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头孢替坦在儿科的实验与临床评估

[Experimental and clinical evaluation of cefotetan in pediatrics].

作者信息

Toyonaga Y, Kurosu Y, Sugita M, Kita A, Yoshino N, Kouda N, Kumagai K, Horiuchi K, Hori M, Takahashi T

出版信息

Jpn J Antibiot. 1983 Jun;36(6):1243-60.

PMID:6581330
Abstract

Preclinical and clinical studies were carried out on cefotetan (CTT), a new synthetic cephamycin antibacterial agent. The results are described below. Antibacterial activity The minimum inhibitory concentrations (MICs) of CTT, CEZ, CTM and CMZ were determined against clinical isolates of S. aureus, E. coli, K. pneumoniae and P. mirabilis. To CTT S. aureus, showed its sensitivity peak (in the graphic plot of the MIC distribution) at a concentration range of 3.13-6.25 micrograms/ml when a 100-fold dilution of the pathological specimen was employed as the inoculum. These results were inferior to those with CEZ and CTM by 2-4 concentration tubes. The CTT results were also about 2 tubes inferior to the results with CMZ, which is a cephamycin antibiotic. On the other hand, CTT was found to show very strong antibacterial activity against Gram-negative rods. For example, the sensitivity peak of E. coli, occurred at an antibiotic concentration of less than or equal to 0.1-0.2 microgram/ml, regardless of whether the inoculum was the undiluted pathological specimen or the 100-fold dilution thereof. Similar results were obtained in relation to the K. pneumoniae strains: at a CTT concentration of less than or equal to 0.1 microgram/ml, suppression of growth was achieved in 74% of the strains when the inocula were the undiluted specimens, and 86% when the inocula were the 100-fold dilutions thereof. In addition, against P. mirabilis, when the inoculum consisted of the undiluted pathological specimen the MIC peak for CTT occurred at a concentration range of 0.39-0.78 microgram/ml, whereas the peak occurred at 0.2-0.39 microgram/ml when the bacterial inoculum was the 100-fold dilution of the collected specimen. In contrast, CTM showed slightly stronger antibacterial activity than CTT in relation to P. mirabilis; that is, its MIC peak occurred at less than or equal to 0.1-0.2 microgram/ml when the inoculum was the undiluted pathological specimen, and at less than or equal to 0.1 microgram/ml when the bacterial inoculum was the 100-fold dilution. Otherwise, against these 3 species of bacteria, CTT yielded results which were clearly superior to those achieved with the other 3 antibiotics. Absorption and excretion CTT was administered to children at a dosage of 10 mg/kg and 20 mg/kg as a one-shot intravenous injection or as a 1-hour intravenous drip infusion. Thereafter, the serum concentration of the antibiotic was monitored and it excretion rate in the urine was also determined.(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

对新型合成头孢霉素类抗菌剂头孢替坦(CTT)进行了临床前和临床研究。结果如下。抗菌活性:测定了CTT、头孢唑林(CEZ)、头孢噻肟(CTM)和头孢美唑(CMZ)对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和奇异变形杆菌临床分离株的最低抑菌浓度(MIC)。对于CTT,当使用病理标本100倍稀释液作为接种物时,金黄色葡萄球菌在3.13 - 6.25微克/毫升的浓度范围内显示出其敏感性峰值(在MIC分布的图表中)。这些结果比CEZ和CTM低2 - 4个浓度管。CTT的结果也比头孢霉素类抗生素CMZ的结果低约2个管。另一方面,发现CTT对革兰氏阴性杆菌显示出非常强的抗菌活性。例如,无论接种物是未稀释的病理标本还是其100倍稀释液,大肠杆菌的敏感性峰值都出现在抗生素浓度小于或等于0.1 - 0.2微克/毫升时。肺炎克雷伯菌菌株也得到了类似的结果:当接种物为未稀释标本时,在CTT浓度小于或等于0.1微克/毫升时,74%的菌株生长受到抑制;当接种物为100倍稀释液时,86%的菌株生长受到抑制。此外,对于奇异变形杆菌,当接种物为未稀释的病理标本时,CTT的MIC峰值出现在0.39 - 0.78微克/毫升的浓度范围内,而当细菌接种物为采集标本的100倍稀释液时,峰值出现在0.2 - 0.39微克/毫升。相比之下,CTM对奇异变形杆菌的抗菌活性略强于CTT;也就是说,当接种物为未稀释的病理标本时,其MIC峰值出现在小于或等于0.1 - 0.2微克/毫升,当细菌接种物为100倍稀释液时,峰值出现在小于或等于0.1微克/毫升。否则,对于这3种细菌,CTT产生的结果明显优于其他3种抗生素。吸收与排泄:以10毫克/千克和20毫克/千克的剂量对儿童进行一次性静脉注射或1小时静脉滴注给予CTT。此后,监测抗生素的血清浓度并测定其在尿液中的排泄率。(摘要截短于400字)

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引用本文的文献

1
Clinical pharmacokinetics of cefotetan.头孢替坦的临床药代动力学
Clin Pharmacokinet. 1994 Apr;26(4):248-58. doi: 10.2165/00003088-199426040-00002.
2
Cefotetan. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.头孢替坦:抗菌活性、药代动力学特性及治疗用途综述
Drugs. 1985 Nov;30(5):382-426. doi: 10.2165/00003495-198530050-00002.