Ursodiol Medications

Ursodiol is a bile acid used to treat gallstones by reducing cholesterol in bile and to manage liver diseases like primary biliary cholangitis.

Urso

Ursodiol

$1.07 per pill

150 | 300mg

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What is Ursodiol

Ursodiol (ursodeoxycholic acid) is a naturally occurring bile acid used primarily to treat disorders of bile flow. In Australia it is listed on the Therapeutic Goods Administration (TGA) register for primary biliary cholangitis (PBC) and for the non-surgical dissolution of cholesterol gallstones. The compound belongs to the class of hepatoprotective bile acids that modify the composition of the bile pool and improve cholestasis. By influencing cholesterol metabolism and protecting cholangiocytes from toxic bile acids, ursodiol reduces liver enzyme elevations and promotes the gradual clearance of small gallstones. Generic formulations are widely available, while branded products such as Urso, Ursodiol-USP and Actigall are sold in many markets. Off-label, clinicians sometimes prescribe ursodiol for primary sclerosing cholangitis, non-alcoholic fatty liver disease (NAFLD) or for liver dysfunction related to certain medications, although these uses lack formal regulatory endorsement.

What is Ursodiol?

Ursodiol is a secondary bile acid derived from the bear bile of Ursus species and now produced synthetically for medical use. It is classified as a hepatoprotective and cholagogue agent. The TGA approved ursodiol in 1995 for primary biliary cholangitis, and the FDA granted approval in 1993 for the same indication and for gallstone dissolution. Subsequent label updates in the United States and Europe added recommendations for use in intra-hepatic cholestasis of pregnancy (off-label in Australia).

At the molecular level, ursodiol replaces more hydrophobic, potentially toxic bile acids in the enterohepatic circulation. This substitution lowers the overall cytotoxicity of bile, reduces hepatic inflammation, and stimulates the secretion of bile fluid. The drug is marketed under several brand names-including Urso and Ursodiol-USP-and is also offered as inexpensive generic tablets that can be purchased through our online pharmacy.

How Ursodiol Works

Mechanism of Action

Ursodiol exerts its effect by several coordinated actions: it reduces the synthesis of cholesterol in hepatocytes, promotes the conversion of cholesterol to bile acids, and alters the bile acid pool to favor less toxic, more hydrophilic species. The result is a decrease in the formation of cholesterol-rich gallstones and a protective environment for cholangiocytes.

Therapeutic Effects

By lowering intra-hepatic bile acid concentrations, ursodiol alleviates cholestasis, leading to reductions in serum alkaline phosphatase and bilirubin levels in patients with PBC. In gallstone disease, the drug gradually dissolves stones smaller than 10 mm, often in conjunction with a low-fat diet and bile-acid-binding resins.

Onset and Duration

Clinical trials show that biochemical improvement in PBC can be detected within 12 weeks of daily dosing, while gallstone dissolution may require 6-12 months of continuous therapy. Ursodiol’s half-life is approximately 3-5 hours, and steady-state concentrations are achieved after about five days of regular dosing.

Approved Uses and Applications

Approved Indications

Primary biliary cholangitis (PBC): Recommended by the TGA and the American Association for the Study of Liver Diseases for adults with early-stage disease.
Cholesterol gallstone dissolution: Indicated for patients with radiolucent stones ≤ 10 mm when surgical removal is contraindicated or declined.

Both indications rely on evidence from randomized controlled trials published in The New England Journal of Medicine and Lancet that demonstrated statistically significant reductions in disease progression markers and stone size, respectively.

Off-Label Uses

Primary sclerosing cholangitis (PSC): Small cohort studies suggest modest biochemical benefit, but regulatory agencies have not approved it for PSC.
Non-alcoholic fatty liver disease (NAFLD): Early phase-II trials report improved liver enzymes, yet larger trials are needed for formal endorsement.

Clinical Efficacy

In a pivotal PBC trial, 60 % of patients receiving ursodiol achieved a ≥ 40 % reduction in alkaline phosphatase after one year, compared with 15 % in the placebo arm. Gallstone dissolution studies report complete clearance in 30-50 % of treated stones after 12 months, with a low recurrence rate when lifestyle measures are maintained.

Buying Ursodiol from Our Online Pharmacy

Why Choose Our Service

Our pharmacy service bridges the gap for Australians who encounter supply shortages or high out-of-pocket costs for branded bile-acid therapies. By sourcing verified generic batches, we keep prices competitive while maintaining strict quality standards.

Brand Names and Generic Options

Urso (brand) - 300 mg tablets, priced at a premium.
Ursodiol-USP - 250 mg tablets, widely prescribed.
Actigall - 500 mg tablets, often used for gallstone protocols.

Generic versions of the same strengths are available at up to 55 % less cost, providing a budget-friendly alternative without compromising efficacy.

Quality & Safety

We partner with licensed international pharmacies that comply with WHO Good Manufacturing Practice (GMP) guidelines, ensuring each bottle meets rigorous purity and potency specifications.

