Research progress on the pharmacological effects and mechanisms of oxazepam

doi:10.12092/j.issn.1009-2501.2026.03.007

Abstract

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, GABA_A receptor, biological rhythm, sleep, anxiety

CLC Number:

R971
R749.5

Yiqun WANG, Zhilin WANG, Qingyang LI, Wenjie CEN, Qiaoyuan ZHENG, Zhili HUANG. Research progress on the pharmacological effects and mechanisms of oxazepam[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2026, 31(3): 352-361.

Figures/Tables 2

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药理作用	作用机制	作用特点
调节生物节律	调节SCN内昼夜节律中枢；影响下丘脑-垂体-肾上腺皮质轴活动及皮质醇分泌	存在昼夜依赖性，给药时机需结合生理节律
改善睡眠	增加NREM睡眠第2阶段，并增强σ纺锤波活动；抑制NREM睡眠第3阶段，抑制REM睡眠；	在健康个体中不会破坏整体脑电结构
缓解焦虑	抑制杏仁核过度激活；作用于行为抑制系统，降低应激源引发的皮肤电反应	适用于急性及广泛性焦虑，不诱发反常激动
减轻药物依赖	与TSPO结合，影响内源性神经类固醇生成	可减轻苯二氮?类、酒精及毒品戒断症状
改善认知	抑制杏仁核过度激活	作用具有间接性、短期性和情境性

药理作用	作用机制	作用特点
调节生物节律	调节SCN内昼夜节律中枢；影响下丘脑-垂体-肾上腺皮质轴活动及皮质醇分泌	存在昼夜依赖性，给药时机需结合生理节律
改善睡眠	增加NREM睡眠第2阶段，并增强σ纺锤波活动；抑制NREM睡眠第3阶段，抑制REM睡眠；	在健康个体中不会破坏整体脑电结构
缓解焦虑	抑制杏仁核过度激活；作用于行为抑制系统，降低应激源引发的皮肤电反应	适用于急性及广泛性焦虑，不诱发反常激动
减轻药物依赖	与TSPO结合，影响内源性神经类固醇生成	可减轻苯二氮?类、酒精及毒品戒断症状
改善认知	抑制杏仁核过度激活	作用具有间接性、短期性和情境性

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