头孢洛扎

头孢洛扎
臨床資料
商品名（英语：Drug nomenclature）	Zerbaxa（与他唑巴坦联用时）
给药途径	静脉注射
法律規範狀態
法律規範	2015年1月在美国获批;
识别信息
	IUPAC命名法 (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; ;
CAS号	689293-68-3
PubChem CID	53234134;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID901031217 ;
化学信息
化学式	C23H30N12O8S2
摩尔质量	666.69 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC(C)(C(=O)O)O/N=C(/c1nc(sn1)N)\C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C[n+]4cc(c(n4C)N)NC(=O)NCCN)C(=O)[O-];
	InChI InChI=1S/C23H30N12O8S2/c1-23(2,20(40)41)43-31-11(15-30-21(26)45-32-15)16(36)29-12-17(37)35-13(19(38)39)9(8-44-18(12)35)6-34-7-10(14(25)33(34)3)28-22(42)27-5-4-24/h7,12,18,25H,4-6,8,24H2,1-3H3,(H7,26,27,28,29,30,32,36,38,39,40,41,42)/b31-11-/t12-,18-/m1/s1; Key:JHFNIHVVXRKLEF-DCZLAGFPSA-N;

头孢洛扎^[1]（ceftolozane）是第五代头孢类抗生素，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

^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ FDA approves new antibacterial drug Zerbaxa. 2014-12-09 [2015-06-02]. （原始内容存档于2015-05-09）.

[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] FDA approves new antibacterial drug Zerbaxa. 2014-12-09 [2015-06-02]. （原始内容存档于2015-05-09）.

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