Athanassa Zoe, Papakyriakopoulou Paraskevi, Marquez Megias Silvia, Saitani Elmina-Marina, Manioudaki Sofia, Dimoula Katerina, Petsa Irina, Valsami Georgia, Sakagianni Aikaterini, Koumaki Vassiliki, Dokoumetzidis Aristides, Tsakris Athanassios
Intensive Care Unit, Sismanogleio General Hospital, Athens, Greece.
Department of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece.
J Antimicrob Chemother. 2025 May 2;80(5):1420-1426. doi: 10.1093/jac/dkaf090.
Multidrug-resistant Acinetobacter baumannii (MDR-A. baumannii) has become an emerging pathogen, causing ventilator-associated pneumonia (VAP), with limited treatment options available. MIN has re-emerged as a potential treatment option for MDR pathogens. However, evidence regarding MIN pharmacokinetic properties in critically ill patients is scarce and primarily limited to IV administration. To address the knowledge gap in regions where IV MIN is unavailable, a prospective, open-label study was conducted to describe the pharmacokinetic properties of orally administered MIN.
The study included 24 critically ill patients with MDR-A. baumannii VAP. A population PK (popPK) model was developed and the PTA for different MICs was assessed by Monte Carlo simulations. A one-compartment model with first-order absorption and linear elimination best described the data.
The values of the estimated population parameters were found equal to 183.3 L, 6.55 L/h and 1.66 h⁻¹, for the apparent volume of distribution (V/F), the apparent clearance (CL/F) and the absorption rate constant (ka), respectively (F representing oral bioavailability). PTA analysis showed that for a daily dose of 400 mg, adequate exposure [free AUC/MIC (fAUC/MIC > 25)] was achieved only for MICs ≤ 0.25 mg/L, while for the ratio of fAUC/MIC = 13.75, high PTA values are calculated up to MIC = 0.5 mg/L.
This study provides a popPK model for oral MIN in critically ill adults. The developed popPK model contributes to a better understanding of MIN's PK and can inform dosing strategies and future studies on MIN use in critical care settings.
多重耐药鲍曼不动杆菌(MDR - A.baumannii)已成为一种新兴病原体,可引发呼吸机相关性肺炎(VAP),且可用的治疗选择有限。米诺环素(MIN)已重新成为治疗MDR病原体的一种潜在选择。然而,关于米诺环素在重症患者中药代动力学特性的证据稀缺,且主要限于静脉给药。为填补静脉用米诺环素无法获取地区的知识空白,开展了一项前瞻性、开放标签研究以描述口服米诺环素的药代动力学特性。
该研究纳入了24例患有MDR - A.baumannii VAP的重症患者。建立了群体药代动力学(popPK)模型,并通过蒙特卡洛模拟评估不同最低抑菌浓度(MIC)下的达标概率(PTA)。具有一级吸收和线性消除的单室模型能最好地描述数据。
对于表观分布容积(V/F)、表观清除率(CL/F)和吸收速率常数(ka),估计的群体参数值分别为183.3 L、6.55 L/h和1.66 h⁻¹(F代表口服生物利用度)。PTA分析表明,对于每日剂量400 mg,仅当MIC≤0.25 mg/L时才能实现足够的暴露[游离血药浓度-时间曲线下面积/最低抑菌浓度(fAUC/MIC>25)],而对于fAUC/MIC = 13.75的情况,计算得出直至MIC = 0.5 mg/L时均有较高的PTA值。
本研究为重症成年患者口服米诺环素提供了一个popPK模型。所建立的popPK模型有助于更好地理解米诺环素的药代动力学,并可为重症监护环境中米诺环素的给药策略及未来研究提供参考。