Skip to content

What is the drug febuxostat used for? A comprehensive guide to its purpose and risks

4 min read

In 2019, the U.S. Food and Drug Administration (FDA) issued a Boxed Warning for the drug febuxostat due to an increased risk of heart-related death compared to allopurinol in patients with known cardiovascular disease. This medication is specifically indicated for the long-term management of chronic hyperuricemia in adults with gout.

Quick Summary

Febuxostat is a medication used to lower high blood uric acid levels in adults with gout, particularly when allopurinol has failed or is not tolerated. It works by inhibiting the enzyme xanthine oxidase, but carries a Boxed Warning for increased cardiovascular risk.

Key Points

  • Chronic Gout Management: Febuxostat is a medication prescribed for the long-term treatment of hyperuricemia in adult patients with gout.

  • Second-Line Treatment: It is typically used as an alternative for patients who cannot tolerate or have not adequately responded to allopurinol.

  • Mechanism of Action: The drug inhibits the enzyme xanthine oxidase to reduce the body's production of uric acid, which helps prevent future gout attacks.

  • Cardiovascular Risk Warning: The FDA has issued a Boxed Warning highlighting an increased risk of heart-related death associated with febuxostat compared to allopurinol.

  • Prophylaxis for Flares: An increase in gout flares can occur when treatment is initiated, so doctors often prescribe a separate anti-inflammatory medication to be taken concurrently.

  • Not for Acute Attacks: Febuxostat is not intended for treating active gout attacks; it is a preventative therapy.

In This Article

What is Febuxostat?

Febuxostat, sold under the brand name Uloric, is a prescription medication belonging to a class of drugs known as xanthine oxidase inhibitors (XOIs). Its primary function is to reduce the amount of uric acid produced in the body, addressing the root cause of gout and its related complications.

The mechanism behind the medication

To understand what febuxostat is used for, it is essential to know its mechanism of action. Febuxostat works by inhibiting xanthine oxidase, an enzyme that plays a critical role in the purine metabolism pathway. This pathway converts purines from food and cellular turnover into uric acid. By blocking this enzyme, febuxostat decreases the production of uric acid, helping to lower blood levels and prevent the formation of urate crystals that cause gout flares.

The Primary Purpose: Treating Gout

Febuxostat is approved for the chronic management of hyperuricemia (abnormally high uric acid levels) in adults who have gout. This makes it a key part of long-term gout management, aiming to keep uric acid levels consistently low to prevent future joint damage and gout attacks. It is important to note that febuxostat is not used for treating an acute, ongoing gout attack, as it can initially worsen symptoms.

Febuxostat is a second-line therapy

Due to concerns over cardiovascular risks, febuxostat is not a first-choice treatment for most patients. The FDA recommends it only for those who have not been treated effectively with a maximally titrated dose of allopurinol or who cannot tolerate allopurinol due to severe side effects.

Febuxostat vs. Allopurinol: A Comparative Look

For many years, allopurinol was the only option in its class for long-term gout management. Febuxostat offers an alternative, but there are key differences, most notably regarding cardiovascular safety and efficacy. Healthcare providers must consider a patient's individual health profile when deciding between the two medications.

Feature Febuxostat Allopurinol
Drug Class Xanthine Oxidase Inhibitor Xanthine Oxidase Inhibitor
First/Second-Line Second-line, reserved for specific patients due to cardiovascular risk. First-line, most commonly prescribed urate-lowering therapy.
Cardiovascular Risk Carries a Boxed Warning for increased heart-related death compared to allopurinol in patients with heart disease. Generally considered safer regarding cardiovascular risk for most patients.
Effectiveness May be more effective at lowering uric acid levels in some patients, especially at higher doses. Effective, but dose may need to be titrated slowly, especially in those with kidney problems.
Use in Kidney Impairment Safe for use with mild to moderate kidney problems without dose adjustment. Dosing requires careful adjustment based on kidney function.
Hypersensitivity Less risk of severe skin reactions compared to allopurinol, which is beneficial for those with prior intolerance. Associated with a small risk of severe, potentially fatal, skin reactions in some patients.

