Chen Qingbin, Deng Li, Jia Zhen
Department of Surgical Anesthesiology, Affiliated Hospital of Qinghai University, Xining, Qinghai, 810000, China.
Sci Rep. 2025 Jul 8;15(1):24426. doi: 10.1038/s41598-025-09447-4.
This study investigated the impact of high-altitude hypoxic environment on the pharmacokinetics and respiratory effects of remimazolam in a rat model. Forty Sprague-Dawley rats were randomly divided into plain and plateau groups, with the plateau group exposed to a simulated altitude of 5,000 m for 72 h prior to drug administration. Pharmacokinetic parameters, respiratory function, and safety profiles were evaluated following intravenous administration of remimazolam. Results showed that high-altitude exposure significantly altered remimazolam pharmacokinetics, with increased maximum plasma concentration (1368.2 ± 227.5 vs. 1025.6 ± 184.3 ng/mL), prolonged elimination half-life (63.5 ± 10.4 vs. 48.6 ± 8.2 min), and reduced clearance (0.89 ± 0.16 vs. 1.26 ± 0.24 L/h/kg) in the plateau group compared to the plain group. The plateau group also exhibited more pronounced respiratory depression, with greater decreases in PaO₂ and oxygen saturation, and higher incidence of adverse reactions. These findings suggest that high-altitude hypoxic environment significantly impacts remimazolam pharmacokinetics and respiratory effects, necessitating careful dose adjustment and monitoring in high-altitude clinical settings.
本研究在大鼠模型中探究了高海拔低氧环境对瑞马唑仑药代动力学及呼吸效应的影响。将40只Sprague-Dawley大鼠随机分为平原组和高原组，高原组在给药前暴露于模拟海拔5000米的环境中72小时。静脉注射瑞马唑仑后评估药代动力学参数、呼吸功能和安全性。结果显示，与平原组相比，高原组暴露于高海拔环境显著改变了瑞马唑仑的药代动力学，最大血浆浓度升高（1368.2±227.5 vs. 1025.6±184.3 ng/mL），消除半衰期延长（63.5±10.4 vs. 48.6±8.2分钟），清除率降低（0.89±0.16 vs. 1.
