Tsuji Brian T, Rybak Michael J
Anti-Infective Research Laboratory, Department of Pharmacy Practice, Eugene Applebaum College of Pharmacy and Health Sciences, Detroit, Michigan 48201, USA.
Antimicrob Agents Chemother. 2005 Jul;49(7):2735-45. doi: 10.1128/AAC.49.7.2735-2745.2005.
The ability to maximize bactericidal activity while minimizing toxicity is a therapeutic goal in the treatment of infective endocarditis. We evaluated the impact of administering short-course regimens of gentamicin in combination with daptomycin or vancomycin against one methicillin-susceptible (MSSA 1199) and one methicillin-resistant (MRSA 494) Staphylococcus aureus isolate using an in vitro pharmacodynamic model with simulated endocardial vegetations over 96 h. Human therapeutic dosing regimens for daptomycin (6 and 8 mg/kg of body weight), vancomycin, and gentamicin were simulated. Short-course combination regimens involving gentamicin were administered either as a single 5-mg/kg dose or three 1-mg/kg doses for only the first 24 h and compared to the regimens administered for the full 96-h duration. For all experiments, physiologic conditions of albumin, calcium, and pH were simulated. Both regimens of daptomycin achieved 99.9% kill by 32 h and maintained bactericidal activity against both isolates, which was significantly different from vancomycin, which displayed bacteriostatic activity (P < 0.05). The effects of all short-course regimens of gentamicin were equal to those of the full-duration regimens in combination with daptomycin. Adding three doses of gentamicin (1 mg/kg) to daptomycin resulted in enhancement and bactericidal activity at 24 h against both MRSA and MSSA. The addition of a single dose of gentamicin (5 mg/kg) enhanced or improved the activity of daptomycin and resulted in early bactericidal activity at 4 h against both isolates. The addition of three doses of gentamicin (1 mg/kg) did not improve the activity of vancomycin. However, the addition of a single 5-mg/kg dose of gentamicin to vancomycin resulted in early enhancement at 4 h and 99.9% kill at 32 h for MRSA. These results suggest that a single high dose of gentamicin in combination with daptomycin or vancomycin may be of utility to maximize synergistic and bactericidal activity and minimize toxicity. Further investigation is warranted.
在治疗感染性心内膜炎时,将杀菌活性最大化同时使毒性最小化是一个治疗目标。我们使用体外药效学模型,在96小时内模拟心内膜赘生物,评估了庆大霉素短疗程方案联合达托霉素或万古霉素对一株甲氧西林敏感金黄色葡萄球菌(MSSA 1199)和一株甲氧西林耐药金黄色葡萄球菌(MRSA 494)的影响。模拟了达托霉素(6和8mg/kg体重)、万古霉素和庆大霉素的人类治疗给药方案。涉及庆大霉素的短疗程联合方案,要么仅在前24小时给予单次5mg/kg剂量,要么给予三次1mg/kg剂量,并与全程96小时给药方案进行比较。对于所有实验,模拟了白蛋白、钙和pH的生理条件。两种达托霉素方案在32小时时均实现了99.9%的杀灭率,并对两种菌株均保持杀菌活性,这与显示抑菌活性的万古霉素有显著差异(P<0.05)。庆大霉素所有短疗程方案的效果与联合达托霉素的全程方案效果相当。在达托霉素中添加三剂庆大霉素(1mg/kg)可增强并在24小时时对MRSA和MSSA产生杀菌活性。添加单剂庆大霉素(5mg/kg)可增强达托霉素的活性,并在4小时时对两种菌株产生早期杀菌活性。添加三剂庆大霉素(1mg/kg)并未改善万古霉素的活性。然而,在万古霉素中添加单剂5mg/kg庆大霉素可在4小时时早期增强活性,并在32小时时对MRSA实现99.9%的杀灭率。这些结果表明,单剂高剂量庆大霉素联合达托霉素或万古霉素可能有助于使协同和杀菌活性最大化并使毒性最小化。有必要进行进一步研究。