Jacobs M R, Aronoff S C, Johenning S, Shlaes D M, Yamabe S
Antimicrob Agents Chemother. 1986 Jun;29(6):980-5. doi: 10.1128/AAC.29.6.980.
The in vitro synergistic activities of the beta-lactamase inhibitors YTR 830, clavulanate, and sulbactam, combined with ampicillin, ticarcillin, mezlocillin, azlocillin, piperacillin, and apalcillin, were determined against 34 strains of members of the Enterobacteriaceae family, Pseudomonas aeruginosa, Aeromonas hydrophila, and Haemophilus influenzae with characterized plasmid or chromosomal beta-lactamases or both. Strains were tested against fixed concentrations of beta-lactamase inhibitors (8 micrograms/ml) combined with doubling dilutions of beta-lactams. Synergy was defined as a fourfold or greater decrease in the MIC of the beta-lactam. Against Enterobacteriaceae producing Richmond and Sykes class III and V plasmid-mediated beta-lactamases, synergy was obtained against most strains with YTR 830- and clavulanate-beta-lactam combinations, with sulbactam being less effective. Against Enterobacteriaceae producing class I chromosomal beta-lactamases, combinations containing YTR 830 or sulbactam were more synergistic than combinations containing clavulanate. Against strains producing class V PSE enzymes, all three inhibitors were synergistic with piperacillin and apalcillin against strains producing PSE-1, -3, and -4 enzymes, while the PSE-2-producing strain was resistant to all inhibitors. YTR 830-beta-lactam combinations were also synergistic against strains producing the novel beta-lactamases OHIO-1, TLE-1, AER-1, and ROB-1. Overall, YTR 830 with piperacillin or apalcillin was the most effective combination.
测定了β-内酰胺酶抑制剂YTR 830、克拉维酸和舒巴坦与氨苄西林、替卡西林、美洛西林、阿洛西林、哌拉西林和阿帕西林联合使用时,对34株具有特征性质粒或染色体β-内酰胺酶或两者皆有的肠杆菌科成员、铜绿假单胞菌、嗜水气单胞菌和流感嗜血杆菌的体外协同活性。将菌株分别与固定浓度(8微克/毫升)的β-内酰胺酶抑制剂及双倍稀释的β-内酰胺进行测试。协同作用定义为β-内酰胺的最低抑菌浓度(MIC)降低四倍或更多。对于产生里士满和赛克斯III类及V类质粒介导的β-内酰胺酶的肠杆菌科细菌,YTR 830与β-内酰胺的组合以及克拉维酸与β-内酰胺的组合对大多数菌株有协同作用,舒巴坦的效果较差。对于产生I类染色体β-内酰胺酶的肠杆菌科细菌,含YTR 830或舒巴坦的组合比含克拉维酸的组合更具协同作用。对于产生V类PSE酶的菌株,所有三种抑制剂与哌拉西林和阿帕西林联合使用时,对产生PSE-1、-3和-4酶的菌株有协同作用,而产生PSE-2的菌株对所有抑制剂均耐药。YTR 830与β-内酰胺的组合对产生新型β-内酰胺酶OHIO-1、TLE-1、AER-1和ROB-1的菌株也有协同作用。总体而言,YTR 830与哌拉西林或阿帕西林的组合是最有效的组合。