Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado, Aurora, 80045, USA.
J Am Pharm Assoc (2003). 2012;52(6):e210-9. doi: 10.1331/JAPhA.2012.12051.
To evaluate the literature regarding the use of histamine-1 (H(1)) receptor antagonists and to describe their role in the treatment of insomnia in adult patients, including the elderly.
Literature was identified via PubMed and Medline through April 1, 2012, using the search terms insomnia and sleep, each individually combined with histamine antagonist, tricyclic antidepressant, trazodone, mirtazapine, doxepin, amitriptyline, nortriptyline, trimipramine, doxylamine, diphenhydramine, and antihistamine.
Data included randomized double-blind trials that statistically evaluated H(1) receptor antagonist treatment in patients with insomnia compared with a placebo control or Food and Drug Administration-approved insomnia treatment. Trials selected evaluated sleep latency, wake after sleep onset, total sleep time, number of awakenings, and/or sleep efficiency in a subjective or objective manner. A total of 65 trials were evaluated, and 16 met inclusion criteria.
With the exception of low-dose doxepin (Silenor-Somaxon), trials evaluating the clinical effectiveness of H(1) receptor antagonists show mixed results and are limited by sample size and generalizability. Large, randomized, appropriately controlled trials are lacking, making it difficult to define the safety and efficacy of these agents. In contrast, low-dose doxepin has been shown to provide consistent sleep benefit compared with placebo.
Over-the-counter antihistamines may have a role for short-term insomnia treatment in younger adults, but tolerance develops rapidly. Mirtazapine should not be used solely for the treatment of insomnia. Sedating antidepressants can be considered after failure of first-line insomnia treatments. Patients taking these agents chronically should be evaluated for continued efficacy and potential harm. Low-dose doxepin may have a unique role in the treatment of insomnia in elderly patients given its tolerability, documented efficacy, and lack of important adverse effects.
评估关于组胺 1（H（1））受体拮抗剂的文献，并描述其在治疗成年患者（包括老年人）失眠中的作用。
通过 PubMed 和 Medline 进行文献检索，检索词为失眠和睡眠，每个词分别与组胺拮抗剂、三环类抗抑郁药、曲唑酮、米氮平、多塞平、阿米替林、去甲替林、三甲丙咪嗪、 doxylamine、 diphenhydramine 和抗组胺药组合使用，检索时间截至 2012 年 4 月 1 日。
纳入的数据包括随机双盲试验，这些试验统计学评估了与安慰剂对照或美国食品和药物管理局批准的失眠治疗相比，H（1）受体拮抗剂治疗失眠患者的效果。选择的试验以主观或客观的方式评估了睡眠潜伏期、睡眠起始后觉醒、总睡眠时间、觉醒次数和/或睡眠效率。共评估了 65 项试验，其中 16 项符合纳入标准。
除了低剂量 doxepin（Silenor-Somaxon）外，评估 H（1）受体拮抗剂临床疗效的试验结果不一，且受到样本量和普遍性的限制。缺乏大型、随机、适当对照的试验，因此难以确定这些药物的安全性和疗效。相比之下，低剂量 doxepin 已被证明与安慰剂相比能提供一致的睡眠益处。
非处方抗组胺药可能在年轻成年人的短期失眠治疗中有一定作用，但很快会产生耐受性。米氮平不应单独用于失眠的治疗。在一线失眠治疗失败后，可以考虑使用镇静性抗抑郁药。长期服用这些药物的患者应评估其持续疗效和潜在危害。鉴于 doxepin 的耐受性、已证实的疗效和缺乏重要的不良反应，低剂量 doxepin 在老年失眠患者的治疗中可能具有独特的作用。
