Barber Katie E, Werth Brian J, Ireland Cortney E, Stone Nicole E, Nonejuie Poochit, Sakoulas George, Pogliano Joseph, Rybak Michael J
Anti-Infective Research Laboratory, Eugene Applebaum College of Pharmacy and Health Sciences, Detroit, MI 48201, USA.
University of California San Diego, Division of Biology, La Jolla, CA 92093, USA.
J Antimicrob Chemother. 2014 Nov;69(11):3006-10. doi: 10.1093/jac/dku236. Epub 2014 Jul 1.
Ceftobiprole is a broad-spectrum cephalosporin that demonstrates activity against Staphylococcus aureus resistant to methicillin, including strains with reduced susceptibility to glycopeptides and lipopeptides. The addition of this agent provides a potential therapeutic option for difficult-to-treat infections. Synergy has been demonstrated between β-lactams combined with glycopeptides and lipopeptides against S. aureus. This study sought to determine whether ceftobiprole was synergistic with daptomycin, vancomycin or standard-of-care combination agents (gentamicin or rifampicin) against methicillin-resistant S. aureus (MRSA) strains with varying degrees of vancomycin susceptibility.
Broth microdilution MICs of ceftobiprole, daptomycin, vancomycin, rifampicin and gentamicin were evaluated for 20 MRSA isolates. Combination MICs were additionally evaluated in the presence of subinhibitory concentrations of ceftobiprole to assess synergism. Time-kill curves for five representative isolates were performed utilizing combinations of ceftobiprole plus daptomycin, vancomycin, rifampicin and gentamicin to further quantify the degree of synergy for each regimen.
Ceftobiprole plus daptomycin represented the most potent combination with a 4-fold decrease in MIC and synergy against all strains evaluated in time-kill evaluations. Additionally, binding studies demonstrated enhanced daptomycin binding in the presence of subinhibitory concentrations of ceftobiprole.
The use of combination therapy with ceftobiprole may provide a needed addition for the treatment of Gram-positive infections resistant to daptomycin or vancomycin. Consistent with what has been observed with other β-lactams, ceftobiprole increased bodipy-tagged daptomycin binding on the surface of S. aureus, potentially explaining this potent synergy observed in time-kill evaluations. More detailed evaluation of ceftobiprole is warranted to better characterize observed synergy.
头孢比普是一种广谱头孢菌素,对耐甲氧西林金黄色葡萄球菌具有活性,包括对糖肽类和脂肽类敏感性降低的菌株。添加这种药物为难治性感染提供了一种潜在的治疗选择。β-内酰胺类与糖肽类和脂肽类联合使用对金黄色葡萄球菌已显示出协同作用。本研究旨在确定头孢比普与达托霉素、万古霉素或标准治疗联合用药(庆大霉素或利福平)对不同程度万古霉素敏感性的耐甲氧西林金黄色葡萄球菌(MRSA)菌株是否具有协同作用。
对20株MRSA分离株评估头孢比普、达托霉素、万古霉素、利福平和庆大霉素的肉汤微量稀释MIC。在亚抑菌浓度的头孢比普存在下额外评估联合MIC,以评估协同作用。利用头孢比普加达托霉素、万古霉素、利福平和庆大霉素的组合对5株代表性分离株进行时间杀菌曲线测定,以进一步量化每种方案的协同程度。
头孢比普加达托霉素是最有效的组合,MIC降低4倍,且在时间杀菌评估中对所有评估菌株均有协同作用。此外,结合研究表明,在亚抑菌浓度的头孢比普存在下,达托霉素的结合增强。
联合使用头孢比普治疗可能为治疗对达托霉素或万古霉素耐药的革兰氏阳性感染提供必要补充。与其他β-内酰胺类药物观察到的情况一致,头孢比普增加了金黄色葡萄球菌表面硼二吡咯标记的达托霉素结合,这可能解释了在时间杀菌评估中观察到的这种强效协同作用。有必要对头孢比普进行更详细的评估,以更好地表征观察到的协同作用。