Barenbaum Rubén D, Rilla Manta Luis
Vertex. 2004;15 Suppl 1:5-11.
Benzodiazepines are effective and widely used in anxiety disorders, but they produce sedation and dependency. Molecular studies have shown that binding benzodiazepines to GABAA receptors containing the Alpha1 subunit mediates the sedative properties of benzodiazepines. Other strategies are being developed including the use of the selective GABA reuptake inhibitor tiagabine and the voltage gated calcium ion channel ligand pregabalin. Several novel strategies are being developed based on preclinical observations, including corticotrophin-releasing factor (CRF) antagonists, substance P antagonists, and drugs inhibiting glutamate neurotransmission.
苯二氮䓬类药物在焦虑症治疗中疗效显著且应用广泛,但会产生镇静作用和依赖性。分子研究表明,苯二氮䓬类药物与含有α1亚基的GABAA受体结合介导了其镇静特性。其他策略也在不断开发中,包括使用选择性GABA再摄取抑制剂噻加宾和电压门控钙离子通道配体普瑞巴林。基于临床前观察,正在开发几种新策略,包括促肾上腺皮质激素释放因子(CRF)拮抗剂、P物质拮抗剂以及抑制谷氨酸神经传递的药物。