Adult: For chronic cases in patients with gout or urate deposition (including a history, or presence of tophus and/or gouty arthritis): Initially, 40 mg once daily. Dose may be increased to 80 mg once daily if serum uric acid is >6 mg/dL after 2 weeks. Alternatively, 80 mg once daily. May increase dose to 120 mg once daily if serum uric acid is >6 mg/dL after 2-4 weeks. Gout flare prophylaxis for at least 6 months with an NSAID or colchicine is recommended at treatment initiation.
Oral Cancer therapy-induced hyperuricaemia
Adult: Prophylaxis and treatment of cases in patients undergoing chemotherapy for haematologic malignancies at intermediate to high risk of tumour lysis syndrome (TLS): 120 mg once daily. Started 2 days before the beginning of cytotoxic therapy and continued for 7-9 days based on chemotherapy duration.
Renal Impairment
Hyperuricaemia:
CrCl (mL/min)
Dosage
<30
Max: 40 mg once daily.
Hepatic Impairment
Hyperuricaemia:
Mild: Max: 80 mg daily.
Administration
May be taken with or without food. May be taken w/o regard to antacid use.
Contraindications
Concomitant use with azathioprine, mercaptopurine.
Special Precautions
Patient with history of hypersensitivity reaction to allopurinol; major CV disease (e.g. MI, stroke, unstable angina), ischaemic heart disease or CHF; thyroid disorders. Not to be started during an acute attack of gout; continue treatment if acute attacks occur in patients already receiving febuxostat, and treat the acute attack separately. Should only be used in patients who have an inadequate response to a maximally titrated allopurinol dose, who are intolerant to allopurinol, or when treatment with allopurinol is not advisable. Not recommended in organ transplant recipients, patients at increased risk of urate formation (e.g. Lesch-Nyhan syndrome, malignant disease and its treatment) or for the treatment of asymptomatic hyperuricaemia. Hepatic and severe renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: MI, stroke; gout flares, xanthine deposition, LFT abnormalities (e.g. increased serum AST/ALT), increased TSH. Cardiac disorders: Palpitation, left bundle branch block, sinus tachycardia. Eye disorders: Rarely, blurred vision. Gastrointestinal disorders: Diarrhoea, nausea, altered taste, abdominal pain. General disorders and administration site conditions: Oedema. Musculoskeletal and connective tissue disorders: Arthralgia. Nervous system disorders: Headache, dizziness, paraesthesia. Psychiatric disorders: Somnolence. Skin and subcutaneous tissue disorders: Rash. Vascular disorders: Flushing, hypertension, haemorrhage. Potentially Fatal: CV death, hepatic failure. Rarely, hypersensitivity (e.g. acute anaphylactic shock) and serious skin reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms).
Patient Counseling Information
This drug may cause dizziness, somnolence, paraesthesia and blurred vision; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor LFTs at baseline and periodically thereafter; serum uric acid levels 2 weeks after initiation of treatment; baseline renal function. Monitor cardiac function as clinically indicated in patients undergoing chemotherapy for haematologic malignancies at intermediate to high risk of TLS. Assess for gout flares, and signs or symptoms of CV events, liver injury, and hypersensitivity or severe skin reactions.
Drug Interactions
May increase the plasma concentrations of theophylline. May decrease the efficacy with potent UGT enzyme inducers. Potentially Fatal: Increased plasma concentrations resulting in severe toxicity of mercaptopurine and azathioprine.
Action
Description: Febuxostat is a potent, non-purine, selective inhibitor of xanthine oxidase, the enzyme that catalyses the conversion of hypoxanthine to xanthine to uric acid. The inhibition of xanthine oxidase decreases the serum concentrations of uric acid. Pharmacokinetics: Absorption: Rapidly and well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1-1.5 hours. Distribution: Plasma protein binding: Approx 99%, mainly to albumin. Metabolism: Extensively metabolised via conjugation by the uridine diphosphate glucuronosyltransferase (UGT) enzyme system and via oxidation by the CYP450 isoenzyme system into active hydroxyl metabolites. Excretion: Via urine (approx 49% as metabolites and 3% as unchanged drug); faeces (approx 45% as metabolites and 12% as unchanged drug). Elimination half-life: Approx 5-8 hours.
Chemical Structure
Febuxostat Source: National Center for Biotechnology Information. PubChem Database. Febuxostat, CID=134018, https://pubchem.ncbi.nlm.nih.gov/compound/Febuxostat (accessed on Jan. 20, 2020)
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