Kuwabara M, Matsui K
Jpn J Antibiot. 1984 Dec;37(12):2338-42.
Ceftriaxone (Ro 13-9904, CTRX), a newly developed third-generation cephem antibiotic, reportedly has an antibacterial spectrum of wide-range and shows a much greater activity than cefazolin especially against Gram-negative bacteria and satisfactory effectiveness against anaerobes. In the gyneco-obstetric infections, the relation between the level in the intrapelvic organs and MIC is an important subject in many respects. The levels in the blood and each tissue determined in 54 cases, as presented in Fig. 2, show that a high concentration can be maintained for a long time. In particular the half-life time in the uterine artery and cubital vein was 8.2 hours and 7.8 hours, respectively, which was longer than that of any other existing antibiotics. This fact suggests that CTRX exhibits sufficient efficacy when administered intravenously even in a small dosage of 1 g in the present study. The clinical efficacy was good or above in all the 7 cases treated. There was neither clinical adverse reaction nor laboratory test abnormality found during and after the administration in any of the 54 cases in the fundamental study and 7 cases in the clinical study. It is suggested from the above-mentioned results that CTRX is an unprecedentedly useful antibiotic with an antibacterial spectrum of wide-range.
头孢曲松（Ro 13 - 9904，CTRX）是一种新开发的第三代头孢菌素抗生素，据报道其抗菌谱广泛，对革兰氏阴性菌的活性比头孢唑林强得多，对厌氧菌也有令人满意的疗效。在妇产科感染中，盆腔内器官中的药物水平与最低抑菌浓度（MIC）之间的关系在许多方面都是一个重要课题。图2所示的54例患者血液及各组织中的药物水平表明，头孢曲松能长时间维持高浓度。特别是在子宫动脉和肘静脉中的半衰期分别为8.2小时和7.8小时，比其他现有抗生素的半衰期都长。这一事实表明，在本研究中即使静脉注射小剂量1 g的头孢曲松也能发挥足够的疗效。接受治疗的7例患者临床疗效均为良好及以上。在基础研究的54例患者和临床研究的7例患者中，给药期间及给药后均未发现临床不良反应及实验室检查异常。从上述结果可以看出，头孢曲松是一种抗菌谱广泛、前所未有的有用抗生素。
