Rybak M J, Bailey E M, Lamp K C, Kaatz G W
College of Pharmacy and Allied Health Professions, Wayne State University, Detroit, Michigan.
Antimicrob Agents Chemother. 1992 May;36(5):1109-14. doi: 10.1128/AAC.36.5.1109.
The pharmacokinetics and bactericidal killing rates (BR) of daptomycin (D) and vancomycin (V) in 12 intravenous drug abusers (6 treated with daptomycin and 6 treated with vancomycin) were evaluated. Pharmacokinetic parameters were determined from multiple serum samples drawn at steady state over a 12-h dosing interval after intravenous infusions of 3 mg of D per kg of body weight and 1,000 mg of V. The BRs were determined from the 1- and 6-h serum samples by using four isolates of Staphylococcus aureus (three methicillin susceptible and one methicillin resistant) obtained from the patients enrolled in the study. Peak serum daptomycin concentrations were lower and volumes of distribution were higher than reported in healthy volunteers. Although not statistically different, D clearance was 22% higher than reported in healthy volunteers. V pharmacokinetics were similar to those reported in previous studies. Daptomycin's BRs, although comparable to those of V in patients' serum, were significantly decreased compared with those found in broth. This may be related to the high degree of protein binding of D (93% versus 50% for V). Conversely, the BRs of V in serum were significantly greater than those in broth. The BRs of D and V in broth were greater when killing curves were performed with test strains in logarithmic versus stationary-phase growth. The ability to kill organisms in stationary phase may be an important factor in determining the performance of an antibiotic in deep-seated infections such as endocarditis.3+
对12名静脉吸毒者(6名接受达托霉素治疗,6名接受万古霉素治疗)体内达托霉素(D)和万古霉素(V)的药代动力学及杀菌率(BR)进行了评估。在静脉输注每千克体重3毫克D和1000毫克V后,于12小时给药间隔的稳态下采集多个血清样本,测定药代动力学参数。通过使用从参与研究的患者中分离出的4株金黄色葡萄球菌(3株对甲氧西林敏感,1株对甲氧西林耐药),从1小时和6小时的血清样本中测定BR。血清达托霉素峰值浓度低于健康志愿者报告值,分布容积高于健康志愿者报告值。尽管无统计学差异,但D的清除率比健康志愿者报告值高22%。V的药代动力学与先前研究报告相似。达托霉素的BRs,尽管在患者血清中与V相当,但与肉汤中的BRs相比显著降低。这可能与D的高度蛋白结合(93%,而V为50%)有关。相反,V在血清中的BRs显著高于肉汤中的BRs。当用处于对数生长期与稳定期生长的测试菌株进行杀灭曲线实验时,D和V在肉汤中的BRs更高。在稳定期杀灭微生物的能力可能是决定抗生素在诸如心内膜炎等深部感染中疗效的一个重要因素。3+