Administration

Febuxostat is an oral tablet typically taken once daily, with or without food. The dosage is determined by a healthcare professional and is based on the patient's individual needs and response to treatment. Regular monitoring of uric acid levels is necessary to determine the drug's effectiveness and whether adjustments are needed.

Important Safety Considerations and Precautions

  • Cardiovascular Health: Individuals with a history of heart attack, stroke, or other heart diseases should discuss the risks with their doctor. Symptoms such as chest pain, shortness of breath, or irregular heartbeat warrant immediate medical attention.
  • Initial Gout Flares: Paradoxically, starting a urate-lowering medication like febuxostat can temporarily increase gout flare-ups as the body adjusts. Physicians often prescribe a prophylactic medication, such as colchicine or an NSAID, during the first few months of treatment to manage this.
  • Drug Interactions: Febuxostat should not be taken with certain other medications, including azathioprine and mercaptopurine, as it can dangerously increase their levels in the blood. It is crucial to inform your doctor about all other medicines and supplements you are taking.
  • Liver Function: Regular liver function tests are recommended, as febuxostat can cause abnormalities in liver enzyme levels in some patients. Seek medical care if you experience symptoms of liver issues, such as yellowing skin or dark urine.

Side Effects of Febuxostat

Like all medications, febuxostat can cause side effects. Some of the most common include:

  • Nausea and joint pain
  • Rash and other allergic reactions
  • Abnormal liver function tests
  • Diarrhea

More serious side effects are less common but can include life-threatening conditions like severe skin reactions (e.g., Stevens-Johnson syndrome) and allergic responses with facial or throat swelling. Any severe reaction requires immediate medical attention.

Conclusion

In summary, the drug febuxostat is used for the chronic management of hyperuricemia in adults with gout, serving as a second-line therapy when the standard treatment, allopurinol, is not suitable. It effectively lowers uric acid levels by inhibiting the enzyme xanthine oxidase, which helps prevent future gout attacks and associated complications. However, its use is limited by a Boxed Warning regarding an increased risk of cardiovascular-related death. Patients starting this treatment should be aware of the risk of initial gout flares and should receive appropriate prophylaxis. With careful consideration of a patient's cardiovascular history and proper medical guidance, febuxostat remains a valuable option for many individuals struggling with chronic gout.

For more detailed prescribing information and FDA guidance, visit the FDA's official page on Uloric.

Frequently Asked Questions

Febuxostat starts lowering uric acid levels in the blood within a few hours of taking the first dose. However, it may take several months of continuous treatment to reduce the frequency of gout flares.

No, febuxostat should not be used to treat an acute gout attack. For managing a flare, your doctor may recommend a different medication, such as an NSAID or colchicine.

Both are xanthine oxidase inhibitors used for gout, but febuxostat is generally considered a second-line therapy due to an increased risk of heart-related death compared to allopurinol. Febuxostat may be preferred for those intolerant to allopurinol or with certain kidney issues.

Common side effects can include nausea, joint pain, rash, and diarrhea. Abnormal liver test results are also possible, so regular monitoring is advised.

Patients with a history of heart disease, stroke, or other serious heart problems should use febuxostat with caution or avoid it. It is also contraindicated for patients taking azathioprine or mercaptopurine.

The appropriate dosage for febuxostat is determined by a healthcare professional based on the individual patient's medical condition and response to treatment. It is crucial to follow their specific instructions regarding dosage.

When you first start treatment, the rapid decrease in uric acid levels can cause urate crystals to shift within your joints, which can trigger more frequent gout attacks. Your doctor will likely prescribe another medication to prevent this during the initial months.

References

  1. 1
  2. 2
  3. 3
  4. 4
  5. 5
  6. 6
  7. 7
  8. 8
  9. 9

Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.