丁螺环酮:一种独特的抗焦虑药物的最新进展。
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Jann兆瓦
丁螺环酮:一种独特的抗焦虑药物的最新进展。
药物治疗。1988;8(2):100 - 16。
- PubMed ID
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3041384 (PubMed视图］
- 摘要
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丁螺环酮(Buspar)是一种氮杂螺癸二酮类抗焦虑药。其作用机制极其复杂，但目前的研究表明其主要的神经药理作用是由5-HT1A受体介导的。其他神经受体系统也可能参与其中，丁环酮对DA2自身受体和5-HT2受体表现出一定的亲和力。有人提出抑制血清素的合成和释放是神经受体和次级信使系统共同作用的结果。这一作用抑制了中缝背侧含有5- ht的神经元的放电速率。与苯二氮平类不同的是，丁螺环酮缺乏抗惊厥和肌肉松弛的特性，只能引起最小的镇静作用。该药口服后吸收迅速，平均生物利用度为3.9%。单次口服后，平均消除半衰期为2.1小时。丁螺环酮主要与白蛋白和- 1-酸性糖蛋白结合。它被代谢为活性代谢物1-(2-嘧啶基)哌嗪(1- pp)。 The mean elimination half-life of 1-PP is 6.1 hours. Buspirone is indicated in the treatment of generalized anxiety disorders. Its efficacy is comparable to the benzodiazepines. Its use in depression and panic disorders requires further investigation. When combined with alcohol or given alone, psychomotor impairment was not detected. Abuse, dependence, and withdrawal symptoms have not been reported. The frequency of adverse effects is low, and the most common effects are headaches, dizziness, nervousness, and lightheadness. Buspirone should be added to drug formularies and could represent a significant addition in psychopharmacology.