Febuxostat
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Contents |
Indications
- treatment of gout Contrandications: (caution)
- creatinine clearance < 30 mL/min
- hepatic disease, Child-Pugh class C
Dosage
- start 40 mg PO day
- increase to 80 mg/day after 2 weeks if serum uric acid > 6 mg/dL
- maximum 80 mg/day
- Tabs: 40 mg, 80 mg
Dosage-adjustment-in-renal-failure
- none for mild to moderate renal insufficiency (CrCl >= 30 mL/min)
Pharmacokinetics
- metabolized in the liver by both oxidation via cytochrome P450s CYP1A2, CYP2C8, & CYP2C9 & non-P450 enzymes & by conjugation via various uridine diphosphate glucuronosyltransferase
- eliminated by both liver & kidneys
Monitor
- baseline serum uric acid level, LFTs, & CBC
- recheck after 2 & 4 months, then periodically [4]
Adverse-effects
- abnormal liver function tests (4-7%)
- nausea (1%)
- arthralgia (1%)
- rash (1-2%)
Drug-interactions
- avoid use in combination with theophylline, mercaptopurine, or azathioprine; these drugs are metabolized by xanthine oxidase, thus may accumulate to toxic levels
Mechanism-of-action
- xanthine oxidase inhibitor
Notes
- Cost: ~$160/month (2009)
More General Terms
References
- Prescriber's Letter 16(4): 2009 New Drug: Uloric (Febuxostat) Detail-Document#: [1] (subscription needed) [2]
- Bruce SP. Febuxostat: a selective xanthine oxidase inhibitor for the treatment of hyperuricemia and gout. Ann Pharmacother 2006;40:2187-94 PMID: [3]
- Mayer MD et al Pharmacokinetics and pharmacodynamics of febuxostat, a new non-purine selective inhibitor of xanthine oxidase in subjects with renal impairment. Am J Ther 2005;12:22-34. PMID: [4]
- Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: [5] (subscription needed) [6]
- National Guideline Clearinghouse Febuxostat for the management of hyperuricaemia in people with gout. National Institute for Health and Clinical Excellence (NICE). ngc-guideline: [7]
