Ishigami J, Mita T, Tanikaze S, Fujii A, Kuroda M
Jpn J Antibiot. 1976 Dec;29(12):1052-69.
In order to elucidate the usefulness of cephacetrile (CEC), comparative trials with cefazolin (CEZ) were carried out in the patients with complicated infections of the urinary tract, and the following results were obtained: 1. There were no statistically significant differences or tendencies observed between the groups given CEC and CEZ in either of the global effects, bacteriological effects, rate of superinfection, relapse, relapse with bacterial alternation, drug usefulness, rate of improvements in symptoms and findings in all the cases. 2. According to a result of stratified analyses, there were statistically significant differences observed, showing more inferior results of CEC than CEZ in either stratum of "below 50" in the age, "acute" in the disease phase, "infections of the upper urinary tract" in the disease pattern, and "E. coli including mixed infections with gram-positive organisms" in the pathogenic strains. However, it should be taken into consideration that certain background factors influence greatly in the effects and there were some problems on deviated backgrounds in these strata. On the other hand, CEC displayed better bacteriological effects than those of CEZ in higher stratum of "chronic" in the disease phase and "Klebsiella, Proteus, Citrobacter, Enterobacter including mixed infections" in the pathogenic strains, and statistically significant differences were not observed. 3. In consequence of bacteriological studies, CEC showed stronger resistance than CEZ against beta-lactamase produced in all the strains of gram-negative bacilli. Particularly there were significant differences or tendencies observed in those of Proteus, Cirtobacter, and Enterobacter, and at the same time there were great differences in the activity of beta-lactamase between CEC and CEZ as the substrate. 4. In correlation of the MIC and effects, CEC showed weaker actions than CEZ against susceptible organisms, but slightly stronger actions against moderately or highly resistant strains. A study of the relationship between the MIC of pathogenic strains, beta-lactamase, and bacteriological effects, showed possibilities that even the high activity of beta-lactamase results in remarkable effects in susceptible strains and the drugs with stronger resistance against beta-lactamase given better results in moderately or highly resistant organisms. 5. The incidence rate of adverse reactions was 2 out of 51 cases in the CEC group (3.9%) and 3 out of 50 cases in the CEZ group (6.0%), showing no significant difference, and those symptoms were similar. In conclusion, when the usefulness of CEC in complicated infections of the urinary tract is compared with that of CEZ, the former is said to be equal to the latter without significant difference as a whole...
为阐明头孢乙腈(CEC)的效用,在患有复杂性尿路感染的患者中开展了与头孢唑林(CEZ)的对比试验,结果如下:1. 在总体疗效、细菌学疗效、二重感染发生率、复发率、细菌交替性复发率、药物效用、所有病例症状及检查结果改善率等方面,接受CEC和CEZ治疗的组间未观察到统计学上的显著差异或趋势。2. 根据分层分析结果,在年龄“50岁以下”、疾病阶段“急性”、疾病类型“上尿路感染”以及病原菌“包括革兰氏阳性菌混合感染的大肠杆菌”的各分层中,均观察到统计学上的显著差异,表明CEC的结果比CEZ更差。然而,应考虑到某些背景因素对疗效有很大影响,且这些分层中存在背景偏差问题。另一方面,在疾病阶段“慢性”以及病原菌“克雷伯菌属、变形杆菌属、柠檬酸杆菌属、肠杆菌属包括混合感染”的较高分层中,CEC显示出比CEZ更好的细菌学疗效,且未观察到统计学上的显著差异。3. 细菌学研究结果显示,CEC对所有革兰氏阴性杆菌菌株产生的β-内酰胺酶的耐药性比CEZ更强。特别是在变形杆菌属、柠檬酸杆菌属和肠杆菌属中观察到显著差异或趋势,同时CEC和CEZ作为底物时β-内酰胺酶的活性存在很大差异。4. 在最低抑菌浓度(MIC)与疗效的相关性方面,CEC对敏感菌的作用比CEZ弱,但对中度或高度耐药菌株的作用稍强。对病原菌MIC、β-内酰胺酶与细菌学疗效之间关系的研究表明,即使β-内酰胺酶活性高,在敏感菌株中也可能产生显著疗效,而对β-内酰胺酶耐药性更强的药物在中度或高度耐药菌中效果更好。5. CEC组51例中有2例(3.9%)出现不良反应,CEZ组50例中有3例(6.0%)出现不良反应,差异无统计学意义,且症状相似。总之,当比较CEC在复杂性尿路感染中的效用与CEZ时,总体而言前者据说与后者相当,无显著差异……