Febuxostat Administration Route
Febuxostat is not available in injectable form and is only administered orally as tablets. 1, 2, 3
Available Formulation and Administration
- Febuxostat is only available as an oral medication in tablet form for the management of hyperuricemia in patients with gout 2, 4
- The pharmacokinetic studies consistently demonstrate that febuxostat has been developed and studied exclusively as an oral medication with approximately 85% oral bioavailability 5
- Febuxostat is rapidly absorbed when taken orally, with peak plasma concentrations reached within 0.5-1.3 hours after administration 2
- Standard dosing is once daily, with no injectable formulation mentioned in any clinical guidelines or pharmacokinetic studies 1, 3
Pharmacokinetic Properties
- Febuxostat demonstrates linear pharmacokinetics within the 10-120 mg dose range with a mean apparent total clearance of 10-12 L/h 2
- The drug is extensively metabolized via glucuronidation (22-44% of the dose) and oxidation (2-8%), with only 1-6% excreted unchanged via the kidneys 2, 5
- The elimination half-life ranges from 1.3 to 15.8 hours, with a terminal half-life of approximately 9.4 hours at therapeutic doses 2, 5
- Febuxostat's pharmacokinetic parameters are not significantly affected by mild to moderate hepatic or renal impairment 3, 6
Clinical Considerations
- In clinical practice, febuxostat is used as an alternative to allopurinol for patients with hyperuricemia and gout, particularly for those who cannot tolerate allopurinol 1
- The American College of Rheumatology guidelines only discuss oral febuxostat administration and make no mention of any injectable formulation 1
- For patients with tumor lysis syndrome requiring rapid uric acid reduction, rasburicase (an injectable medication) is mentioned as an alternative, while febuxostat is only referenced in its oral form 1
- Patients with cardiovascular disease should be aware of potential cardiovascular risks associated with febuxostat, as highlighted by the FDA black box warning 1, 7
Important Considerations When Using Oral Febuxostat
- Prophylaxis with colchicine or NSAIDs is recommended when initiating febuxostat to prevent gout flares due to rapid urate lowering 7, 4
- No dose adjustment is required for patients with mild to moderate renal impairment 3, 6
- The most common adverse reactions include abnormal liver function tests, headache, and gastrointestinal symptoms 4
- Careful consideration should be given before using febuxostat in patients with cardiovascular disease due to potential increased risk of cardiovascular-related death 1, 7