Department of Medical Microbiology, Amsterdam UMC, University of Amsterdam, Meibergdreef 9, 1105 AZ, Amsterdam, The Netherlands.
Division of Infectious Diseases, Department of Internal Medicine, Amsterdam UMC, University of Amsterdam, Meibergdreef 9, 1105 AZ, Amsterdam, The Netherlands.
Clin Pharmacokinet. 2022 Aug;61(8):1075-1094. doi: 10.1007/s40262-022-01143-0. Epub 2022 Jun 27.
Gentamicin is an aminoglycoside antibiotic with a small therapeutic window that is currently used primarily as part of short-term empirical combination therapy. Gentamicin dosing schemes still need refinement, especially for subpopulations where pharmacokinetics can differ from pharmacokinetics in the general adult population: obese patients, critically ill patients, paediatric patients, neonates, elderly patients and patients on dialysis. This review summarizes the clinical pharmacokinetics of gentamicin in these patient populations and the consequences for optimal dosing of gentamicin for infections caused by Gram-negative bacteria, highlighting new insights from the last 10 years. In this period, several new population pharmacokinetic studies have focused on these subpopulations, providing insights into the typical values of the most relevant pharmacokinetic parameters, the variability of these parameters and possible explanations for this variability, although unexplained variability often remains high. Both dosing schemes and pharmacokinetic/pharmacodynamic (PK/PD) targets varied widely between these studies. A gentamicin starting dose of 7 mg/kg based on total body weight (or on adjusted body weight in obese patients) appears to be the optimal strategy for increasing the probability of target attainment (PTA) after the first administration for the most commonly used PK/PD targets in adults and children older than 1 month, including critically ill patients. However, evidence that increasing the PTA results in higher efficacy is lacking; no studies were identified that show a correlation between estimated or predicted PK/PD target attainment and clinical success. Although it is unclear if performing therapeutic drug monitoring (TDM) for optimization of the PTA is of clinical value, it is recommended in patients with highly variable pharmacokinetics, including patients from all subpopulations that are critically ill (such as elderly, children and neonates) and patients on intermittent haemodialysis. In addition, TDM for optimization of the dosing interval, targeting a trough concentration of at least < 2 mg/L but preferably < 0.5-1 mg/L, has proven to reduce nephrotoxicity and is therefore recommended in all patients receiving more than one dose of gentamicin. The usefulness of the daily area under the plasma concentration-time curve for predicting nephrotoxicity should be further investigated. Additionally, more research is needed on the optimal PK/PD targets for efficacy in the clinical situations in which gentamicin is currently used, that is, as monotherapy for urinary tract infections or as part of short-term combination therapy.
庆大霉素是一种氨基糖苷类抗生素,治疗窗较窄,目前主要作为短期经验性联合治疗的一部分。庆大霉素的给药方案仍需完善,特别是在药代动力学与普通成年人群不同的亚人群中:肥胖患者、危重症患者、儿科患者、新生儿、老年患者和透析患者。本综述总结了这些患者人群中庆大霉素的临床药代动力学特征,以及这些患者人群中感染革兰氏阴性菌时最佳庆大霉素剂量的后果,重点介绍了过去 10 年的新见解。在此期间,几项新的群体药代动力学研究集中在这些亚人群,深入了解了最相关药代动力学参数的典型值、这些参数的可变性以及这种可变性的可能解释,尽管未解释的可变性仍然很高。这些研究之间的剂量方案和药代动力学/药效学(PK/PD)目标差异很大。对于最常用于成人和 1 个月以上儿童的 PK/PD 目标,包括危重症患者,基于总体重(或肥胖患者的调整后体重)的 7mg/kg 起始剂量似乎是增加首次给药后目标达到率(PTA)的最佳策略。然而,尚无证据表明增加 PTA 可提高疗效;未发现研究表明估计或预测的 PK/PD 目标达到率与临床成功之间存在相关性。虽然尚不清楚是否需要进行治疗药物监测(TDM)以优化 PTA 是否具有临床价值,但在药代动力学高度可变的患者中,包括所有处于危急状态的亚人群患者(如老年、儿童和新生儿)和间歇性血液透析患者,建议进行 TDM。此外,优化给药间隔的 TDM,目标为谷浓度至少<2mg/L,但最好<0.5-1mg/L,已被证明可降低肾毒性,因此建议所有接受超过一剂庆大霉素的患者进行 TDM。还需要进一步研究预测庆大霉素肾毒性的血浆浓度时间曲线下面积的日值的用途。此外,还需要对庆大霉素目前用于治疗的临床情况下的最佳 PK/PD 目标进行更多研究,即用于治疗尿路感染的单药治疗或作为短期联合治疗的一部分。