febuxostat hemihydrate: clinical use

Prescribing considerations

• Use cautiously and monitor regularly in pre-existing major cardiovascular disease.
• Discontinue immediately if serious hypersensitivity is suspected; never rechallenge after a serious reaction.
• Early gout flares alone are not an indication to discontinue febuxostat.
• Evidence is limited in severe renal impairment, moderate hepatic impairment and organ-transplant recipients; severe hepatic impairment has not been studied.
• Avoid use in Lesch–Nyhan syndrome because of absent clinical experience and potential urinary xanthine deposition.
• The product contains lactose.

Contraindications and cautions

• Hypersensitivity to febuxostat or any product excipient.

Monitoring

• Measure serum urate to assess biochemical response.
• Check liver function before treatment and periodically according to clinical judgement.
• Monitor patients with major cardiovascular disease regularly.
• Assess promptly for rash, mucosal lesions, facial swelling, fever or systemic hypersensitivity.
• Consider thyroid status where pre-existing thyroid dysfunction is present.

Clinical pharmacology

Febuxostat is a potent non-purine inhibitor of oxidised and reduced xanthine oxidase. It is extensively metabolised through glucuronidation and CYP-mediated oxidation, with hepatic and renal elimination.

Formulation and product differences

• The selected product is a pale-yellow to yellow, capsule-shaped film-coated tablet marked “EM 48”.
• It contains lactose monohydrate and is essentially sodium-free.
• The selected formulation is licensed for established urate deposition and chemotherapy-associated hyperuricaemia in eligible adults.

Tablet

Route: Oral

Strengths: 80 mg, 120 mg