丁螺环酮:更新一个独特的抗焦虑剂。
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Jann兆瓦
丁螺环酮:更新一个独特的抗焦虑剂。
药物治疗。1988;8 (2):100 - 16。
- PubMed ID
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3041384 (在PubMed]
- 文摘
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丁螺环酮(Buspar)是一个azaspirodecanedione抗焦虑剂。其作用机理是非常复杂的,但是目前的调查表明,其主要neuropharmacologic 5-HT1A受体介导的影响。其他神经受体系统可能涉及,丁螺环酮显示一些DA2受体和5-HT2受体的亲和力。已经提出,抑制血清素的合成和释放结果通过神经受体引起的联合互动和第二信使系统。这一行动导致抑制5-HT-containing神经元的放电频率在中缝背。从这本小说形象,不同于苯二氮卓类,丁螺环酮缺乏抗痉挛的肌肉松弛剂性质,只造成最小的镇静。药物口服后迅速吸收,平均3.9%的生物利用度。单剂量口服后,意味着消除半衰期2.1小时。丁螺环酮主要是白蛋白和α1-acid糖蛋白。代谢是一个活跃的代谢物1 - (2-pyrimidinyl)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.