Vanhoof R, Bérin C, Carpentier M, Fagnart O, Glupczynski Y, Mans I, Nyssen H J, Surmont I, Van Nimmen L
Pasteurinstituut-Brussel, Eenheid Antibiotica-onderzoek, Engelandstraat 642, B-1180 Brussel.
Acta Clin Belg. 2001 Nov-Dec;56(6):354-9. doi: 10.1179/acb.2001.053.
Temocillin, a methoxy-derivative of the broad-spectrum penicillin, ticarcillin, has been introduced into clinical practice in Belgium in 1988. Since then, not many surveys of its in vitro activity have been published. This study addresses this issue in a prospective collection of 300 consecutive Gram-negative isolates originating from in-patients in five general hospitals throughout Belgium. In addition to temocillin, seven common antibiotics were tested: amoxicillin-clavulanate, piperacillin-tazobactam, cefotaxime, aztreonam, meropenem, ciprofloxacin and amikacin. Meropenem appeared to exhibit the best activity overall, whereas amoxicillin-clavulanate scored the worst. Cumulative MIC plot for two subsets of organisms are given: temocillin, meropenem and cefotaxime are the most active on E. coli and Klebsiella spp., while a significant percentage is resistant to ciprofloxacin and amoxicillin-clavulanate. In the group of inducible Enterobacteriaceae, temocillin, meropenem and amikacin are the most active drugs, while the activity of amoxicillin-clavulanate, piperacillin-tazobactam, cefotaxime and ciprofloxacin is largely decreased. Taking this well preserved in vitro activity of temocillin into account, and looking at its convenient pharmacokinetics and low cost of acquisition, this drug may prove a useful alternative in the treatment of severe nosocomial infections.
替莫西林是广谱青霉素替卡西林的甲氧基衍生物,于1988年在比利时投入临床使用。从那时起,关于其体外活性的研究报道并不多。本研究通过前瞻性收集来自比利时五家综合医院住院患者的300株连续革兰氏阴性菌分离株来解决这个问题。除替莫西林外,还测试了七种常用抗生素:阿莫西林-克拉维酸、哌拉西林-他唑巴坦、头孢噻肟、氨曲南、美罗培南、环丙沙星和阿米卡星。美罗培南总体表现出最佳活性,而阿莫西林-克拉维酸活性最差。给出了两组菌株的累积MIC图:替莫西林、美罗培南和头孢噻肟对大肠杆菌和克雷伯菌属最具活性,而相当比例的菌株对环丙沙星和阿莫西林-克拉维酸耐药。在可诱导肠杆菌科菌群中,替莫西林、美罗培南和阿米卡星是最具活性的药物,而阿莫西林-克拉维酸、哌拉西林-他唑巴坦、头孢噻肟和环丙沙星的活性大幅降低。考虑到替莫西林良好的体外活性,以及其便利的药代动力学和较低的购置成本,该药可能是治疗严重医院感染的一种有用替代药物。