Jules K, Neu H C
Antimicrob Agents Chemother. 1982 Sep;22(3):453-60. doi: 10.1128/AAC.22.3.453.
Temocillin, a 6-alpha-methoxy penicillin, inhibited 90% of strains of Escherichia coli, Klebsiella pneumoniae, Citrobacter, Proteus, Providencia, Salmonella, and Shigella at a concentration of less than or equal to 16 micrograms/ml. Haemophilus influenzae and Neisseria gonorrhoea were inhibited by less than or equal to 1 microgram/ml. Changing the medium or pH of the cultures did not alter the minimal inhibitory concentrations, which were similar in broth and human serum, as were the minimal bactericidal concentrations. An increase in inoculum size from 10(5) to 10(7) colony-forming units increased concentration required for inhibition. Temocillin inhibited strains resistant to ampicillin, ticarcillin, cefazolin, cefamandole, and cefoxitin. Most Pseudomonas aeruginosa strains and other Pseudomonas spp. and Acinetobacter spp. were resistant, as were gram-positive organisms. Temocillin was not hydrolyzed by the common plasmid and chromosomal beta-lactamases but inhibited them. The resistance of certain gram-negative bacilli to temocillin seemed to be a result of failure of the molecule to enter through the cell wall, since combination of temocillin with EDTA made Pseudomonas, Acinetobacter, and Enterobacter strains susceptible to low concentrations of the compound.
替莫西林是一种6-α-甲氧基青霉素,在浓度小于或等于16微克/毫升时,可抑制90%的大肠杆菌、肺炎克雷伯菌、柠檬酸杆菌、变形杆菌、普罗威登斯菌、沙门菌和志贺菌菌株。流感嗜血杆菌和淋病奈瑟菌在浓度小于或等于1微克/毫升时被抑制。改变培养基或培养物的pH值不会改变最低抑菌浓度,其在肉汤和人血清中相似,最低杀菌浓度也是如此。接种量从10⁵增加到10⁷菌落形成单位会增加抑制所需的浓度。替莫西林可抑制对氨苄西林、替卡西林、头孢唑林、头孢孟多和头孢西丁耐药的菌株。大多数铜绿假单胞菌菌株以及其他假单胞菌属和不动杆菌属菌株耐药,革兰氏阳性菌也耐药。替莫西林不会被常见的质粒和染色体β-内酰胺酶水解,但可抑制它们。某些革兰氏阴性杆菌对替莫西林的耐药性似乎是由于该分子无法穿过细胞壁进入细胞,因为替莫西林与EDTA联合使用可使假单胞菌、不动杆菌和肠杆菌菌株对低浓度的该化合物敏感。