莱博雷生临床应用中国专家共识

doi:10.12114/j.issn.1007-9572.2025.0272

中国全科医学 ›› 2026, Vol. 29 ›› Issue (05): 545-558.DOI: 10.12114/j.issn.1007-9572.2025.0272

莱博雷生临床应用中国专家共识

中国睡眠研究会, 广东省医师协会睡眠医学专业委员会, 广东省医院协会医院药事管理专业委员会, 郭俊龙¹, 郑萍², 贾福军³, 李雪丽³, 詹淑琴⁴, 王远青⁵, 顾平⁶, 冯媛¹, 莫立乾², 郝永慈⁶, 郑舒琼¹, 曾海梅², 张斌¹^,^*(), 李亦蕾²^,^*()

1．510515　广东省广州市，南方医科大学南方医院精神心理科　睡眠医学中心
2．510515　广东省广州市，南方医科大学南方医院药学部
3．510080　广东省广州市，南方医科大学附属广东省人民医院　广东省医学科学院　广东省精神卫生中心
4．100053　北京市，首都医科大学宣武医院神经内科
5．276800　山东省日照市人民医院神经内科
6．050031　河北省石家庄市，河北医科大学第一医院神经内科

收稿日期:2025-07-31 修回日期:2025-09-09 出版日期:2026-02-15 发布日期:2026-01-05
通讯作者: 张斌, 李亦蕾
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
执笔人：
郭俊龙和郑萍为共同第一作者，对本文贡献同等
基金资助:
广州市科技计划项目(2024A04J5101); 南方医科大学南方医院临床研究专项(2021CR009); "科创中国"睡眠数字产业科技服务团项目; 医院药学高质量发展研究课题智慧药学专项(NIHAYSZX2528)

Chinese Expert Consensus on the Clinical Application of Lemborexant

Chinese Sleep Research Society, Sleep Medicine Professional Committee of Guangdong Medical Doctor Association, Pharmacy Administration Committee of Guangdong Province Hospital Association, GUO Junlong¹, ZHENG Ping², JIA Fujun³, LI Xueli³, ZHAN Shuqin⁴, WANG Yuanqing⁵, GU Ping⁶, FENG Yuan¹, MO Liqian², HAO Yongci⁶, ZHENG Shuqiong¹, ZENG Haimei², ZHANG Bin¹^,^*(), LI Yilei²^,^*()

1. Department of Psychiatry/Sleep Medicine Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China
2. Clinical Pharmacy Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China
3. Guangdong Mental Health Center, Guangdong Provincial People's Hospital/Guangdong Academy of Medical Sciences, Southern Medical University, Guangzhou 510080, China
4. Department of Neurology, Xuanwu Hospital, Capital Medical University, Beijing 100053, China
5. Department of Neurology, People's Hospital of Rizhao, Rizhao 276800, China
6. Department of Neurology, the First Hospital of Hebei Medical University, Shijiazhuang 050031, China

Received:2025-07-31 Revised:2025-09-09 Published:2026-02-15 Online:2026-01-05
Contact: ZHANG Bin, LI Yilei
About author:
GUO Junlong and ZHENG Ping are co-first authors who contributed equally to this work

分享到

摘要/Abstract

摘要： 失眠是最常见的睡眠紊乱，显著影响患者的生活质量和工作表现，且与躯体疾病、精神障碍等疾病相关。莱博雷生作为新型催眠药，是中国首个获批上市的食欲素双受体拮抗剂（DORA）。然而，目前我国尚缺乏莱博雷生临床应用的相关规范。为此，中国睡眠研究会、广东省医师协会睡眠医学专业委员会和广东省医院协会医院药事管理专业委员会组织国内药学和临床医学领域专家，依据国内外研究进展，结合中国首个莱博雷生的真实世界研究，制订《莱博雷生临床应用中国专家共识》。本共识针对莱博雷生的药理作用、药代动力学、适应证、临床应用方法等进行阐述，经过多轮讨论、修订和投票表决后最终形成17条推荐意见，以期为莱博雷生的临床应用提供全面而规范的参考和建议。

关键词: 莱博雷生, 失眠, 食欲素双受体拮抗剂, 临床应用

Abstract:

Insomnia is the most common sleep disorder. It not only significantly disturbs patients' quality of life and occupational performance, but is also associated with physical illness and mental disorders. Lemborexant, a new type of hypnotic drug, is the first dual orexin receptor antagonist (DORA) approved in China. However, there's still a lack of standardized guidelines for the usage of Lemborexant in China. Therefore, Chinese Sleep Research Society, the Sleep Medicine Professional Committee of Guangdong Medical Doctor Association and the Pharmacy Administration Committee of Guangdong Province Hospital Association collaborated with domestic experts in pharmacology and clinical medicine to develop the Expert Consensus on the Clinical Application of Lemborexant in China, elaborating on the pharmacological effects, pharmacokinetics, indications, and clinical application methods of Lemborexant. After multiple rounds of discussions, revisions, and voting, 17 recommendations were finally reached, aiming to provide comprehensive and standardized references and suggestions for the clinical application of Lemborexant.