Pricing & Access

Standard generic pricing starts at AUD 12 per 30-tablet pack, while branded options may exceed AUD 45. All repeat orders receive a Lifetime 10 % discount, encouraging long-term adherence for chronic conditions.

Discreet Delivery

Express shipping arrives within ≈ 7 days; standard shipping takes about 3 weeks. Packages are sealed in unmarked, padded boxes to protect privacy and prevent accidental exposure.

Dosing, Formulations & Administration

Available Formulations

Ursodiol is offered as oral tablets of 250 mg, 300 mg, and 500 mg. A liquid suspension (250 mg/5 mL) is also marketed for patients with swallowing difficulties.

Typical Dosing Ranges

PBC: Clinicians often start at 13-15 mg/kg/day, divided into two or three doses, and titrate to a maximum of 20 mg/kg/day based on liver-function monitoring.
Gallstone dissolution: The usual regimen is 10-15 mg/kg/day, taken in two divided doses for at least 6 months; treatment may extend to 12 months if stones persist.

These examples illustrate common practice; the exact dose must be individualized by a healthcare professional.

Administration Guidelines

Ursodiol can be taken with or without food, but taking it with a light meal may reduce occasional gastrointestinal upset. Patients should avoid high-fat meals immediately before dosing, as excessive fat can delay absorption. The liquid formulation should be shaken well before measurement to ensure uniform concentration.

A qualified clinician must determine the precise regimen based on the patient’s weight, liver status, and concomitant medications.

Safety Profile & Considerations

Common Side Effects

Diarrhea: Reported in 12-15 % of patients; usually mild and self-limiting.
Nausea: Occurs in roughly 10 % of users.
Abdominal discomfort: Seen in 8 % of trial participants.
Elevated liver enzymes: Transient rise in ALT/AST occurs in ≤ 5 % of cases.

These adverse events are generally dose-related and improve with continued therapy or dose adjustment.

Serious Adverse Events

Rarely, ursodiol can cause severe hepatitis, cholangitis, or hypersensitivity reactions such as rash and angioedema. Immediate medical evaluation is warranted if jaundice, unexplained fever, or swelling develops.

Contraindications

Known hypersensitivity to ursodiol or any component of the formulation.
History of severe cholestatic liver disease where bile flow is critically impaired.

Drug Interactions

CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase serum concentrations, requiring careful monitoring.
Other bile-acid agents (e.g., cholestyramine) can bind ursodiol in the gut, reducing its absorption; separate dosing times are advised.
Antifungal azoles may potentiate hepatotoxicity; liver function tests should be performed regularly.

Special Populations

Pregnancy: Limited data suggest safety, but the drug is classified as Category B in Australia; use only when benefits outweigh potential risks.
Breastfeeding: Small amounts are secreted in milk; clinicians usually recommend caution.
Elderly: Dose adjustments may be needed for reduced hepatic clearance; monitor for increased sedation or dizziness.
Renal/Hepatic impairment: Severe liver dysfunction contraindicates use; mild to moderate impairment may require lower dosing.

Frequently Asked Questions

What is the ursodiol mechanism of action? Ursodiol replaces hydrophobic bile acids with a more hydrophilic species, lowering bile toxicity, stimulating bile flow, and reducing hepatic cholesterol synthesis.
How does ursodiol differ from chenodeoxycholic acid? While both are bile acids, ursodiol is more hydrophilic and less likely to cause hepatocellular injury, making it preferable for chronic cholestatic conditions.
How long before ursodiol produces noticeable effects for primary biliary cholangitis? Biochemical improvements usually appear within 12 weeks, though full clinical benefit may take up to a year of continuous therapy.
When can I expect gallstones to dissolve with ursodiol? Small cholesterol stones often begin to shrink after 3 months; complete dissolution typically requires 6-12 months of daily dosing.
What should I do if I experience diarrhea from ursodiol? Mild diarrhea often resolves on its own; if it persists beyond two weeks or is severe, contact a healthcare provider for possible dose adjustment.
What are the most serious side effects that require immediate medical attention? Signs of severe hepatitis (jaundice, dark urine), unexplained fever, or an allergic reaction (rash, swelling) should prompt urgent evaluation.
Does taking ursodiol with food affect its absorption? Food can modestly slow absorption but does not significantly alter overall exposure; a light meal may lessen gastrointestinal discomfort.
Can I use ursodiol if I have liver disease unrelated to PBC? Off-label use in conditions like primary sclerosing cholangitis has been explored, but treatment decisions must be individualized by a specialist.
Is it safe to combine ursodiol with cholesterol-lowering medications? No major pharmacokinetic interaction has been identified, yet clinicians often monitor lipid panels to assess any additive effect.
What information should I provide my doctor when discussing ursodiol?
- Complete list of current prescription and over-the-counter medications, including supplements.
- Detailed medical history, especially any liver, gall bladder, or cholestatic disorders.
- Recent laboratory results (liver function tests, lipid profile).
- Specific symptoms you hope to address (e.g., fatigue, pruritus, gallstone pain).

Disclaimer

The information provided about ursodiol is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing ursodiol for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing ursodiol.