Blaser J, Stone B B, Zinner S H
Antimicrob Agents Chemother. 1985 Mar;27(3):343-9. doi: 10.1128/AAC.27.3.343.
Several aminoglycoside dosage regimens were studied in a kinetic in vitro model. Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus were exposed in serially placed artificial capillary units to netilmicin concentrations that changed based on human two-compartment pharmacokinetics. The same total dose per 24 h was administered as a continuous infusion (3.7 micrograms/ml) or in 1-h infusions given every 24 (24 micrograms/ml) or 8 h (8 micrograms/ml). The once daily administration showed the best response in terms of either faster killing of E. coli, K. pneumoniae, and S. aureus or greater reduction of the inocula of P. aeruginosa. After 28 h of treatment, however, all regimens reduced the nonpseudomonads by more than 99.99%, whereas all three P. aeruginosa strains regrew to greater than 10(8) CFU/ml due to selection of resistant subpopulations. In contrast to the bactericidal effect of the first dose, no killing occurred after subsequent doses if the ratio of peak drug concentration to MIC was low (less than or equal to 6). These results support the concept of administering high doses of aminoglycosides once every 24 h.
在一个体外动力学模型中研究了几种氨基糖苷类药物的给药方案。将铜绿假单胞菌、大肠杆菌、肺炎克雷伯菌和金黄色葡萄球菌置于串联的人工毛细血管单元中,使其暴露于根据人体二室药代动力学变化的奈替米星浓度下。每24小时给予相同的总剂量,以持续输注(3.7微克/毫升)或每24小时(24微克/毫升)或每8小时(8微克/毫升)进行1小时输注的方式给药。就更快杀灭大肠杆菌、肺炎克雷伯菌和金黄色葡萄球菌或更大程度减少铜绿假单胞菌接种量而言,每日一次给药显示出最佳反应。然而,治疗28小时后,所有给药方案均使非铜绿假单胞菌减少超过99.99%,而由于耐药亚群的选择,所有三株铜绿假单胞菌菌株均重新生长至大于10⁸CFU/毫升。与首剂的杀菌作用相反,如果药物峰浓度与MIC的比值较低(小于或等于6),后续剂量则无杀菌作用。这些结果支持每24小时给予高剂量氨基糖苷类药物的概念。