Cunha B A, Quintiliani R, Deglin J M, Izard M W, Nightingale C H
Rev Infect Dis. 1981 Nov-Dec;3 suppl:S269-72.
After a single 1-g intravenous dose of vancomycin, the mean peak concentration in the serum of 29 anephric patients was 48.3 micrograms/ml. An initial rapid decline to 15 micrograms/ml within 3-5 hr was followed by slow elimination, with 3.5 micrograms/ml present after 18 days. Intermittent dialysis had no appreciable effect on drug levels in serum. The biphasic decline in serum concentrations of vancomycin indicates at least two-compartment pharmacokinetics in both anephric and normal patients. In anephric patients the elimination half-life was 7.5 days and the elimination rate constant was 0.32; these values were 8 hr and 10.25, respectively, in normal patients. On the basis of these results, the vancomycin regimen recommended for anephric patients is an initial 1-g intravenous dose followed by 500 mg every eight days. With these dosages peak concentrations are 49 micrograms/ml (well below reported toxic levels) and trough concentrations are 7 micrograms/ml (well above the minimal inhibitory concentrations for susceptible pathogens causing shunt infections).
在单次静脉注射1克万古霉素后,29名无肾患者血清中的平均峰值浓度为48.3微克/毫升。最初在3至5小时内迅速下降至15微克/毫升,随后消除缓慢,18天后仍有3.5微克/毫升。间歇性透析对血清中的药物水平没有明显影响。万古霉素血清浓度的双相下降表明无肾患者和正常患者至少存在两室药代动力学。在无肾患者中,消除半衰期为7.5天,消除速率常数为0.32;在正常患者中,这些值分别为8小时和10.25。基于这些结果,推荐给无肾患者的万古霉素治疗方案是初始静脉注射1克,随后每八天注射500毫克。使用这些剂量时,峰值浓度为49微克/毫升(远低于报告的中毒水平),谷浓度为7微克/毫升(远高于引起分流感染的敏感病原体的最低抑菌浓度)。