Department of Pharmacokinetics & Pharmacodynamics, Gause Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia.
Antimicrob Agents Chemother. 2012 Mar;56(3):1223-8. doi: 10.1128/AAC.05964-11. Epub 2011 Dec 27.
To compare the antipseudomonal efficacy of doripenem and imipenem as well as their abilities to restrict the enrichment of resistant Pseudomonas aeruginosa, multiple-dosing regimens of each drug were simulated at comparable values of the cumulative percentages of a 24-h period that the drug concentration exceeds the MIC under steady-state pharmacokinetic conditions (T(>MIC)) and ratios of the 24-hour area under the curve (AUC(24)) to the MIC. Three clinical isolates of ciprofloxacin-resistant P. aeruginosa (MIC of doripenem, 1 μg/ml; MICs of imipenem, 1, 2, and 2 μg/ml) were exposed to thrice-daily doripenem or imipenem for 3 days at AUC(24)/MIC ratios of from 50 to 170 h (doripenem) and from 30 to 140 h (imipenem). The antimicrobial effects for susceptible and resistant subpopulations of bacteria were expressed by the areas between control growth and time-kill curves (I(E)s) and areas under the bacterial mutant concentration curves (AUBC(M)s), respectively. With each antibiotic, the I(E) and AUBC(M) versus log AUC(24)/MIC relationships were bacterial strain independent. At similar AUC(24)/MIC ratios, doripenem was slightly less efficient than imipenem against susceptible and resistant subpopulations of bacteria. However, doripenem appeared to be somewhat more efficient than imipenem at clinically achievable AUC(24)s related to the means of the MICs for the three studied strains and had higher antimutant potentials for two of the three strains.
为了比较多利培南与亚胺培南的抗假单胞菌疗效及其对耐药铜绿假单胞菌富集的抑制能力,在稳态药代动力学条件下(T(>MIC)),模拟了两种药物的多次给药方案,使药物浓度超过 MIC 的 24 小时累积百分比(T(>MIC))与 24 小时 AUC(24)与 MIC 的比值(AUC(24)/MIC)值相当。将三种临床分离的环丙沙星耐药铜绿假单胞菌(多利培南 MIC,1μg/ml;亚胺培南 MICs,1、2 和 2μg/ml)暴露于每日三次的多利培南或亚胺培南治疗 3 天,AUC(24)/MIC 比值为 50 至 170 h(多利培南)和 30 至 140 h(亚胺培南)。细菌敏感和耐药亚群的抗菌效果分别用对照生长和时间杀伤曲线之间的区域(I(E)s)和细菌突变体浓度曲线下的区域(AUBC(M)s)表示。对于每种抗生素,I(E)和 AUBC(M)与 log AUC(24)/MIC 之间的关系与细菌株无关。在相似的 AUC(24)/MIC 比值下,多利培南对敏感和耐药亚群的细菌的疗效略低于亚胺培南。然而,多利培南在与三种研究菌株 MIC 的平均值相关的临床可达到 AUC(24)下,似乎比亚胺培南更有效,并且对三种菌株中的两种具有更高的抗突变潜力。