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TAKEDA PHARMACE
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64764091830

brand uloric 40 mg tablet

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Uses

Gout

Febuxostat is used for long-term management of hyperuricemia in patients with gout. The drug is not recommended for the management of asymptomatic hyperuricemia.

The major goal in the management of hyperuricemia and gout is long-term reduction in serum urate concentrations to levels below the limit of urate solubility (about 6.8 mg/dL). Such a reduction over time will prevent or reverse the formation and deposition of urate crystals.

Efficacy of febuxostat was evaluated in 3 randomized, active-controlled studies in patients with hyperuricemia (serum urate concentrations of at least 8 mg/dL) and gout. Because initiation of therapy with urate-lowering agents is associated with an increased frequency of acute gouty attacks (gout flare), patients received concomitant therapy with naproxen or colchicine as prophylaxis against gout flares. At the final evaluation (6 months for 2 studies, 12 months for 1 study), 45%, 67-74%, or 36-42% of those receiving febuxostat 40 mg daily, febuxostat 80 mg daily, or allopurinol (300 mg daily in those with normal renal function; reduced dosage in those with renal impairment), respectively, achieved serum urate concentrations of less than 6 mg/dL.

Dosage and Administration

General

Acute gout attacks (gout flare) may occur after initiation of therapy with febuxostat. Therefore, gout flare prophylaxis with a nonsteroidal anti-inflammatory agent (NSAIA) or colchicine should be considered; these agents may be started when febuxostat therapy is initiated and may be beneficial for up to 6 months. If a gout flare occurs, febuxostat may be continued, and the gout flare managed as appropriate.

Testing for target serum urate concentrations can be performed after 2 weeks of febuxostat therapy.

Administration

Febuxostat is administered orally without regard to meals or antacids.

Dosage

The recommended initial dosage of febuxostat for the management of hyperuricemia in patients with gout is 40 mg once daily. The dosage of febuxostat may be increased to 80 mg once daily in patients who do not achieve serum urate concentrations of less than 6 mg/dL following 2 weeks of therapy with febuxostat 40 mg once daily.

Special Populations

Dosage adjustment is not needed in patients with mild to moderate renal or hepatic impairment.

Cautions

Contraindications

Concomitant therapy with azathioprine, mercaptopurine, or theophylline.(See Drug Interactions.)

Warnings/Precautions

Acute Gout

An increased frequency of acute gout attacks (gout flare) may occur after initiation of febuxostat due to increased mobilization of urate from tissue deposits in response to reduction in serum uric acid concentrations. Gout flare prophylaxis with a nonsteroidal anti-inflammatory agent (NSAIA) or colchicine should be considered; these agents may be started when febuxostat therapy is initiated.

Cardiovascular Events

In the randomized controlled studies to date, a higher rate of cardiovascular thromboembolic events (cardiovascular deaths, nonfatal myocardial infarction, nonfatal stroke) was reported in patients receiving febuxostat than in patients receiving allopurinol. A causal relationship to febuxostat has not been established. Patients should be monitored for signs and symptoms of myocardial infarction and stroke.

Hepatic Effects

Serum transaminase concentrations exceeding 3 times the upper limit of normal have been reported in patients receiving febuxostat. Liver function tests should be performed during therapy (e.g., at months 2 and 4 of therapy and then periodically).

Specific Populations

Pregnancy

Category C.

Lactation

Febuxostat is distributed into milk in rats; not known whether the drug is distributed into human milk. Use with caution in nursing women.

Pediatric Use

Safety and efficacy have not been established in pediatric patients younger than 18 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity of some older patients cannot be ruled out.

Pharmacokinetic values in geriatric adults were similar to those in younger adults. Dosage adjustment based on age is not needed.

Hepatic Impairment

Not studied in patients with severe hepatic impairment (Child-Pugh class C); caution if used in these individuals. Dosage adjustment is not needed in patients with mild to moderate hepatic impairment (Child-Pugh class A or B).

Renal Impairment

Insufficient data in patients with severe renal impairment (creatinine clearance of less than 30 mL/minute); caution if used in these individuals. Dosage adjustment is not needed in patients with mild to moderate renal impairment (creatinine clearance of 30-89 mL/minute).

Not studied in individuals with end-stage renal disease who are undergoing dialysis.

Secondary Hyperuricemia

Not evaluated in patients with secondary hyperuricemia. Use of febuxostat in patients whose rate of urate formation is greatly increased is not recommended.

Common Adverse Effects

Adverse effects reported in 1% or more of patients receiving febuxostat include liver function abnormalities, nausea, arthralgia, and rash.

Drug Interactions

Drugs Affecting Hepatic Microsomal or Other Enzymes

Febuxostat is metabolized by conjugation by glucuronosyltransferase (uridine diphosphoglucuronosyltransferase, UDP-glucuronate β-d-glucuronosyltransferase [acceptor-unspecific], UGT) enzymes, including UGT1A1, UGT1A3, UGT1A9, and UGT2B7, as well as by oxidation by cytochrome P-450 (CYP) isoenzymes, including CYP 1A2, 2C8, and 2C9, and non-CYP enzymes. However, the relative contribution of each enzyme isoform to the drug's metabolism is not clear. Drug interactions generally are not expected between febuxostat and inhibitors or inducers of particular enzyme isoforms.

Drugs Metabolized by Hepatic Microsomal Enzymes

Febuxostat does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, 2C19, or 3A4, but is a weak inhibitor of CYP2D6. Febuxostat does not induce CYP isoenzymes 1A2, 2B6, 2C9, 2C19, or 3A4. Pharmacokinetic interactions are unlikely between febuxostat and substrates of these isoenzymes.

Desipramine

Effects of febuxostat on desipramine pharmacokinetics are not considered clinically important; dosage adjustment is not expected to be necessary.

Drugs Metabolized by Xanthine Oxidase

Febuxostat is a xanthine oxidase inhibitor. Although studies have not been conducted to evaluate interactions between febuxostat and drugs metabolized by xanthine oxidase, inhibition of the enzyme by febuxostat is expected to increase plasma concentrations of these substrates, resulting in toxicity. Increased plasma concentrations have been reported when allopurinol, another xanthine oxidase inhibitor, was administered concomitantly with azathioprine, mercaptopurine, or theophylline. Therefore, concomitant use of febuxostat with these drugs is contraindicated.(See Contraindications.)

Antacids

Pharmacokinetic interaction unlikely.

Antineoplastic Agents

Studies have not been conducted with antineoplastic agents; data are not available regarding safety of febuxostat in patients receiving antineoplastic agents.(See Drug Interactions: Drugs Metabolized by Xanthine Oxidase.)

Colchicine

Clinically important pharmacokinetic interaction unlikely; dosage adjustment not needed.

Hydrochlorothiazide

Clinically important pharmacokinetic interaction unlikely; dosage adjustment not needed.

Nonsteroidal Anti-inflammatory Agents

Indomethacin

Clinically important pharmacokinetic interaction unlikely; dosage adjustment not needed.

Naproxen

Clinically important pharmacokinetic interaction unlikely; dosage adjustment not needed.

Warfarin

Pharmacokinetic interaction unlikely; dosage adjustment not needed.

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