Uloric: first new option for gout in more than 40 years

Takeda Canada will soon be introducing Uloric (febuxostat 80 mg) tablets, the first new drug to be marketed for gout in more than four decades. Febuxostat, a nonpurine selective xanthine oxidase (XO) inhibitor, is indicated for lowering serum uric acid levels in patients with gout.Dosage: The recommended dosage of febuxostat is 80 mg once daily, taken without regard to food or antacids. No dose adjustment is needed in patients with mild or moderate hepatic or renal impairment. Febuxostat should not be started until an acute attack of gout has completely subsided.After initiating febuxostat, an increase in gout flares is frequently seen. To reduce their occurrence, concurrent flare prophylaxis with a nonsteroidal anti-inflammatory drug or colchicine is recommended for up to six months. If an acute flare occurs, febuxostat should be continued while the flare is managed with appropriate therapy. Adverse effects: The most common adverse effects in febuxostat clinical studies were liver function abnormalities (4.6%), diarrhea (3.0%), rash (1.6%), nausea (1.3%) and dizziness (1.1%). A higher rate of thromboembolic events (cardiovascular death, nonfatal myocardial infarction, nonfatal stroke) were reported in patients receiving febuxostat (1.09 per 100 person-years) compared to allopurinol (0.60 per 100 person-years); therefore, the product monograph recommends monitoring for signs and symptoms of myocardial infarction and stroke.Transaminase elevations > 3 times the upper limit of normal have been observed to a similar degree in both febuxostat- and allopurinol-treated patients; liver function tests (serum transaminases) are recommended prior to starting febuxostat and periodically thereafter.Drug interactions: Febuxostat may increase the plasma concentrations of drugs metabolized by XO, potentially leading to toxicity. Concomitant administration with substrates of XO (i.e., azathioprine, mercaptopurine, theophylline) is contraindicated.Comments: To date, chronic gout has been treated primarily with allopurinol, a purine analogue xanthine oxidase inhibitor, and uricosurics (e.g., probenecid) that stimulate the renal excretion of uric acid. Clinical trials have shown that the new drug, febuxostat 80 mg/day, is at least as effective or superior to allopurinol 300 mg/day (200 mg/day in renal impairment), with a similar safety profile.Unlike allopurinol, no dose adjustment is required for febuxostat in patients with mild-to-moderate renal impairment. Allopurinol will likely remain the first-line option for management of hyperuricemia and gout, due to extensive clinical experience with the drug and its lower cost.Febuxostat will provide an important alternative for patients unable to use allopurinol, those with very high serum urate levels and those with refractory gouty tophi (nodules). Healthcare professionals should emphasize the importance of adherence to urate-lowering therapy, since these drugs must be taken consistently to achieve sustained benefits.ReferencesTakeda Canada Inc. Uloric (febuxostat tablet) product monograph. Mississauga, Ont.; September 21, 2010.Gaffo AL, Saag KG. Febuxostat: the evidence for its use in the treatment of hyperuricemia and gout. Core Evid 2009;4:25-36. www.ncbi.nlm.nih.gov/pmc/articles/PMC2899777/?tool=pubmed (accessed October 5, 2010).Doghramji PP, Edwards NL, McTigue J. Managing gout in the primary care setting: what you and your patients need to know. Am J Med 2010;123:S2.Love BL, Barrons R, Veverka A, et al. Urate-lowering therapy for gout: focus on febuxostat. Pharmacotherapy 2010;30:594-608.Becker MA, Schumacher HR, Espinoza LR, et al. The urate-lowering efficacy and safety of febuxostat in the treatment of the hyperuricemia of gout: the CONFIRMS trial.Arthritis Res Ther 2010;12(2):R63.Ernst ME, Fravel MA Febuxostat: a selective xanthine-oxidase/xanthine-dehydrogenase inhibitor for the management of hyperuricemia in adults with gout. Clin Ther 2009;31:2503-18.Edwards NL. Febuxostat: a new treatment for hyperuricaemia in gout. Rheumatology 2009;48(Suppl 2):ii15-ii19.

Uloric: first new option for gout in more than 40 years

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