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。該藥的給藥途徑為口服。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]。
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系统(IUPAC)命名名称 | |
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2-(3-cyano-4-isobutoxyphenyl)-4-methyl- 1,3-thiazole-5-carboxylic acid | |
临床数据 | |
商品名 | Uloric, Adenuric[1] |
Drugs.com | Monograph |
MedlinePlus | a609020 |
医疗法规 |
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妊娠分级 | |
给药途径 | 口服 |
合法狀態 | |
合法状态 |
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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 ![]() |
ATC代码 | M04AA03 |
PubChem | CID 134018 |
IUPHAR/BPS | 6817 |
DrugBank | DB04854 |
ChemSpider | 118173 ![]() |
UNII | 101V0R1N2E ![]() |
KEGG | D01206 ![]() |
ChEBI | CHEBI:31596 |
ChEMBL | CHEMBL1164729 ![]() |
化学 | |
化学式 | C16H16N2O3S |
摩尔质量 | 316.38 g·mol−1 |
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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
- Drugs.com Drugs.com international names for febuxostat Page accessed June 25, 2015
- . Drugs.com. 22 February 2019 [17 May 2020].
- (PDF). European Medicines Agency. 2019-08-06.
- . Drugs.com. American Society of Health-System Pharmacists. [26 February 2019] (英语).
- 76. Pharmaceutical Press. 2018: 1087. ISBN 9780857113382.
- . FDA. 21 February 2019 [26 February 2019] (英语).
- . European Medicines Agency - Commission. 17 September 2018 [26 February 2019] (英语).
- . Drugs.com. [1 August 2019] (英语).
- . [15 April 2020].
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