利奈唑胺

利奈唑胺
利奈唑胺的结构式
臨床資料
商品名英语Drug nomenclatureZyvox, Zyvoxam, Zyvoxid
AHFS/Drugs.comMonograph
MedlinePlusa602004
核准狀況
懷孕分級
  • : C
给药途径静脉注射,口服
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度~100% (口服)
血漿蛋白結合率低 (31%)
药物代谢经肝 (50–70%, CYP not 参与)
生物半衰期4.2–5.4 h (儿童更短)
排泄途徑非肾, 尿液, 粪便
识别信息
  • (S)-N-({3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide
CAS号165800-03-3  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
NIAID ChemDB
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.121.520 編輯維基數據鏈接
化学信息
化学式C16H20FN3O4
摩尔质量337.35 g·mol−1
3D模型(JSmol英语JSmol
  • O=C1O[C@@H](CNC(=O)C)CN1c3cc(F)c(N2CCOCC2)cc3
  • InChI=1S/C16H20FN3O4/c1-11(21)18-9-13-10-20(16(22)24-13)12-2-3-15(14(17)8-12)19-4-6-23-7-5-19/h2-3,8,13H,4-7,9-10H2,1H3,(H,18,21)/t13-/m0/s1 checkY
  • Key:TYZROVQLWOKYKF-ZDUSSCGKSA-N checkY

利奈唑胺Linezolid)为一种人工合成的唑烷酮类抗生素,主要抑制细菌蛋白质合成,可用于治疗由需氧的革兰阳性菌引起的感染,亦可用于耐多药结核杆菌治疗。

利奈唑胺由Pharmacia和Upjohn公司开发,用于治疗对其它几种抗生素有抗性的革兰氏阳性菌所造成的严重感染。利奈唑胺对大多数引起疾病的革兰氏阳性细菌具有活性,包括链球菌耐万古霉素肠球菌(VRE)和耐甲氧西林金黄色葡萄球菌(MRSA)。用于治疗皮肤感染与肺炎,不过可能可以用于其他感染,如耐药结核病。使用方法为口服或静脉注射。

医疗用途

皮肤和软组织感染

肺炎

其他

中枢神经系统感染

尿路感染

禁忌症

  腎臟扮演了清除Linezolid及其主要代謝物的重要角色,在腎臟受損的患者血液中Linezolid及其主要代謝物的濃度明顯比腎臟未受損的患者來的高[1],目前市場上的Linezolid藥物標示有註記:「由於Linezolid藥物的初級代謝物之累積缺乏臨床上的數據,腎臟功能缺乏的患者應被注意其使用的潛在風險。」

参考

  1. ^ Souza; E., Crass, R. L., Felton, J., Hanaya, K., & Pai, M. P. Accumulation of major linezolid metabolites in patients with renal impairment.. Antimicrobial Agents and Chemotherapy. 2020, 64(5). PMID 32152085. 

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