生物活性

• 描述Linezolid is the first of a new class of antibacterial drugs, the oxazolidinones. It has inhibitory activity against a broad range of gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide-intermediate S. aureus (GISA), vancomycin-resistant enterococci (VRE) and penicillin-resistant Streptococcus pneumoniae. The drug also shows activity against certain anaerobes, including Clostridium perfringens, C. difficile, Peptostreptococcus spp. and Bacteroidesfragilis^[3]. Linezolid is bacteriostatic against most susceptible organisms but displays bactericidal activity against some strains of pneumococci, Bacteroides fragilis and C. perfringens. Moreover, linezolid 600 mg twice daily produced >85% clinical/microbiological cure in vancomycin-resistant enterococcal infections^[4]. Linezolid inhibits bacterial growth by targeting bacterial ribosomes and by interfering with bacterial protein synthesis. Lactic acidosis is a rare, but potentially lethal, side effect of linezolid^[5]. In addition, the incidence of vomiting, diarrhea, and thrombocytopenia in patients treated with linezolid is significantly higher than that with other treatments. Linezolid seems to be more effective than vancomycin for treating people with SSTIs (skin and soft tissue infections) ^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01592032	Catheter-Related Infections ... more >> Bacteremia. Collapse <<	Phase 4	Unknown	December 2015	Spain ... more >> Clinica Universidad de Navarra Pamplona, Navarra, Spain, 31008 Collapse <<
  NCT03583333	Hospital-Acquired Bacterial Pn... more >>eumonia Ventilator-Associated Bacterial Pneumonia Collapse <<	Phase 3	Recruiting	April 25, 2021	China, Beijing ... more >> Peking University Third Hospital ( Site 0115) Recruiting Beijing, Beijing, China, 100191 Contact: Study Coordinator    +8613910125933       China, Guangdong The First Affiliated Hospital of Guangzhou Medical University ( Site 0123) Recruiting Guangzhou, Guangdong, China, 510120 Contact: Study Coordinator    +8613902273260       Guangzhou First People's Hospital ( Site 0101) Recruiting Guangzhou, Guangdong, China, 510180 Contact: Study Coordinator    +862081048888       Southern Medical University Nanfang Hospital ( Site 0120) Recruiting Guangzhou, Guangdong, China, 510515 Contact: Study Coordinator    +8613119545239       Shenzhen People s Hospital ( Site 0134) Recruiting Shenzhen, Guangdong, China, 518020 Contact: Study Coordinator    +8675525533018       China, Jiangsu First Hospital Affiliated to Suzhou University ( Site 0111) Recruiting Suzhou, Jiangsu, China, 215008 Contact: Study Coordinator    +8651267780040       Wuxi People's Hospital ( Site 0124) Recruiting Wuxi, Jiangsu, China, 214023 Contact: Study Coordinator    +86051085350348       China, Jiangxi Jiangxi Provincial People's Hospital ( Site 0129) Recruiting Nanchang, Jiangxi, China, 330006 Contact: Study Coordinator    +8679186895863       The First Affiliated Hospital of Nanchang University ( Site 0132) Recruiting Nanchang, Jiangxi, China, 330006 Contact: Study Coordinator    +8613707089183       China, Shanghai Huashan Hospital of Fudan University ( Site 0105) Recruiting Shanghai, Shanghai, China, 200040 Contact: Study Coordinator    +8621528899       Shanghai General Hospital ( Site 0125) Recruiting Shanghai, Shanghai, China, 200080 Contact: Study Coordinator    8602163240090       China, Zhejiang The First Affiliated Hospital.Zhejiang University ( Site 0102) Recruiting Hangzhou, Zhejiang, China, 310003 Contact: Study Coordinator    +8613505719970       Sir Run Run Shaw Hospital School of Medicine, Zhejiang University ( Site 0110) Recruiting Hangzhou, Zhejiang, China, 310016 Contact: Study Coordinator    +86057186006102       The 2nd Affiliated Hospital of Wenzhou Medical University ( Site 0130) Recruiting Wenzhou, Zhejiang, China, 325000 Contact: Study Coordinator    +8613857715778       China Aero Space center hospital ( Site 0118) Recruiting Beijing, China, 100049 Contact: Study Coordinator    +8613611106725       Beijing Hospital ( Site 0127) Recruiting Beijing, China, 100730 Contact: Study Coordinator    +8613701097436       Ruijin Hospital Shanghai Jiao Tong University School of Medicine ( Site 0104) Recruiting Shanghai, China, 200025 Contact: Study Coordinator    +8602134186000 Collapse <<
  NCT00035269	Pneumonia, Pneumococcal ... more >> Community Acquired Infections Gram-positive Bacterial Infections Collapse <<	Phase 3	Completed	-	-

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• 参考文献

• [1] Swaney SM, Aoki H, et al. The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria. Antimicrob Agents Chemother. 1998 Dec;42(12):3251-5.

  [2] Shinabarger DL, Marotti KR, et al. Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother. 1997 Oct;41(10):2132-6.

  [3] Perry CM, Jarvis B. Linezolid: a review of its use in the management of serious gram-positive infections [published correction appears in Drugs. 2003;63(19):2126]. Drugs. 2001;61(4):525–551

  [4] Clemett D, Markham A. Linezolid. Drugs. 2000;59(4):815–828

  [5] Santini A, Ronchi D, Garbellini M, Piga D, Protti A. Linezolid-induced lactic acidosis: the thin line between bacterial and mitochondrial ribosomes. Expert Opin Drug Saf. 2017;16(7):833–843

  [6] Li Y, Xu W. Efficacy and safety of linezolid compared with other treatments for skin and soft tissue infections: a meta-analysis. Biosci Rep. 2018;38(1):BSR20171125. Published 2018 Feb 13

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