Amifloxacin (Win49375) is a fluorinated quinolone-carboxylic acid antibacterial agent with activity against a broad range of gram-negative organisms.
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Amifloxacin (Win49375) is a fluorinated quinolone-carboxylic acid antibacterial agent with activity against a broad range of gram-negative organisms. The MICs for 90% of isolates of representative urinary tract pathogens are 0.125μg/ml for Escherichia coli, 0.5μg/ml for Klebsiella pneumoniae, 1.0ug/ml for Proteus vulgaris, 0.5ug/ml for Citrobacter freundii, 2.0μg/ml for Pseudomonas aeruginosa, and 0.5ug/ml for Serratia marcescens [1].
Amifloxacin (Win49375), was an effective drug against experimental infections in mice when given parenterally. Amifloxacin (Win49375) was highly active by the oral route, with 50% effective doses within two- to three fold of those obtained with parenteral medication [2].
参考文献:
[1]. Neu H C, Labthavikul P. Antibacterial activity of amifloxacin (WIN 49, 375), a new quinolone agent[J]. Diagnostic microbiology and infectious disease, 1985, 3(6): 469-478.
[2]. Cornett J B, Wagner R B, Dobson R A, et al. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin)[J]. Antimicrobial agents and chemotherapy, 1985, 27(1): 4-10.
Amifloxacin (Win49375) 是一种氟化喹诺酮羧酸类抗菌剂,对多种革兰氏阴性菌具有活性。 90% 的代表性尿路病原体分离株的 MIC 为大肠杆菌 0.125μg/ml,肺炎克雷伯菌 0.5μg/ml,普通变形杆菌 1.0ug/ml,弗氏柠檬酸杆菌 0.5ug/ml,弗氏柠檬酸杆菌 2.0μg/ml铜绿假单胞菌和粘质沙雷氏菌 0.5ug/ml [1].
Amifloxacin (Win49375) 是一种有效的药物,当通过胃肠外给药时,它可以有效对抗小鼠的实验性感染。阿米沙星 (Win49375) 在口服途径中具有很高的活性,50% 的有效剂量是肠胃外用药的两到三倍[2]。
Animal experiment [1]: | |
Animal models |
ICR female mice weighing 18 to 20 g |
Preparation Method |
ICR female mice were inoculated intraperitoneally with 0.5 ml of the E. coli Vogel bacterial suspension and then distributed into subgroups of 10 to receive serial twofold doses of the test agents and a subgroup of 20 to serve as untreated controls. The infected mice were medicated p.o. 0.8-1.3 mg/kg or s.c. 0.2-1.6 mg/kg of Amifloxacin (Win49375). The number of survivors was determined daily for 7 days. |
Dosage form |
0.8-1.3 mg/kg/d for 7 days, p.o.; 0.2-1.6 mg/kg/d for 7 days, s.c. |
Applications |
Amifloxacin (Win49375) showed a consistently high protective effect against bacterial infection, with ED50s of 1.0 mg/kg for p.o. and 1.0 mg/kg for s.c. . |
参考文献: [1]: Cornett J B, Wagner R B, Dobson R A, et al. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin)[J]. Antimicrobial agents and chemotherapy, 1985, 27(1): 4-10. |
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