Ishii Y, Kanashige E, Tanimura T, Hayashi Y, Sekiba K, Katayama S, Fukumoto S, Hayase R, Hayata K
Jpn J Antibiot. 1985 Apr;38(4):1001-10.
The findings from recent fundamental and clinical studies of the efficacy of cefpimizole (AC-1370) in obstetrics and gynecology are reported in this paper. The AC-1370 concentrations in genital tissues sampled 30 to 56 minutes (a mean of 41.4 minutes) after intravenous injection of 1 g of the drug were 14 to 76 micrograms/g (a mean of 32.4 micrograms/g). The mean transfer ratios of the drug into the genital tissues to the concentration in the uterine arterial blood were such that the transfer ratio into the portio vaginalis was the highest, followed by the uterine cervix and the myometrium, and that into the oviduct was the lowest with about 1/2 that into the portio vaginalis. The concentration in the antecubital venous blood and that in the uterine arterial blood remained similar for all patients. The transfer of AC-1370 into the pelvic dead space exudate reached a peak (49.5 micrograms/ml) 1 hour, and also a peak (49.8 micrograms/ml) 2 hours after the intravenous injection. It then decreased gradually, but remained high, being higher than that in the antecubital venous blood about 50 minutes after the intravenous injection. Ten patients with infections in gynecology were treated with 1.0 to 4.0 g daily of AC-1370, to a total dose of 6 to 52 g, over a period of 3 to 13 days. One of them showed excellent response, 8 showed moderate response, and another showed poor response to the treatment: in other words, a response rate of 90% was achieved. Bacteriologically, pathogens were eradicated from 3 and decreased in 3, and microbial substitution occurred in another patient. No side effects of the drug were observed except for eruption in 1 patient. None of the 10 patients showed any abnormalities in laboratory findings. From the present fundamental and clinical studies of AC-1370, we have drawn the conclusion that the drug is one of extremely useful antibiotics in the treatment of infections in obstetrics and gynecology.
本文报道了近期头孢咪唑（AC - 1370）在妇产科疗效的基础及临床研究结果。静脉注射1g该药后30至56分钟（平均41.4分钟）采集的生殖组织中，AC - 1370浓度为14至76微克/克（平均32.4微克/克）。药物进入生殖组织与子宫动脉血中浓度的平均转移率情况为，进入阴道部的转移率最高，其次是子宫颈和子宫肌层，进入输卵管的转移率最低，约为进入阴道部转移率的1/2。所有患者的肘前静脉血浓度和子宫动脉血浓度保持相似。AC - 1370向盆腔死腔渗出液中的转移在静脉注射后1小时达到峰值（49.5微克/毫升），2小时时也达到峰值（49.8微克/毫升）。随后逐渐下降，但仍维持在较高水平，在静脉注射后约50分钟高于肘前静脉血中的浓度。10例妇科感染患者接受每日1.0至4.0g的AC - 1370治疗，总剂量为6至52g，疗程为3至13天。其中1例显示出极佳疗效，8例显示出中度疗效，另1例显示疗效不佳：也就是说，总有效率达到90%。从细菌学角度来看，3例患者的病原体被根除，3例患者的病原体数量减少，另有1例患者发生了微生物替代。除1例患者出现皮疹外，未观察到该药的其他副作用。10例患者的实验室检查结果均未显示任何异常。基于目前对AC - 1370的基础及临床研究，我们得出结论，该药是治疗妇产科感染极为有效的抗生素之一。
