非布司他

非布司他(Febuxostat)是一种用于治疗痛风的药物,而藥品所針對的痛風基本因尿酸水平过高而引起[4]。該藥物通過抑制黄嘌呤氧化酶,从而减少体内尿酸的产生。該藥的給藥途徑口服。該藥常见的副作用包括肝脏出現问题、恶心、关节痛和皮疹[4]等症狀。妊娠或哺乳期婦女不建议服用該藥物[5][6]

非布司他
系统(IUPAC)命名名称
2-(3-cyano-4-isobutoxyphenyl)-4-methyl-
1,3-thiazole-5-carboxylic acid
临床数据
商品名Uloric, Adenuric[1]
Drugs.comMonograph
MedlinePlusa609020
医疗法规
妊娠分级
给药途径口服
合法狀態
合法状态
  • US: 处方药(-only)
  • EU: Rx-only
药代动力学数据
生物利用度≥84% absorbed
蛋白结合度99.2%至albumin
代谢通過CYP1A1, CYP1A2, CYP2C8, CYP2C9, UGT1A1, UGT1A8, UGT1A9[3]
生物半衰期~5–8 小時
排泄Urine (~49%, mostly as metabolites, 3% as unchanged drug); feces (~45%, mostly as metabolites, 12% as unchanged drug)
识别
CAS注册号144060-53-7  N
ATC代码M04AA03
PubChemCID 134018
IUPHAR/BPS6817
DrugBankDB04854
ChemSpider118173 
UNII101V0R1N2E 
KEGGD01206 
ChEBICHEBI:31596
ChEMBLCHEMBL1164729 
化学
化学式C16H16N2O3S
摩尔质量316.38 g·mol−1

非布司他于2008年和2009年分别在欧盟和美国被批准用于医疗用途[7][4]。2019年,還藥的仿制藥被監管部門批准,2020年起正式上市[8] [9]

参考文献

  1. Drugs.com Drugs.com international names for febuxostat Page accessed June 25, 2015
  2. . Drugs.com. 22 February 2019 [17 May 2020].
  3. (PDF). European Medicines Agency. 2019-08-06.
  4. . Drugs.com. American Society of Health-System Pharmacists. [26 February 2019] (英语).
  5. 76. Pharmaceutical Press. 2018: 1087. ISBN 9780857113382.
  6. . FDA. 21 February 2019 [26 February 2019] (英语).
  7. . European Medicines Agency - Commission. 17 September 2018 [26 February 2019] (英语).
  8. . Drugs.com. [1 August 2019] (英语).
  9. . [15 April 2020].
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.