Department of Infection, Inflammation and Rheumatology, Great Ormond Street Institute of Child Health, University College London, London, UK.
Department of Pharmaceutical Biosciences, Uppsala University, Uppsala, Sweden.
J Antimicrob Chemother. 2018 Jul 1;73(7):1908-1916. doi: 10.1093/jac/dky128.
Sepsis and bacterial meningitis are major causes of mortality and morbidity in neonates and infants. Meropenem, a broad-spectrum antibiotic, is not licensed for use in neonates and infants below 3 months of age and sufficient information on its plasma and CSF disposition and dosing in neonates and infants is lacking.
To determine plasma and CSF pharmacokinetics of meropenem in neonates and young infants and the link between pharmacokinetics and clinical outcomes in babies with late-onset sepsis (LOS).
Data were collected in two recently conducted studies, i.e. NeoMero-1 (neonatal LOS) and NeoMero-2 (neonatal meningitis). Optimally timed plasma samples (n = 401) from 167 patients and opportunistic CSF samples (n = 78) from 56 patients were analysed.
A one-compartment model with allometric scaling and fixed maturation gave adequate fit to both plasma and CSF data; the CL and volume (standardized to 70 kg) were 16.7 (95% CI 14.7, 18.9) L/h and 38.6 (95% CI 34.9, 43.4) L, respectively. CSF penetration was low (8%), but rose with increasing CSF protein, with 40% penetration predicted at a protein concentration of 6 g/L. Increased infusion time improved plasma target attainment, but lowered CSF concentrations. For 24 patients with culture-proven Gram-negative LOS, pharmacodynamic target attainment was similar regardless of the test-of-cure visit outcome.
Simulations showed that longer infusions increase plasma PTA but decrease CSF PTA. CSF penetration is worsened with long infusions so increasing dose frequency to achieve therapeutic targets should be considered.
败血症和细菌性脑膜炎是新生儿和婴儿死亡和发病的主要原因。美罗培南是一种广谱抗生素,未获准用于 3 个月以下的新生儿和婴儿,且缺乏其在新生儿和婴儿中的血浆和脑脊液分布及剂量方面的充分信息。
确定美罗培南在新生儿和婴儿中的血浆和脑脊液药代动力学,以及药代动力学与迟发型败血症(LOS)婴儿临床结局之间的关系。
数据来自最近进行的两项研究,即 NeoMero-1(新生儿 LOS)和 NeoMero-2(新生儿脑膜炎)。对 167 例患者的最佳时间点血浆样本(n = 401)和 56 例患者的机会性脑脊液样本(n = 78)进行了分析。
采用同种异体缩放和固定成熟的单室模型对血浆和脑脊液数据均具有良好的拟合度;CL 和标准化至 70 kg 的体积分别为 16.7(95% CI 14.7,18.9)L/h 和 38.6(95% CI 34.9,43.4)L。CSF 穿透率较低(8%),但随着 CSF 蛋白浓度的增加而升高,当蛋白浓度为 6 g/L 时,预测穿透率为 40%。增加输注时间可提高血浆靶目标达标率,但降低 CSF 浓度。对于 24 例经培养证实的革兰氏阴性 LOS 患者,无论治愈测试的结果如何,药代动力学靶目标达标率相似。
模拟结果表明,延长输注时间可增加血浆 PTA,但降低 CSF PTA。长时间输注会使 CSF 穿透率恶化,因此应考虑增加剂量频率以达到治疗目标。