艾司佐匹克隆的临床研究进展及应用

Clinical research and application of eszopiclone

艾司佐匹克隆(eszopiclone)是佐匹克隆的立体异构体(S)-zopiclone,是最近被美国FDA批准上市的新型镇静催眠药,适应证为慢性失眠证。该药通过作用于苯二氮革类(Ω-1型受体)-GABAA受体复合物特异的结合位点,使GABAA受体发生特异性构型改变,作为GABAA受体复合物的超效激动剂发挥镇静摧眠效果。艾司佐匹克隆对中枢苯二氮革受体的亲和力比佐匹克隆强50倍。该药吸收快速完全,药动学特征与佐匹克隆相似。临床研究显示该药能有效地缩短睡眠潜伏期、改善睡眠维持和提高睡眠质量、延长总睡眠时间,无白天的后遗效应和精神运动性损害。现对其临床研究进展及临床应用进行综述。

Eszopiclone （Brand name is Lunesta, Sepracor Inc. product）, the active （S）-isomer of zopiclone, is a novel sedative hypnotics, approved by Food and Drug Administration （FDA） for the treatment of insomnia on December 15,2004. The effects of eszopiclone is mediated by the action on benzodiapine receptor （Ω-1 receptor）-GABAA receptor compounds. Eszopiclone can be absorbed well and has the similar pharmacokinetic profile to the super-short action benzodiapines. Clinical studies showed that eszopiclone is effective for treatment of insomnia, reduction in sleep onset time and improvement in sleep maintenance, sleep qualities and next-days function, with no evidence of tolerance, rebound insomnia, residual effects, dependence or abuse.