Research Progress on the Pharmacological Characteristics and Organ Protective Mechanisms of Remimazolam

目的：瑞马唑仑是一种新型超短效苯二氮䓬类药物，通过高选择性结合γ-氨基丁酸A型受体(GABAA受体)发挥快速、可控的镇静作用，其羧酸酯酶依赖代谢途径避免了肝药酶介导的药物相互作用。药代动力学显示其分布快、清除率高，且不受年龄或轻中度肝肾功能影响。瑞马唑仑展现出多器官保护潜力，包括通过抑制炎症反应、激活抗氧化通路和调节凋亡/焦亡减轻脑、心、肺、肝肾损伤，并通过脊髓GABA能突触调控缓解神经痛。总之，瑞马唑仑兼具理想麻醉药物特性和多靶点器官保护功能，在围术期器官保护、危重症镇静等领域具有重要应用前景。未来研究需进一步验证其临床转化价值。Objective: Remimazolam is a novel ultra-short-acting benzodiazepine that exerts rapid and controllable sedative effects through highly selective binding to γ-aminobutyric acid type A receptors (GABAA receptors). Its carboxylesterase-dependent metabolic pathway avoids drug-drug interactions mediated by hepatic enzymes. Pharmacokinetic studies demonstrate rapid distribution, high clearance rate, and unaffected metabolism by age or mild-to-moderate hepatic/renal impairment. Remimazolam exhibits multi-organ protective potential, including mitigating brain, heart, lung, liver, and kidney injuries by suppressing inflammatory responses, activating antioxidant pathways, and regulating apoptosis/pyroptosis, as well as alleviating neuropathic pain via spinal GABAergic synaptic modulation. In summary, remimazolam combines ideal anesthetic properties with multi-target organ protection, showing significant application prospects in perioperative organ protection and critical care sedation. Future research should further validate its clinical translation value.