Vuye A, Pijck J
Antimicrob Agents Chemother. 1985 Apr;27(4):574-7. doi: 10.1128/AAC.27.4.574.
The in vitro activity of BMY-28142 was compared with that of cefotaxime, ceftazidime, moxalactam, and imipenem against 639 clinical isolates and a number of in vitro-selected resistant mutants. BMY-28142 was the most potent compound against the members of the family Enterobacteriaceae with a MIC for 90% of the strains of 0.12 micrograms/ml. The activity against Pseudomonas aeruginosa was comparable to that of ceftazidime and imipenem. Strains of staphylococci were moderately susceptible to BMY-28142 (MIC required to inhibit 90% of strains, 4 micrograms/ml), but Streptococcus faecalis isolates were resistant. The activity of the five compounds was inoculum dependent for several gram-negative species. By a single-step selection procedure, resistant mutants were selected from strains of Citrobacter freundii, Enterobacter cloacae, and P. aeruginosa. The mutant frequencies with the cephalosporins, including BMY-28142, ranged between 10(-6) and 10(-8). BMY-28142 was the most active cephalosporin against these resistant organisms, most of them strong beta-lactamase producers. It inhibited all mutants of C. freundii and E. cloacae at 2 micrograms/ml and all mutants of P. aeruginosa at 32 micrograms/ml. Imipenem on the other hand was as active on all of these resistant organisms as on the parent strains.
将BMY - 28142的体外活性与头孢噻肟、头孢他啶、拉氧头孢和亚胺培南针对639株临床分离菌及一些体外选择的耐药突变株进行了比较。BMY - 28142是针对肠杆菌科成员最有效的化合物,90%菌株的最低抑菌浓度(MIC)为0.12微克/毫升。其对铜绿假单胞菌的活性与头孢他啶和亚胺培南相当。葡萄球菌菌株对BMY - 28142中度敏感(抑制90%菌株所需的MIC为4微克/毫升),但粪肠球菌分离株耐药。对于几种革兰阴性菌,这五种化合物的活性均与接种量有关。通过单步选择程序,从弗氏柠檬酸杆菌、阴沟肠杆菌和铜绿假单胞菌菌株中筛选出耐药突变株。包括BMY - 28142在内的头孢菌素的突变频率在10^(-6)至10^(-8)之间。BMY - 28142是针对这些耐药菌最具活性的头孢菌素,其中大多数是强效β-内酰胺酶产生菌。它在2微克/毫升时抑制所有弗氏柠檬酸杆菌和阴沟肠杆菌突变株,在32微克/毫升时抑制所有铜绿假单胞菌突变株。另一方面,亚胺培南对所有这些耐药菌的活性与对亲本菌株的活性相同。