Key words: Lemborexant, Insomnia, Dual orexin receptor antagonist, Clinical application

中图分类号:

R 741

中国睡眠研究会,广东省医师协会睡眠医学专业委员会,广东省医院协会医院药事管理专业委员会,等. 莱博雷生临床应用中国专家共识[J]. 中国全科医学, 2026, 29(05): 545-558. DOI: 10.12114/j.issn.1007-9572.2025.0272.
Chinese Sleep Research Society,Sleep Medicine Professional Committee of Guangdong Medical Doctor Association,Pharmacy Administration Committee of Guangdong Province Hospital Association, et al. Chinese Expert Consensus on the Clinical Application of Lemborexant[J]. Chinese General Practice, 2026, 29(05): 545-558. DOI: 10.12114/j.issn.1007-9572.2025.0272.

图/表 6

参考文献 96

[1]	张斌. 中国失眠障碍诊断和治疗指南[M]. 2版. 北京: 人民卫生出版社, 2025: 147.
[2]	HOC T V, LEE H C. Clinical and polysomnographic characteristics of Asian patients with comorbid insomnia and obstructive sleep apnea[J]. Sci Rep, 2025, 15(1): 11529. DOI: 10.1038/s41598-025-96825-7.
[3]	HERTENSTEIN E, BENZ F, SCHNEIDER C L, et al. Insomnia-a risk factor for mental disorders[J]. J Sleep Res, 2023, 32(6): e13930. DOI: 10.1111/jsr.13930.
[4]	KRYSTAL A D. Insomnia medications: history, characteristics, and guidelines for optimal use in clinical practice[J]. J Sleep Res, 2023, 32(6): e14084. DOI: 10.1111/jsr.14084.
[5]	MOLINE M, ZAMMIT G, YARDLEY J, et al. Lack of residual morning effects of lemborexant treatment for insomnia: summary of findings across 9 clinical trials[J]. Postgrad Med, 2021, 133(1): 71-81. DOI: 10.1080/00325481.2020.1823724.
[6]	LI X, ZHENG S, JIAN W, et al. Reported OUTCOMES for LEMborexant treatment in Chinese patients with insomnia(PROEM): a real-world study[C]//SLEEP 2025, the 39th Annual Meeting of the Associated Professional Sleep Societies, LLC(APSS). Seattle, Washington, USA, 2025.
[7]	陈耀龙, 杨克虎, 王小钦, 等. 中国制订/修订临床诊疗指南的指导原则(2022版)[J]. 中华医学杂志, 2022, 102(10): 697-703. DOI: 10.3760/cma.j.cn112137-20211228-02911.
[8]	CHIEFFI S, CAROTENUTO M, MONDA V, et al. Orexin system: the key for a healthy life[J]. Front Physiol, 2017, 8: 357. DOI: 10.3389/fphys.2017.00357.
[9]	NEVÁREZ N, DE LECEA L. Recent advances in understanding the roles of hypocretin/orexin in arousal, affect, and motivation[J]. F1000Res, 2018, 7: F1000FacultyRev-F1000Faculty1421. DOI: 10.12688/f1000research.15097.1.
[10]	ARDELJAN A, HUREZEANU R. Lemborexant[J]. Am J Health Syst Pharm, 2020, 77(17): 1358-1361.
[11]	HOYER D, ALLEN A, JACOBSON L H. Hypnotics with novel modes of action[J]. Br J Clin Pharmacol, 2020, 86(2): 244-249. DOI: 10.1111/bcp.14180.
[12]	FRONCZEK R, LAMMERS G J, BALESAR R, et al. The number of hypothalamic hypocretin (orexin) neurons is not affected in Prader-Willi syndrome[J]. J Clin Endocrinol Metab, 2005, 90(9): 5466-5470. DOI: 10.1210/jc.2005-0296.
[13]	THANNICKAL T C, MOORE R Y, NIENHUIS R, et al. Reduced number of hypocretin neurons in human narcolepsy[J]. Neuron, 2000, 27(3): 469-474. DOI: 10.1016/s0896-6273(00)00058-1.
[14]	MIEDA M, HASEGAWA E, KISANUKI Y Y, et al. Differential roles of orexin receptor-1 and-2 in the regulation of non-REM and REM sleep[J]. J Neurosci, 2011, 31(17): 6518-6526. DOI: 10.1523/JNEUROSCI.6506-10.2011.
[15]	PEYRON C, FARACO J, ROGERS W, et al. A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains[J]. Nat Med, 2000, 6(9): 991-997. DOI: 10.1038/79690.
[16]	FULLER M C, CARLSON S F, GRANT C, et al. A comprehensive review of lemborexant to treat insomnia[J]. Psychopharmacol Bull, 2024, 54(1): 43-64.
[17]	COLEMAN P J, GOTTER A L, JOSEPH HERRING W, et al. The discovery of suvorexant, the first orexin receptor drug for insomnia[J]. Annu Rev Pharmacol Toxicol, 2017, 57: 509-533. DOI: 10.1146/annurev-pharmtox-010716-104837.
[18]	BEUCKMANN C T, SUZUKI M, UENO T, et al. In vitro and in silico characterization of lemborexant (E2006), a novel dual orexin receptor antagonist[J]. J Pharmacol Exp Ther, 2017, 362(2): 287-295. DOI: 10.1124/jpet.117.241422.
[19]	SAKURAI T, AMEMIYA A, ISHII M, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior[J]. Cell, 1998, 92(4): 573-585. DOI: 10.1016/s0092-8674(00)80949-6.
[20]	KISHI T, NISHIDA M, KOEBIS M, et al. Evidence-based insomnia treatment strategy using novel orexin antagonists: a review[J]. Neuropsychopharmacol Rep, 2021, 41(4): 450-458. DOI: 10.1002/npr2.12205.
[21]	KISHI T, NOMURA I, MATSUDA Y, et al. Lemborexant vs suvorexant for insomnia: a systematic review and network meta-analysis[J]. J Psychiatr Res, 2020, 128: 68-74. DOI: 10.1016/j.jpsychires.2020.05.025.
[22]	FDA. DAYVIGO (Lemborexant): highlights of prescribing information[EB/OL]. [2025-05-08].
