头孢洛扎

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头孢洛扎
Ceftolozane.svg
系统(IUPAC)命名名称
(6R,7R)-3-([3-Amino-4-(2-aminoethylcarbamoylamino)-2-methylpyrazol-1-ium-1-yl]methyl)-7-([(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(2-carboxypropan-2-yloxyimino)acetyl]amino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
临床数据
商品名 Zerbaxa(与他唑巴坦联用时)
给药途径 静脉注射
合法狀態
合法状态
  • 2015年1月在美国获批
识别信息
CAS注册号689293-68-3 ✓
PubChem CID 53234134
化学信息
化学式 C23H30N12O8S2
摩尔质量 666.689 g/mol

头孢洛扎(Ceftolozane)[1] ,是第五代头孢抗生素,用来治疗对常规抗生素耐药的革兰氏阴性菌[2] 实验证明其对尿路感染、腹腔内感染、呼吸机相关性细菌性肺炎有效。头孢洛扎常与他唑巴坦与β-内酰胺酶抑制剂他唑巴坦英语Tazobactam联用,有防止头孢洛扎分解的作用。联用的头孢洛扎/他唑巴坦商品名为“Zerbaxa”。[3][4][5][6][7] 证据表明头孢洛扎可以治疗复杂尿路感染与复杂腹腔内感染。[8]

引用[编辑]

  1. ^ 高田田; 沈承武. 新型抗菌药物头孢洛扎/他唑巴坦的研究进展. 解放军药学学报. 2017, 5. 
  2. ^ Long, T. E.; Williams, J. T. Cephalosporins currently in early clinical trials for the treatment of bacterial infections. Expert Opinion on Investigational Drugs. 2014, 23 (10): 1375. doi:10.1517/13543784.2014.930127. 
  3. ^ Takeda, S; Nakai, T; Wakai, Y; Ikeda, F; Hatano, K. In vitro and in vivo activities of a new cephalosporin, FR264205, against Pseudomonas aeruginosa. Antimicrobial Agents and Chemotherapy. 2007, 51 (3): 826–30. PMC 1803152. PMID 17145788. doi:10.1128/AAC.00860-06. 
  4. ^ Toda, A; Ohki, H; Yamanaka, T; Murano, K; Okuda, S; Kawabata, K; Hatano, K; Matsuda, K; Misumi, K; Itoh, K; Satoh, K; Inoue, S. Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: Discovery of FR264205. Bioorganic & Medicinal Chemistry Letters. 2008, 18 (17): 4849–52. PMID 18701284. doi:10.1016/j.bmcl.2008.07.085. 
  5. ^ Sader, H. S.; Rhomberg, P. R.; Farrell, D. J.; Jones, R. N. Antimicrobial activity of CXA-101, a novel cephalosporin tested in combination with tazobactam against Enterobacteriaceae, Pseudomonas aeruginosa, and Bacteroides fragilis strains having various resistance phenotypes. Antimicrobial Agents and Chemotherapy. 2011, 55 (5): 2390–4. PMC 3088243. PMID 21321149. doi:10.1128/AAC.01737-10. 
  6. ^ Craig, W. A.; Andes, D. R. In vivo activities of ceftolozane, a new cephalosporin, with and without tazobactam against Pseudomonas aeruginosa and Enterobacteriaceae, including strains with extended-spectrum β-lactamases, in the thighs of neutropenic mice. Antimicrobial Agents and Chemotherapy. 2013, 57 (4): 1577–82. PMC 3623364. PMID 23274659. doi:10.1128/AAC.01590-12. 
  7. ^ Zhanel, G. G.; Chung, P; Adam, H; Zelenitsky, S; Denisuik, A; Schweizer, F; Lagacé-Wiens, P. R.; Rubinstein, E; Gin, A. S.; Walkty, A; Hoban, D. J.; Lynch Jp, 3rd; Karlowsky, J. A. Ceftolozane/tazobactam: A novel cephalosporin/β-lactamase inhibitor combination with activity against multidrug-resistant gram-negative bacilli. Drugs. 2014, 74 (1): 31–51. PMID 24352909. doi:10.1007/s40265-013-0168-2. 
  8. ^ 存档副本. [2015-06-02]. (原始内容存档于2015-05-09).