Product Details

FEBUXOSTAT

Class:

• Antigout
• Xanthine Oxidase Inhibitor

Mechanism of Action:

Febuxostat is a xanthine oxidase inhibitor which acts by decreasing serum uric acid.

Pharmacokinetics:

Absorption:

• Bioavailability,oral: 75% to 85%
• Effect of food: Cmax decreased by 49% and AUC decrease by 19%; may be taken without regard to food.

Distribution:

• Protein binding, albumin, primarily: 98% to 99%
• Vd: 41 to 50L

Metabolism:

• Hepatic: Extensive
• Active metabolites: Hydroxy febuxostat metabolites

Excretion:

• Fecal; 45%, 12% unchanged
• Renal: 49%, 3% unchanged

Elimination Half Life: 5 to 9.4 hours

FAD Indiaction:

Gout - Hyperuricemia

• Inital, 40mg orally once daily; may be increased to 80mg once daily if serum uric acid levels of less than 6mg/dl are not achieved after 2 weeks.

Non-FAD Indication:

• Increased uric acid level, in patients receiving chemotherapy and at intermediate to high risk of tumor lysis syndrome; Prophylaxis.
• 120mg orally once daily for 7 to 9 days, starting 2 days prior to chemotherapy with adequate or increased hydration upto 3L/m/day.

Contraindication:

• Concomitant use of azathioprine or mercaptopurine

Adverse Effects:

• Common: Nausea, Rash, Arthralgia
• Serious: Abnormal liver function, Stevens-Johnson syndrome, myocardial infraction, Cerebrovascular accident.

Clinical Teaching:

• Advise patient to report signs/symptoms of gout flares or elevated liver enzymes.
• Patient should report signs/symptoms of cardiovascular events or a stroke (eg, Chest pain, shortness of breath, or neurologic symptoms).