[23]	LANDRY I, HALL N, ALURI J, et al. Effect of alcohol coadministration on the pharmacodynamics, pharmacokinetics, and safety of lemborexant: a randomized, placebo-controlled crossover study[J]. J Psychopharmacol, 2022, 36(6): 745-755. DOI: 10.1177/02698811221080459.
[24]	LALOVIC B, MAJID O, ALURI J, et al. Population pharmacokinetics and exposure-response analyses for the most frequent adverse events following treatment with lemborexant, an orexin receptor antagonist, in subjects with insomnia disorder[J]. J Clin Pharmacol, 2020, 60(12): 1642-1654. DOI: 10.1002/jcph.1683.
[25]	LANDRY I, NAKAI K Y, FERRY J, et al. Pharmacokinetics, pharmacodynamics, and safety of the dual orexin receptor antagonist lemborexant: findings from single-dose and multiple-ascending-dose phase 1 studies in healthy adults[J]. Clin Pharmacol Drug Dev, 2021, 10(2): 153-165. DOI: 10.1002/cpdd.817.
[26]	MANO Y, UENO T, HOTTA K. Establishment of a simultaneous assay for lemborexant, a novel dual orexin receptor antagonist, and its three metabolites, and its application to a clinical protein binding study[J]. J Pharm Biomed Anal, 2020, 187: 113359. DOI: 10.1016/j.jpba.2020.113359.
[27]	UENO T, ISHIDA T, ALURI J, et al. Disposition and metabolism of [14C] lemborexant in healthy human subjects and characterization of its circulating metabolites[J]. Drug Metab Dispos, 2021, 49(1): 31-38. DOI: 10.1124/dmd.120.000229.
[28]	ROSENBERG R, MURPHY P, ZAMMIT G, et al. Comparison of lemborexant with placebo and zolpidem tartrate extended release for the treatment of older adults with insomnia disorder: a phase 3 randomized clinical trial[J]. JAMA Netw Open, 2019, 2(12): e1918254. DOI: 10.1001/jamanetworkopen.2019.18254.
[29]	MOLINE M, ZAMMIT G, CHENG J Y, et al. Comparison of the effect of lemborexant with placebo and zolpidem tartrate extended release on sleep architecture in older adults with insomnia disorder[J]. J Clin Sleep Med, 2021, 17(6): 1167-1174. DOI: 10.5664/jcsm.9150.
[30]	MCELROY H, O'LEARY B, ADENA M, et al. Comparative efficacy of lemborexant and other insomnia treatments: a network meta-analysis[J]. J Manag Care Spec Pharm, 2021, 27(9): 1296-1308. DOI: 10.18553/jmcp.2021.21011.
[31]	YUE J L, CHANG X W, ZHENG J W, et al. Efficacy and tolerability of pharmacological treatments for insomnia in adults: a systematic review and network meta-analysis[J]. Sleep Med Rev, 2023, 68: 101746. DOI: 10.1016/j.smrv.2023.101746.
[32]	MIYATA S, IWAMOTO K, OKADA I, et al. Assessing the real-world, long-term impact of lemborexant on sleep quality in a home-based clinical study[J]. Nat Sci Sleep, 2024, 16: 291-303. DOI: 10.2147/NSS.S448871.
[33]	TERAUCHI M, CHENG J Y, YARDLEY J, et al. Efficacy and safety of lemborexant in midlife women with insomnia disorder[J]. Menopause, 2023, 30(8): 839-848. DOI: 10.1097/GME.0000000000002209.
[34]	INOUE Y, WATANABE T, TAKASHIMA S, et al. Efficacy and safety of lemborexant in adults with insomnia: comparing Japanese and non-Japanese subgroups from the global, phase 3, randomized, double-blind, placebo-controlled SUNRISE 2 study[J]. J Clin Sleep Med, 2021, 17(5): 1067-1074. DOI: 10.5664/jcsm.9148.
[35]	ARNOLD V, ANCOLI-ISRAEL S, DANG-VU T T, et al. Efficacy of lemborexant in adults ≥ 65 years of age with insomnia disorder[J]. Neurol Ther, 2024, 13(4): 1081-1098. DOI: 10.1007/s40120-024-00622-9.
[36]	KÄRPPÄ M, YARDLEY J, PINNER K, et al. Long-term efficacy and tolerability of lemborexant compared with placebo in adults with insomnia disorder: results from the phase 3 randomized clinical trial SUNRISE 2[J]. Sleep, 2020, 43(9): zsaa123. DOI: 10.1093/sleep/zsaa123.
[37]	KRYSTAL A, BLIER P, CULPEPPER L, et al. Efficacy and safety of lemborexant in subjects with insomnia disorder receiving medications for depression or anxiety symptoms[J]. Neuropsychopharmacol Rep, 2025, 45(1): e12509. DOI: 10.1002/npr2.12509.
[38]	MURAYAMA T, ITO Y, NARITA K, et al. The effect of lemborexant on insomnia in patients with psychiatric disorders: detailed evaluation using the Athens Insomnia Scale[J]. PCN Rep, 2024, 3(1): e165. DOI: 10.1002/pcn5.165.
[39]	KATSUTA N, TAKAHASHI K, KUROSAWA Y, et al. Safety and real-world efficacy of lemborexant in the treatment of comorbid insomnia[J]. Sleep Med X, 2023, 5: 100070. DOI: 10.1016/j.sleepx.2023.100070.
[40]	HORIKOSHI S, MIURA I, SUZUKI Y, et al. Switching to lemborexant for the management of insomnia in mental disorders: the SLIM study[J]. J Clin Sleep Med, 2023, 19(10): 1753-1758. DOI: 10.5664/jcsm.10668.
