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中国临床药理学与治疗学 ›› 2026, Vol. 31 ›› Issue (3): 352-361.doi: 10.12092/j.issn.1009-2501.2026.03.007

• 综述与讲座 • 上一篇    下一篇

奥沙西泮的药理作用及机制研究进展

王毅群1,2,*(), 王之琳1, 李清杨1, 岑文杰1, 郑乔远1, 黄志力1,2,*()   

  1. 1. 复旦大学基础医学院药理学系,上海 200032
    2. 复旦大学脑功能与脑疾病全国重点实验室,教育部脑科学前沿创新中心,复旦大学脑科学研究院,上海 200032
  • 收稿日期:2025-10-27 修回日期:2026-03-02 出版日期:2026-03-26 发布日期:2026-04-03
  • 通讯作者: 王毅群,黄志力 E-mail:yiqunwang@fudan.edu.cn;huangzl@fudan.edu.cn
  • 基金资助:
    国家自然科学基金项目(82571692,82530045);科技部国家重点研发计划(2022YFA1604504)

Research progress on the pharmacological effects and mechanisms of oxazepam

Yiqun WANG1,2,*(), Zhilin WANG1, Qingyang LI1, Wenjie CEN1, Qiaoyuan ZHENG1, Zhili HUANG1,2,*()   

  1. 1. Department of Pharmacology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China
    2. State Key Laboratory of Brain Function and Disease, Institutes of Brain Science and Collaborative Innovation Center for Brain Science, Fudan University, Shanghai 200032, China
  • Received:2025-10-27 Revised:2026-03-02 Online:2026-03-26 Published:2026-04-03
  • Contact: Yiqun WANG,Zhili HUANG E-mail:yiqunwang@fudan.edu.cn;huangzl@fudan.edu.cn

摘要:

奥沙西泮属于中短效苯二氮?类镇静催眠药,其作用机制主要通过正向变构作用调节γ-氨基丁酸A受体,增强γ-氨基丁酸的抑制性神经传递。研究表明,奥沙西泮在调节生物节律、改善睡眠及缓解焦虑等方面具有显著疗效。近年研究发现,该药还可通过与线粒体易位蛋白结合促进神经类固醇生成,从而在药物成瘾及酒精依赖的治疗中发挥潜在作用。在安全性方面,与部分长效苯二氮?类药物相比,奥沙西泮对认知功能的影响相对较小,尤其在老年患者中因其代谢途径不依赖细胞色素P450,较少出现过度镇静和药物蓄积现象而更具安全性。临床应用此药时需充分考虑患者的症状特点和个体病情,全面权衡利弊,规范合理用药。

关键词: 奥沙西泮, 苯二氮?类药物, GABAA受体, 生物节律, 睡眠, 焦虑

Abstract:

Oxazepam belongs to the class of medium-to-short-acting benzodiazepine sedative-hypnotic drugs. Its mechanism of action mainly involves regulating the γ-aminobutyric acid A receptor through positive allosteric effects, thereby enhancing the inhibitory neural transmission of γ-aminobutyric acid. Studies have shown that oxazepam has significant efficacy in regulating biological rhythms, improving sleep, and alleviating anxiety. Recent researches have found that this drug can also promote the generation of neurosteroids by binding to mitochondrial translocation proteins, thereby potentially playing a role in the treatment of drug addiction and alcohol dependence. In terms of safety, compared with some long-acting benzodiazepine drugs, oxazepam has a relatively smaller impact on cognitive function, especially in elderly patients, as its metabolic pathway does not rely on cytochrome P450, and there are fewer cases of excessive sedation and drug accumulation, making it safer. When using this drug clinically, it is necessary to fully consider the patient's symptom characteristics and individual condition, comprehensively weigh the pros and cons, and use it in a standardized and reasonable manner.

Key words: oxazepam, benzodiazepines, GABAA receptor, biological rhythm, sleep, anxiety

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