Haller I
Arzneimittelforschung. 1986 Feb;36(2):226-9.
1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7-piperazine-1-ylquinoline-3-carboxylic acid (ciprofloxacin, Bay o-9867, Bay q-3939) was evaluated by checkerboard assay in combination with ampicillin, ticarcillin, mezlocillin, azlocillin, piperacillin, cefamandole, cefoxitin, cefotaxime, and ceftazidime. A total of 220 clinical isolates of enterobacteriaceae and Pseudomonas aeruginosa (11 species, 20 strains each) were examined. Predominantly additive combination effects were seen with all antibiotic combinations tested. Synergy was obtained with only a few test strains while antagonistic drug interactions were not observed at all. Time-kill experiments which were performed to assess the bactericidal activities, confirmed these findings. The antibiotic combinations were also evaluated in vivo using a model of experimental thigh muscle infection in neutropenic mice. In-difference or additive therapeutic effects resulted when the beta-lactam compounds and ciprofloxacin were given in combination at doses which were also effective alone. Subinhibitory doses of azlocillin and mezlocillin, on the other hand, appeared to increase the efficacy of ciprofloxacin. The influence of various application schedules was examined by time-kill experiments and in mice. Sequential administration of the drugs at intervals of 2 h did not alter the combination effects regardless of the sequence of administration.
通过棋盘法评估了1-环丙基-6-氟-1,4-二氢-4-氧代-7-哌嗪-1-基喹啉-3-羧酸（环丙沙星，拜耳o-9867，拜耳q-3939）与氨苄西林、替卡西林、美洛西林、阿洛西林、哌拉西林、头孢孟多、头孢西丁、头孢噻肟和头孢他啶联合使用的情况。共检测了220株肠杆菌科细菌和铜绿假单胞菌的临床分离株（11个菌种，每种20株）。在所测试的所有抗生素组合中，主要观察到相加的联合效应。仅在少数测试菌株中获得了协同作用，而完全未观察到拮抗药物相互作用。进行的时间杀菌实验以评估杀菌活性，证实了这些发现。还使用中性粒细胞减少小鼠的实验性大腿肌肉感染模型在体内评估了抗生素组合。当β-内酰胺类化合物和环丙沙星以单独也有效的剂量联合给药时，产生了无差异或相加的治疗效果。另一方面，阿洛西林和美洛西林的亚抑菌剂量似乎增加了环丙沙星的疗效。通过时间杀菌实验和在小鼠中研究了各种给药方案的影响。无论给药顺序如何，以2小时的间隔顺序给药药物不会改变联合效应。