[41]	JIAN W Y, FENG M Y, ZHAO Y F, et al. Efficacy and safety of Lemborexant in treating adult patients with insomnia in China: a single-center, retrospective observational study[J]. Front Neurol, 2025, 16: 1495965. DOI: 10.3389/fneur.2025.1495965.
[42]	KISHI T, KOEBIS M, SUGAWARA M, et al. Orexin receptor antagonists in the treatment of insomnia associated with psychiatric disorders: a systematic review[J]. Transl Psychiatry, 2024, 14(1): 374. DOI: 10.1038/s41398-024-03087-4.
[43]	UEMATSU T, TOMITA T, OBARA R, et al. Reducing the use of psychotropics in a convalescent rehabilitation ward[J]. Neuropsychopharmacol Rep, 2024, 44(1): 227-233. DOI: 10.1002/npr2.12388.
[44]	LIGUORI C, NUCCETELLI M, IZZI F, et al. Rapid eye movement sleep disruption and sleep fragmentation are associated with increased orexin-a cerebrospinal-fluid levels in mild cognitive impairment due to Alzheimer's disease[J]. Neurobiol Aging, 2016, 40: 120-126. DOI: 10.1016/j.neurobiolaging.2016.01.007.
[45]	LIGUORI C, ROMIGI A, NUCCETELLI M, et al. Orexinergic system dysregulation, sleep impairment, and cognitive decline in Alzheimer disease[J]. JAMA Neurol, 2014, 71(12): 1498-1505. DOI: 10.1001/jamaneurol.2014.2510.
[46]	MUSIEK E S, XIONG D D, HOLTZMAN D M. Sleep, circadian rhythms, and the pathogenesis of Alzheimer disease[J]. Exp Mol Med, 2015, 47(3): e148. DOI: 10.1038/emm.2014.121.
[47]	DUNCAN M J, FARLOW H, TIRUMALARAJU C, et al. Effects of the dual orexin receptor antagonist DORA-22 on sleep in 5XFAD mice[J]. Alzheimers Dement, 2019, 5: 70-80. DOI: 10.1016/j.trci.2019.01.003.
[48]	MOLINE M, THEIN S, BSHARAT M, et al. Safety and efficacy of lemborexant in patients with irregular sleep-wake rhythm disorder and Alzheimer's disease dementia: results from a phase 2 randomized clinical trial[J]. J Prev Alzheimers Dis, 2021, 8(1): 7-18. DOI: 10.14283/jpad.2020.69.
[49]	BAYLAN S, GRIFFITHS S, GRANT N, et al. Incidence and prevalence of post-stroke insomnia: a systematic review and meta-analysis[J]. Sleep Med Rev, 2020, 49: 101222. DOI: 10.1016/j.smrv.2019.101222.
[50]	WINROW C J, RENGER J J. Discovery and development of orexin receptor antagonists as therapeutics for insomnia[J]. Br J Pharmacol, 2014, 171(2): 283-293. DOI: 10.1111/bph.12261.
[51]	WINROW C J, GOTTER A L, COX C D, et al. Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist[J]. J Neurogenet, 2011, 25(1/2): 52-61. DOI: 10.3109/01677063.2011.566953.
[52]	KAWADA K, OHTA T, TANAKA K, et al. Addition of suvorexant to ramelteon therapy for improved sleep quality with reduced delirium risk in acute stroke patients[J]. J Stroke Cerebrovasc Dis, 2019, 28(1): 142-148. DOI: 10.1016/j.jstrokecerebrovasdis.2018.09.024.
[53]	OZONE M, HIROTA S, ARIYOSHI Y, et al. Efficacy and safety of transitioning to lemborexant from Z-drug, suvorexant, and ramelteon in Japanese insomnia patients: an open-label, multicenter study[J]. Adv Ther, 2024, 41(4): 1728-1745. DOI: 10.1007/s12325-024-02811-2.
[54]	DE CRESCENZO F, D'ALÒ G L, OSTINELLI E G, et al. Comparative effects of pharmacological interventions for the acute and long-term management of insomnia disorder in adults: a systematic review and network meta-analysis[J]. Lancet, 2022, 400(10347): 170-184. DOI: 10.1016/S0140-6736(22)00878-9.
[55]	TERADA T, HIRAYAMA T, SADAHIRO R, et al. Pilot study of lemborexant for insomnia in cancer patients with delirium[J]. J Palliat Med, 2022, 25(5): 797-801. DOI: 10.1089/jpm.2021.0509.
[56]	OGURA T, UENO S, OKUDA A, et al. Can lemborexant for insomnia prevent delirium in high-risk patients with pancreato-biliary disease after endoscopic procedures under deep sedation?[J]. J Clin Med, 2022, 12(1): 297. DOI: 10.3390/jcm12010297.
[57]	CHENG J Y, FILIPPOV G, MOLINE M, et al. Respiratory safety of lemborexant in healthy adult and elderly subjects with mild obstructive sleep apnea: a randomized, double-blind, placebo-controlled, crossover study[J]. J Sleep Res, 2020, 29(4): e13021. DOI: 10.1111/jsr.13021.
[58]	CHENG J Y, LORCH D, LOWE A D, et al. A randomized, double-blind, placebo-controlled, crossover study of respiratory safety of lemborexant in moderate to severe obstructive sleep apnea[J]. J Clin Sleep Med, 2024, 20(1): 57-65. DOI: 10.5664/jcsm.10788.
[59]	CHENG J Y, MOLINE M, ZAMMIT G K, et al. Respiratory safety of lemborexant in healthy subjects: a single-dose, randomized, double-blind, placebo-controlled, crossover study[J]. Clin Drug Investig, 2021, 41(5): 449-457. DOI: 10.1007/s40261-021-01018-5.
