Product: Uloric
Company: Takeda
Pharmacologic class: Xanthine oxidase inhibitor
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Active ingredient: Febuxostat 40 mg, 80 mg; tabs.
Indication: Chronic management of hyperuricemia in patients with gout.
Pharmacology: Gout is a chronic condition characterized by attacks, or “flares,” that are marked by intense pain, redness, swelling, and heat in the affected joint. These symptoms are caused by the buildup of uric acid that crystallizes and deposits under the skin and in joints. Gout is the most common inflammatory arthritis presenting in men older than age 40 years.
Febuxostat exerts its therapeutic effect by blocking the enzyme xanthine oxidase. Xanthine oxidase is responsible for the breakdown of the purine base, hypoxanthine, to xanthine and subsequently to uric acid. By blocking this enzyme, febuxostat helps to prevent the production of uric acid, thereby reducing the elevated levels of serum uric acid.
Clinical trials: Three randomized, double-blind, controlled clinical studies evaluated the efficacy of daily treatment with febuxostat compared with that of allopurinol 300 mg daily or placebo in 3,402 patients with hyperuricemia and gout. Hyperuricemia was defined as a baseline serum uric acid level ³8 mg/dL. In all three studies, patients also received naproxen 250 mg twice daily or colchicine 0.6 mg once or twice daily for gout flare prophylaxis.
The primary efficacy end point was the proportion of patients with a serum uric acid level <6 mg/dL at the final visit. Febuxostat 40 mg demonstrated comparable efficacy to allopurinol in lowering serum uric acid to <6 mg/dL at the final visit, whereas febuxostat 80 mg demonstrated superior efficacy. Of the patients treated with febuxostat 80 mg, 76% achieved a serum uric acid level <6 mg/dL by Week 2 and 83% of these patients maintained average serum uric acid levels of <6mg/dL throughout the treatment period.
Adults: >18 years: initially 40 mg once daily; if serum uric acid is not <6 mg/dL after two weeks, may increase to 80 mg once daily. Gout flare prophylaxis, with a nonsteroidal anti-inflammatory drug or colchicine, upon initiation of therapy and for up to six months, is recommended.
Children: <18 years: not recommended.
Contraindications: Concomitant azathioprine, mercaptopurine, theophylline.
Precautions: Not recommended for treating asymptomatic hyperuricemia. Cardiovascular events: monitor for signs and symptoms of MI and stroke. Severe renal impairment or end-stage renal disease on dialysis. Severe hepatic impairment. Monitor liver function at two and four months after initiation and periodically thereafter. Obtain target serum uric acid levels <6 mg/dL after two weeks of initiating therapy. Secondary hyperuricemia (e.g., Lesch-Nyhan syndrome, malignant disease, or in organ transplant recipients): not recommended. Pregnancy (Cat .C). Nursing mothers.
Interactions: See Contraindications. Potentiates xanthine oxidase substrate drugs.
Adverse reactions: Liver function abnormalities, nausea, arthralgia, rash, gout flares.
Note: Report suspected adverse reactions to Takeda at 877.825.3327 or FDA at 800.FDA.1088.
How supplied: Tabs
40 mg—30, 90, 500
80 mg—30; 100; 1,000
For more information, call 877.825.3327 or visit www.Uloric.com n
