Division of Pharmacokinetics and Pharmacodynamics, Department of Pharmacology, Toxicology and Therapeutics, School of Pharmacy, Showa University, Tokyo, Japan.
Department of Pharmacy, Japan Community Health Care Organization Tokyo Takanawa Hospital, Tokyo, Japan.
Pharmacol Res Perspect. 2021 Apr;9(2):e00746. doi: 10.1002/prp2.746.
This study sought to investigate whether dosing frequency (the number of doses per day) affects the antimicrobial efficacy and safety of ampicillin/sulbactam (ABPC/SBT) in Japanese elderly pneumonia patients treated with ABPC/SBT at 6 g/day. This was a retrospective observational study that included hospitalized elderly patients (aged ≥75 years, 10 ml/min ≤CLcr <50 ml/min) who received 3 g every 12 h (BID; n = 61) or 1.5 g every 6 h (QID; n = 45) for the treatment of pneumonia. The primary endpoint was clinical response, assessed by measuring body temperature, white blood cell count, and C-reactive protein levels. Pharmacokinetic and pharmacodynamic simulations were conducted in silico to rationalize the clinical findings. The clinical response rates (extremely effective and effective) in the BID and QID groups were 36.1% and 55.6%, respectively (p = .0459). QID tended to be more effective in patients with gram-negative rods detected (p = .0563). According to the simulated minimum plasma ABPC concentrations at steady state for BID and QID were 2.5 and 7.3 μg/ml, respectively (p < .0001). Based on the simulated time above minimum inhibitory concentration (MIC), pharmacological (not clinical) efficacy was predicted to be higher with QID. Both groups had similar safety profiles. The main adverse event in both groups was liver damage. The present retrospective survey demonstrated that ABPC/SBT treatment for elderly patients with pneumonia and renal dysfunction was more effective with QID than with BID. Therefore, the QID regimen is worthy of consideration to improve the clinical outcomes of ABPC/SBT therapy in the present patient population.
这项研究旨在探讨剂量频率(每天给药次数)是否会影响氨苄西林/舒巴坦(ABPC/SBT)在接受 ABPC/SBT 6 g/天治疗的日本老年肺炎患者中的抗菌疗效和安全性。这是一项回顾性观察性研究,纳入了接受 ABPC/SBT 3 g 每 12 小时(BID;n=61)或 1.5 g 每 6 小时(QID;n=45)治疗肺炎的住院老年患者(年龄≥75 岁,CLcr 10 ml/min≤<50 ml/min)。主要终点是通过测量体温、白细胞计数和 C 反应蛋白水平评估的临床反应。通过计算机模拟进行药代动力学和药效动力学研究,以合理化临床发现。BID 和 QID 组的临床反应率(极有效和有效)分别为 36.1%和 55.6%(p=0.0459)。QID 在检测到革兰氏阴性菌的患者中更有效(p=0.0563)。根据 BID 和 QID 的稳态最小血浆 ABPC 浓度模拟值,分别为 2.5 和 7.3 μg/ml(p<0.0001)。根据模拟的高于最低抑菌浓度(MIC)的时间,预测 QID 的药效学(非临床)疗效更高。两组的安全性特征相似。两组的主要不良事件均为肝损伤。本回顾性调查表明,对于肾功能不全的老年肺炎患者,ABPC/SBT 治疗 QID 比 BID 更有效。因此,QID 方案值得考虑,以改善当前患者群体中 ABPC/SBT 治疗的临床结局。