[60]	KUSHIDA C A, ZAMMIT G K, CHENG J Y, et al. Effect of lemborexant on sleep architecture in participants with insomnia disorder and mild obstructive sleep apnea[J]. Sleep Med, 2025, 127: 170-177. DOI: 10.1016/j.sleep.2024.12.023.
[61]	CHENG J Y, LORCH D, HALL N, et al. Respiratory safety of lemborexant in adult and elderly subjects with moderate-to-severe chronic obstructive pulmonary disease[J]. J Sleep Res, 2025, 34(2): e14334. DOI: 10.1111/jsr.14334.
[62]	TOGO Y, KAIZUKA Y, NAGASAWA S, et al. Efficacy and safety of lemborexant for insomnia patients with nocturia-a prospective study[J]. Low Urin Tract Symptoms, 2024, 16(6): e12534. DOI: 10.1111/luts.12534.
[63]	PRESKORN S H. Comparative pharmacology of the 3 marketed dual orexin antagonists-daridorexant, lemborexant, and suvorexant: part 1: pharmacokinetic profiles[J]. J Psychiatr Pract, 2022, 28(6): 478-480. DOI: 10.1097/PRA.0000000000000672.
[64]	MURPHY P, MOLINE M, MAYLEBEN D, et al. Lemborexant, A dual orexin receptor antagonist (DORA) for the treatment of insomnia disorder: results from a Bayesian, adaptive, randomized, double-blind, placebo-controlled study[J]. J Clin Sleep Med, 2017, 13(11): 1289-1299. DOI: 10.5664/jcsm.6800.
[65]	HABIBA U, WASEEM R, SHAIKH T G, et al. Comparative efficacy and safety of lemborexant 5 mg versus 10 mg for the treatment of insomnia: a systematic review[J]. Neurol Sci, 2023, 44(5): 1533-1541. DOI: 10.1007/s10072-023-06601-6.
[66]	LANDRY I, ALURI J, NAKAI K Y, et al. Evaluation of the CYP3A and CYP2B6 drug-drug interaction potential of lemborexant[J]. Clin Pharmacol Drug Dev, 2021, 10(6): 681-690. DOI: 10.1002/cpdd.915.
[67]	UENO T, MIYAJIMA Y, LANDRY I, et al. Physiologically-based pharmacokinetic modeling to predict drug interactions of lemborexant with CYP3A inhibitors[J]. CPT Pharmacometrics Syst Pharmacol, 2021, 10(5): 455-466. DOI: 10.1002/psp4.12606.
[68]	WATANABE K, MISAKA S, KANNO-NOZAKI K, et al. Effect of lemborexant on pharmacokinetics of clozapine: a potential drug-drug interaction mediated by time-dependent inhibition of CYP3A4[J]. Br J Clin Pharmacol, 2024, 90(1): 354-359. DOI: 10.1111/bcp.15889.
[69]	LANDRY I, ALURI J, HALL N, et al. Effect of gastric acid-reducing agents on the pharmacokinetics and efficacy of lemborexant[J]. Pharmacol Res Perspect, 2020, 8(6): e00678. DOI: 10.1002/prp2.678.
[70]	LANDRY I, ALURI J, HALL N, et al. Effects of lemborexant on the pharmacokinetics of oral contraceptives: results from a phase 1 drug-drug interaction study in healthy females[J]. Clin Pharmacol Drug Dev, 2021, 10(9): 1089-1098. DOI: 10.1002/cpdd.953.
[71]	OKINO K, SUZUKI H, TOMIOKA H, et al. Efficacy and safety of lemborexant as an alternative drug for patients with insomnia taking gamma-aminobutyric acid-benzodiazepine receptor agonists or suvorexant[J]. Hum Psychopharmacol, 2023, 38(3): e2868. DOI: 10.1002/hup.2868.
[72]	TAKAESU Y, SAKURAI H, AOKI Y, et al. Treatment strategy for insomnia disorder: Japanese expert consensus[J]. Front Psychiatry, 2023, 14: 1168100. DOI: 10.3389/fpsyt.2023.1168100.
[73]	TACHIBANA M, KANAHARA N, ODA Y, et al. A retrospective clinical practice study comparing the usefulness of dual-orexin receptor antagonists and a melatonin receptor agonist in patients switching from long-term benzodiazepine receptor agonists[J]. J Clin Sleep Med, 2024, 20(4): 603-613. DOI: 10.5664/jcsm.10946.
[74]	PALAGINI L, BRUGNOLI R, DELL' OSSO B M, et al. Clinical practice guidelines for switching or deprescribing hypnotic medications for chronic insomnia: results of European Neuropsychopharmacology and Sleep Expert's Consensus Group[J]. Sleep Med, 2025, 128: 117-126. DOI: 10.1016/j.sleep.2025.01.033.
[75]	HINTZE J P, EDINGER J D. Hypnotic discontinuation in chronic insomnia[J]. Sleep Med Clin, 2020, 15(2): 147-154. DOI: 10.1016/j.jsmc.2020.02.003.
[76]	AHMAD M, KELLY J, MONTANO C B, et al. Transitioning insomnia patients from zolpidem to lemborexant: a multicenter, open-label study evaluating a next-dose transition approach to insomnia pharmacotherapy[J]. Sleep Med X, 2024, 7: 100098. DOI: 10.1016/j.sleepx.2023.100098.
[77]	TANAKA-MIZUNO S, FUJIMOTO K, MISHIMA K, et al. Evaluation of prescribing patterns of switching to and add-on lemborexant in patients treated with hypnotic medication: a nationwide claims database study in Japan[J]. Expert Opin Pharmacother, 2024, 25(12): 1707-1716. DOI: 10.1080/14656566.2024.2392018.
