Febuxostat

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[edit] BRAND NAMES

[edit] STRUCTURE

Febuxostat.jpg

[edit] MECHANISM OF ACTION

Uric acid is the end product of purine metabolism in humans and is generated in the cascade of hypoxanthine → xanthine → uric acid. Both steps in the above transformations are catalyzed by xanthine oxidase (XO). Hyperuricaemia (greater than 7 mg/dL) can lead to urate crystals forming and building up in the joints and the kidneys. When this happens in the joints and causes pain, it is known as gout.

Febuxostat is a potent, non-purine selective inhibitor of xanthine oxidase (XO). It achieves its therapeutic effect by decreasing serum uric acid and stopping crystals from building up. This can reduce the symptoms of gout. Keeping uric-acid levels low for long enough can also shrink tophi (‘stones’, larger deposits of urate crystals that can cause joint and bone damage)

Febuxostat was more effective than Allopurinol in reducing blood uric-acid levels. In a study, 48% of the patients taking 80 mg Febuxostat once a day and 65% of the patients taking 120 mg once a day had levels of uric acid below 6 mg/dl in the final three measurements. This was compared with 22% of the patients taking allopurinol.

[edit] INDICATIONS

  • Chronic management of hyperuricemia in patients with gout.
    Febuxostat is used in patients who already have signs of a build-up of crystals, including arthritis (pain and inflammation in the joints) or tophi (‘stones’, larger deposits of urate crystals that can cause joint and bone damage)

[edit] DOSAGE

Febuxostat is recommended at 40 mg-80 mg once daily, without regard to food.

After initiation of Febuxostat, an increase in gout flares is frequently observed. This increase is due to reduction in serum uric acid levels, resulting in mobilization of urate from tissue deposits. In order to prevent gout flares, concurrent prophylactic treatment with an NSAID or colchicine is recommended for at least the first six months of treatment. Febuxostat treatment should not be stopped if an attack of gout occurs

[edit] DOSAGE FORMS AND STRENGTHS

  • US: Tablets 40 mg, 80 mg
  • Europe: Tablets 80 mg, 120 mg

[edit] CONTRAINDICATIONS

  • Patients concomitantly treated with mercaptopurine or azathioprine. (Inhibition of XO by febuxostat may cause increased plasma concentrations of these drugs leading to toxicity)

[edit] WARNINGS AND PRECAUTIONS

Cardiovascular Events: A higher rate of cardiovascular thromboembolic events was observed in patients treated with Febuxostat than allopurinol in clinical trials. Monitor for signs and symptoms of myocardial infarction and stroke

[edit] INTERACTIONS

Concomitant administration of Febuxostat with XO substrate drugs, azathioprine or mercaptopurine could increase plasma concentrations of these drugs resulting in severe toxicity.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). There are no adequate and well-controlled studies in pregnant women, therefore, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: Febuxostat is excreted in the milk of rats. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Febuxostat is administered to a nursing woman.

[edit] SIDE EFFECTS

The most commonly reported side effects with Febuxostat are gout flare-ups, abnormal liver test results, diarrhea, nausea, headache, arthralgia, rash and edema (swelling). These side effects were mostly mild or moderate in severity. Rare serious hypersensitivity allergic reactions have occurred post-marketing

[edit] RELATED LINKS

Gout: Diet, Symptoms and Medication

[edit] BIBLIOGRAPHY

[edit] REFERENCES