initiating, modifying, or stopping therapy.