[78]	SUZUKI H, HIBINO H. Characteristics of patients who were able to switch from benzodiazepine hypnotics to lemborexant[J]. SAGE Open Med, 2021, 9: 20503121211037903. DOI: 10.1177/20503121211037903.
[79]	WATSON N F, BENCA R M, KRYSTAL A D, et al. Alliance for sleep clinical practice guideline on switching or deprescribing hypnotic medications for insomnia[J]. J Clin Med, 2023, 12(7): 2493. DOI: 10.3390/jcm12072493.
[80]	TAKAESU Y, SUZUKI M, MOLINE M, et al. Effect of discontinuation of lemborexant following long-term treatment of insomnia disorder: secondary analysis of a randomized clinical trial[J]. Clin Transl Sci, 2023, 16(4): 581-592. DOI: 10.1111/cts.13470.
[81]	MAYLEBEN D, ROSENBERG R, PINNER K, et al. Assessment of morning sleep propensity with lemborexant in adults with insomnia disorder in a randomized, placebo-controlled crossover study[J]. Sleep Adv, 2021, 2(1): zpab011. DOI: 10.1093/sleepadvances/zpab011.
[82]	MURPHY P, KUMAR D, ZAMMIT G, et al. Safety of lemborexant versus placebo and zolpidem: effects on auditory awakening threshold, postural stability, and cognitive performance in healthy older participants in the middle of the night and upon morning awakening[J]. J Clin Sleep Med, 2020, 16(5): 765-773. DOI: 10.5664/jcsm.8294.
[83]	VERMEEREN A, JONGEN S, MURPHY P, et al. On-the-road driving performance the morning after bedtime administration of lemborexant in healthy adult and elderly volunteers[J]. Sleep, 2019, 42(4): zsy260. DOI: 10.1093/sleep/zsy260.
[84]	VERMEEREN A, VUURMAN E F P M, LEUFKENS T R M, et al. Residual effects of low-dose sublingual zolpidem on highway driving performance the morning after middle-of-the-night use[J]. Sleep, 2014, 37(3): 489-496. DOI: 10.5665/sleep.3482.
[85]	FORNARO M, CAIAZZA C, ROSSANO F, et al. Residual effects of medications for sleep disorders on driving performance: a systematic review and network meta-analysis of randomized controlled trials: NMA driving and hypnotics[J]. Eur Neuropsychopharmacol, 2024, 81: 53-63. DOI: 10.1016/j.euroneuro.2024.01.011.
[86]	GOTTER A L, WINROW C J, BRUNNER J, et al. The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold[J]. BMC Neurosci, 2013, 14: 90. DOI: 10.1186/1471-2202-14-90.
[87]	NA H J, JEON N, STAATZ C E, et al. Clinical safety and narcolepsy-like symptoms of dual orexin receptor antagonists in patients with insomnia: a systematic review and meta-analysis[J]. Sleep, 2024, 47(2): zsad293. DOI: 10.1093/sleep/zsad293.
[88]	MCINTYRE R S, WONG S, KWAN A T H, et al. Association between dual orexin receptor antagonists (DORAs) and suicidality: reports to the United States Food and Drug Administration Adverse Event Reporting System (FAERS)[J]. Expert Opin Drug Saf, 2025, 24(6): 753-757. DOI: 10.1080/14740338.2024.2361300.
[89]	ASAKURA S, SHIOTANI M, GAUVIN D V, et al. Nonclinical evaluation of abuse liability of the dual orexin receptor antagonist lemborexant[J]. Regul Toxicol Pharmacol, 2021, 127: 105053. DOI: 10.1016/j.yrtph.2021.105053.
[90]	MOLINE M, ASAKURA S, BEUCKMAN C, et al. The abuse potential of lemborexant, a dual orexin receptor antagonist, according to the 8 factors of the Controlled Substances Act[J]. Psychopharmacology, 2023, 240(4): 699-711. DOI: 10.1007/s00213-023-06320-y.
[91]	MISHIMA K, FUJIMOTO K, ENDO A, et al. Safety and efficacy of lemborexant in insomnia patients: results of a postmarketing observational study of dayvigo® tablets[J]. Drugs R D, 2024, 24(2): 211-226. DOI: 10.1007/s40268-024-00462-w.
[92]	DAYAL S, ALURI J, HALL N, et al. Effect of hepatic impairment on pharmacokinetics, safety, and tolerability of lemborexant[J]. Pharmacol Res Perspect, 2021, 9(2): e00758. DOI: 10.1002/prp2.758.
[93]	LANDRY I, ALURI J, HALL N, et al. Effect of severe renal impairment on pharmacokinetics, safety, and tolerability of lemborexant[J]. Pharmacol Res Perspect, 2021, 9(2): e00734. DOI: 10.1002/prp2.734.
[94]	SAITO J, ISHII M, SANDAIJI N, et al. Lemborexant levels in maternal serum, cord blood, and breast milk during pregnancy and lactation: a case report[J]. PCN Rep, 2023, 2(1): e62. DOI: 10.1002/pcn5.62.
[95]	RAWAL S, BRIMHALL D, ALURI J, et al. Lemborexant levels in breast milk after single doses in healthy, lactating women[J]. Br J Clin Pharmacol, 2024, 90(1): 158-163. DOI: 10.1111/bcp.15880.
[96]	GOTFRIED M H, AUERBACH S H, DANG-VU T T, et al. Efficacy and safety of insomnia treatment with lemborexant in older adults: analyses from three clinical trials[J]. Drugs Aging, 2024, 41(9): 741-752. DOI: 10.1007/s40266-024-01135-8.

