Febuxit is indicated for the long-term management of hyperuricemia in adults with gout. It is not recommended for individuals with asymptomatic hyperuricemia.
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Febuxostat, the active ingredient in Febuxit, is a non-purine selective xanthine oxidase (XO) inhibitor. By inhibiting XO, the enzyme responsible for converting hypoxanthine to xanthine and then to uric acid, it effectively lowers serum uric acid levels.
Importantly, Febuxostat does not interfere with other enzymes involved in purine or pyrimidine metabolism at therapeutic doses.
Treatment of Gout
Chronic Gout Management:
Start with 40 mg once daily.
If serum uric acid remains ≥6 mg/dL after 2 weeks, increase to 80 mg once daily.
If needed, escalate to 120 mg once daily after 2–4 weeks.
Tumor Lysis Syndrome (TLS):
Recommended dose: 120 mg once daily, starting 2 days before initiating chemotherapy.
Continue for at least 7 days, or up to 9 days based on the chemotherapy regimen.
Managing Gout Flares:
Flares may occur early in treatment due to shifting uric acid levels.
Use NSAIDs or colchicine for flare prevention when starting Febuxit.
Continue Febuxit during flares; manage symptoms as needed.
Special Populations:
Renal Impairment (mild–moderate): No dose adjustment needed.
Hepatic Impairment (mild–moderate): No dose adjustment required.
Pediatrics: Not established for use in patients under 18 years of age.
Contraindicated:
Azathioprine, Mercaptopurine, Theophylline – due to the risk of severe toxicity.
Cautionary/Monitoring:
Naproxen/NSAIDs/Probenecid: May affect Febuxit metabolism via UGT inhibition.
UGT Inducers: Can reduce Febuxit efficacy – monitor uric acid levels.
Rosiglitazone (CYP2C8 substrates): No dose change needed.
Antacids: May delay absorption, but do not reduce overall exposure.
Safe Co-administration (No dose adjustment needed):
Common side effects include:
Gout flares, liver enzyme elevation, nausea, diarrhea, headache, rash, and edema
Rare cases of serious allergic reactions have been reported.
Pregnancy Category C: Use only if the potential benefit justifies the potential risk.
Lactation: Unknown if excreted in human milk – use caution in nursing women.
Gout Flares: Expected during early therapy; continue Febuxit and treat flares as appropriate.
Cardiovascular Risk: Slightly higher rates of thromboembolic events (e.g., MI, stroke) noted in studies – monitor closely.
Liver Monitoring: Periodically assess liver function during treatment.
Hypersensitivity to Febuxostat
Concurrent use of azathioprine, mercaptopurine, or theophylline
Store below 30°C, protected from light and moisture.
Keep out of reach of children.
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