Department of Pediatrics, Duke University, Durham, North Carolina, USA.
Duke Clinical Research Institute, Durham, North Carolina, USA.
Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0153323. doi: 10.1128/aac.01533-23. Epub 2024 Mar 14.
Pharmacokinetic models rarely undergo external validation in vulnerable populations such as critically ill infants, thereby limiting the accuracy, efficacy, and safety of model-informed dosing in real-world settings. Here, we describe an opportunistic approach using dried blood spots (DBS) to evaluate a population pharmacokinetic model of metronidazole in critically ill preterm infants of gestational age (GA) ≤31 weeks from the Metronidazole Pharmacokinetics in Premature Infants (PTN_METRO, NCT01222585) study. First, we used linear correlation to compare 42 paired DBS and plasma metronidazole concentrations from 21 preterm infants [mean (SD): post natal age 28.0 (21.7) days, GA 26.3 (2.4) weeks]. Using the resulting predictive equation, we estimated plasma metronidazole concentrations (ePlasma) from 399 DBS collected from 122 preterm and term infants [mean (SD): post natal age 16.7 (15.8) days, GA 31.4 (5.1) weeks] from the Antibiotic Safety in Infants with Complicated Intra-Abdominal Infections (SCAMP, NCT01994993) trial. When evaluating the PTN_METRO model using ePlasma from the SCAMP trial, we found that the model generally predicted ePlasma well in preterm infants with GA ≤31 weeks. When including ePlasma from term and preterm infants with GA >31 weeks, the model was optimized using a sigmoidal Emax maturation function of postmenstrual age on clearance and estimated the exponent of weight on volume of distribution. The optimized model supports existing dosing guidelines and adds new data to support a 6-hour dosing interval for infants with postmenstrual age >40 weeks. Using an opportunistic DBS to externally validate and optimize a metronidazole population pharmacokinetic model was feasible and useful in this vulnerable population.
药代动力学模型很少在脆弱人群(如危重症婴儿)中进行外部验证,从而限制了模型指导下的给药在实际环境中的准确性、有效性和安全性。在这里,我们描述了一种使用干血斑(DBS)的机会性方法,以评估一项来自 Metronidazole Pharmacokinetics in Premature Infants(PTN_METRO,NCT01222585)研究的关于甲硝唑在胎龄(GA)≤31 周的危重症早产儿中的群体药代动力学模型。首先,我们使用线性相关性比较了来自 21 名早产儿的 42 对 DBS 和血浆甲硝唑浓度[平均(SD):出生后年龄 28.0(21.7)天,GA 26.3(2.4)周]。使用得出的预测方程,我们从来自 122 名早产儿和足月儿的 399 个 DBS 中估计了血浆甲硝唑浓度(ePlasma)[平均(SD):出生后年龄 16.7(15.8)天,GA 31.4(5.1)周]来自复杂性腹腔内感染婴儿抗生素安全性(SCAMP,NCT01994993)试验。当使用来自 SCAMP 试验的 ePlasma 评估 PTN_METRO 模型时,我们发现该模型通常能很好地预测 GA≤31 周的早产儿的 ePlasma。当包括 GA>31 周的足月儿和早产儿的 ePlasma 时,模型使用基于月经后年龄的 Emax 成熟函数对清除率进行优化,并估计了体积分布的体重指数。优化后的模型支持现有的给药指南,并增加了新的数据以支持月经后年龄>40 周的婴儿 6 小时给药间隔。在这个脆弱的人群中,使用机会性 DBS 来外部验证和优化甲硝唑群体药代动力学模型是可行和有用的。