证据等级	说明
Ⅰ级	具有较窄置信区间的高质量随机临床试验
Ⅱ级	低质量随机试验或高质量队列研究
Ⅲ级	病例对照研究
Ⅳ级	病例系列或较差的病例对照研究、队列研究或病例报告

证据等级	说明
Ⅰ级	具有较窄置信区间的高质量随机临床试验
Ⅱ级	低质量随机试验或高质量队列研究
Ⅲ级	病例对照研究
Ⅳ级	病例系列或较差的病例对照研究、队列研究或病例报告

推荐强度	具体描述
A级	评估依据大量高等级（证据等级Ⅰ级或Ⅱ级）证据和/或强有力的临床共识支持的推荐疗法评估
B级	评估依据为少量高级别（Ⅰ级或Ⅱ级）数据，或大量低级别（Ⅲ级或Ⅳ级）数据，和/或任务组的临床共识
C级	评估基于低等级数据，数据量不足以支持更高等级的推荐，且随着进一步研究的深入，评估结果很可能会有所调整

推荐强度	具体描述
A级	评估依据大量高等级（证据等级Ⅰ级或Ⅱ级）证据和/或强有力的临床共识支持的推荐疗法评估
B级	评估依据为少量高级别（Ⅰ级或Ⅱ级）数据，或大量低级别（Ⅲ级或Ⅳ级）数据，和/或任务组的临床共识
C级	评估基于低等级数据，数据量不足以支持更高等级的推荐，且随着进一步研究的深入，评估结果很可能会有所调整

