chronic management of hypeuricemia in patients with gout.
藥理
Feburic is a potent and selective xanthine oxidase inhibitor, thereby reduces the formation of xanthine and uric acid. Feburic is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations.
藥動學
Bioavailability: 49%, plasma protein binding: 99.2%, primarily to albumin; Metabolism: Extensive conjugation via uridine diphosphate glucuronosyltransferases (UGTs) 1A1, 1A3, 1A9, and 2B7 and oxidation via cytochrome P450 (CYP) 1A2, 2C8, and 2C9 as well as non-P450 enzymes. Oxidation leads to formation of active metabolites; Elimination half life: 5-8 hours.
禁忌症
Hypersensitivity to febuxostat or any component of the formulation; Concurrent use with azathioprine and mercaptopurine.
懷孕分類
C
哺乳分類
Excretion in breast milk unknown/use caution
副作用
Liver function abnormalities (5% to 7%), nausea, arthralgia and rash.
劑量和給藥方法
Orally, start at 40mg once daily; may be increased to 80 mg once daily if serum uric acid levels of less than 6 mg/dL are not achieved after 2 weeks. Administer with or without meals or antacids.
小兒調整劑量
Renal impairment (severe, CrCl, 15 to 29 mL/min): Limit dose to 40 mg QD