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新型镇静药瑞马唑仑药代动力学及药效学研究进展

Research progress in pharmacokinetics and pharmacodynamics of remimazolam-a new sedative
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摘要 瑞马唑仑是一种新型超短效苯二氮[艹卓]类镇静药,起效迅速,作用持续时间短,复苏快,作用持续时间可预测,且可被氟马西尼逆转。瑞马唑仑具有线性药代动力学特征,体内分布容积小,清除率高,半衰期短,连续输注后几乎无蓄积,主要在肝脏通过酯酶水解分裂生成无活性代谢产物CNS7054后经尿液排泄,与经CYP450酶代谢的药物发生相互作用的可能性较小。本文对瑞马唑仑的药代动力学及药效学研究概况进行系统综述,旨在为其临床合理用药提供参考。 Remimazolam is an ultra-short-acting benzodiazepine sedative with a favorable pharmacological profile including rapid onset and offset of sedation and a predictable duration of action.Its pharmacological effects can be quickly reversed by flumazenil.The pharmacokinetics of remimazolam is characterized by being dose proportional with small steady-state volume of distribution,relatively high clearance rate,short elimination half-life and minimal tissue accumulation after continuous infusion.Remimazolam is mainly metabolized via esterases in the liver and results in the formation of inactive metabolite CNS7054 which is subsequently excreted in the urine,and it has a low potential for drug-drug interactions with drugs metabolized by cytochrome P450 enzymes.This paper reviews the research progress in the pharmacokinetics and pharmacodynamics of remimazolam,aiming to provide references for its rational clinical application.
作者 袁君晓寒 白晓峰 张霞 Yuan Junxiaohan;Bai Xiaofeng;Zhang Xia(Department of Anesthesiology,Dalian Medical University,Dalian 116044,China;Stomatology Hospital of Zhejiang University School of Medicine,School of Stomatology of Zhejiang University,Zhejiang Provincial Clinical Research Center for Oral Diseases,Key Laboratory of Oral Biomedical Research of Zhejiang Province,Cancer Center of Zhejiang University,Engineering Research Center of Oral Biomaterials and Devices of Zhejiang Province,Hangzhou 310016,China)
出处 《实用药物与临床》 CAS 2024年第3期216-221,共6页 Practical Pharmacy and Clinical Remedies
基金 辽宁省自然科学基金指导计划立项项目(2021-MS-166)。
关键词 瑞马唑仑 药代动力学 药效动力学 镇静药 Remimazolam Pharmacokinetics Pharmacodynamics Sedative
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