Insomnia Pharmacotherapy
Insomnia Pharmacotherapy
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DOI：
10.1007/s13311-012-0148-3
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发表时间：
2012-10-01
影响因子：
5.7
通讯作者：
Roth, Thomas
中科院分区：
文献类型：
--
作者：
Roehrs, Timothy;Roth, Thomas
苯二氮卓受体激动剂（BzRAs）、褪黑激素受体激动剂和组胺拮抗剂都已被批准作为催眠药。除了它们不同的作用机制外，它们在药代动力学方面也存在差异，在BzRAs中，受体亚型亲和力和配方也存在差异，这为医生提供了广泛的选择，可以根据每个患者的具体需求定制治疗。与它们特定的药代动力学和配方一致，这些食品和药物管理局批准的催眠药已被证明可以改善睡眠，没有证据表明长期使用会产生耐受性。此外，新出现的数据表明，这些药物还能改善白天的功能。它们的副作用要么与药物的直接镇静作用有关，剂量大于临床剂量，要么与酒精或其他镇静药物联合使用。抗焦虑药BzRAs，镇静抗抑郁药和抗精神病药已被用作催眠药。然而，由于缺乏有关其有效性和安全性的剂量范围的信息，将其用作催眠药是不明智的。
The benzodiazepine receptor agonists (BzRAs) a melatonin receptor agonist and a histamine antagonist have all been approved as hypnotics. Beyond their differing mechanisms of action, they have differences in pharmacokinetics, and among the BzRAs differences in receptor subtype affinity and formulations, which provides the physician with broad options for tailoring therapy to each patient's specific needs. Consistent with their specific pharmacokinetics and formulations, these Food and Drug Administration-approved hypnotics have been shown to improve sleep with no evidence of tolerance development in long-term use. In addition, emerging data indicate these drugs also improve aspects of daytime function. Their side effects are either associated with the direct sedating effects of the drugs, doses greater than clinical doses, or a combination with alcohol or other sedating drugs. Anxiolytic BzRAs, sedating antidepressants and antipsychotics have been used off-label as hypnotics. However, in the absence of information regarding their dose range for efficacy and safety, their use as hypnotics is ill-advised.