Sleep Disorders and Research Center, Henry Ford Hospital, Detroit, MI 48202, USA.
Neurotherapeutics. 2012 Oct;9(4):728-38. doi: 10.1007/s13311-012-0148-3.
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.
苯二氮䓬受体激动剂（BzRAs）、褪黑素受体激动剂和组胺拮抗剂都已被批准作为催眠药。除了作用机制不同外，它们在药代动力学方面也存在差异，而在 BzRAs 中，受体亚型亲和力和制剂方面也存在差异，这为医生根据每个患者的具体需求定制治疗方案提供了广泛的选择。这些经美国食品和药物管理局批准的催眠药与其特定的药代动力学和制剂一致，已被证明可改善睡眠，且在长期使用中无耐受性发展的证据。此外，新出现的数据表明，这些药物还可以改善日间功能的各个方面。它们的副作用要么与药物的直接镇静作用有关，要么与剂量大于临床剂量有关，要么与酒精或其他镇静药物合用。苯二氮䓬类抗焦虑药、镇静性抗抑郁药和抗精神病药已被超适应证用作催眠药。然而，由于缺乏关于其疗效和安全性剂量范围的信息，不建议将其用作催眠药。