合用药物	相互作用机制	临床措施
克拉霉素、伊曲康唑、伏立康唑、泊沙康唑、酮康唑、利托那韦、奈非那韦、米非司酮、西柚汁	CYP3A4强抑制剂	避免合用
阿瑞匹坦、地尔硫卓、维拉帕米、决奈达隆、红霉素、氟康唑、艾沙康唑、伊马替尼、五味子	CYP3A4中效抑制剂	避免合用
利福平、卡马西平、苯妥英、米托坦	CYP3A4强诱导剂	避免合用
苯巴比妥、利福喷丁、利福布汀、依非韦伦、波生坦、洛拉替尼、雌二醇/炔诺酮	CYP3A4中效诱导剂	避免合用
阿普唑仑、胺碘酮、氨氯地平、小檗碱、氯唑沙宗、西洛他唑、西咪替丁、环丙沙星、罗红霉素、克霉唑、环孢素、地奥司明、依维莫司、氟伏沙明、异烟肼、拉帕替尼、丙泊酚、托吡酯	CYP3A4弱抑制剂	莱博雷生最大剂量不能超过5 mg/d，每晚不超过1次

莱博雷生临床应用中国专家共识

Chinese Expert Consensus on the Clinical Application of Lemborexant

RichHTML

PDF

可视化

摘要/Abstract

引用本文

使用本文

图/表 6

参考文献 96

相关文章 15

编辑推荐

Metrics

留言

[1]	中国康复医学会社区康复工作委员会. 虚拟现实技术应用于肿瘤相关性失眠居家康复的专家共识（2025年版）[J]. 中国全科医学, 2025, 28(35): 4385-4396.
[2]	徐百川, 王艳, 张彭, 李艺婷, 刘飞来, 谢洋. 慢性阻塞性肺疾病共病肺癌筛查工具分析[J]. 中国全科医学, 2025, 28(30): 3847-3852.
[3]	张红石, 曲子涵, 孙雪峰, 王宇峰, 丛德毓, 张野. 基于蛋白质组学技术分析腹部推拿对失眠大鼠下丘脑的影响研究[J]. 中国全科医学, 2025, 28(27): 3399-3409.
[4]	肖瑶, 万钧. 直接口服抗凝药在静脉血栓栓塞特殊人群中的临床应用[J]. 中国全科医学, 2025, 28(24): 3066-3071.
[5]	中国医师协会睡眠医学专业委员会, 中国医师协会神经内科医师分会睡眠学组. 中国成人失眠共病阻塞性睡眠呼吸暂停诊治指南（2024版）[J]. 中国全科医学, 2025, 28(11): 1289-1303.
[6]	余悦敏, 莫非非, 李乐思, 潘集阳. 中国青少年失眠的评估工具和影响因素：一项范围综述[J]. 中国全科医学, 2025, 28(10): 1213-1219.
[7]	郭玉梦, 崔杨霖, 张宪忠. 基于孟德尔随机化探讨肠道菌群与失眠的因果关联研究[J]. 中国全科医学, 2025, 28(08): 954-961.
[8]	郭佳, 曹春梅, 刘国纯, 郑满, 朱芮含, 龙伟. 不同运动方式对失眠患者睡眠影响效果的网状Meta分析[J]. 中国全科医学, 2024, 27(35): 4376-4387.
[9]	陈鹏飞, 刘雅茜, 王途之, 张桂梅, 蔡艺娴, 潘集阳. 失眠的在线简版行为疗法对失眠障碍的干预效果研究[J]. 中国全科医学, 2024, 27(35): 4370-4375.
[10]	董孟龙, 林志烽, 范孟孟, 薛盛文, 刘宇航, 王怡, 程金湘. 非苯二氮䓬类药物治疗失眠共病睡眠呼吸暂停的临床效果评价研究新进展[J]. 中国全科医学, 2024, 27(35): 4388-4396.
[11]	中国睡眠研究会. 失眠数字疗法中国专家共识[J]. 中国全科医学, 2024, 27(04): 381-390.
[12]	何静漪, 王芳, 税晓玲, 李玲, 梁倩. 非药物干预改善围绝经期失眠症状疗效的网状Meta分析[J]. 中国全科医学, 2023, 26(31): 3963-3974.
[13]	朱琳, 郭闫葵, 高琛, 陈学志, 王法帅. 单纯西药、中成药及其联合治疗卒中后失眠疗效的网状Meta分析[J]. 中国全科医学, 2023, 26(30): 3823-3832.
[14]	中华预防医学会更年期保健分会, 中国人体健康科技促进会妇科内分泌和生育力促进专委会, 北京中西医结合学会更年期专业委员会. 绝经相关失眠临床管理中国专家共识[J]. 中国全科医学, 2023, 26(24): 2951-2958.
[15]	陈品琪, 张丽清, 向婷, 孙熙哲, 潘集阳. 静息态功能磁共振局部一致性在抑郁障碍伴失眠症状患者中的研究进展[J]. 中国全科医学, 2022, 25(35): 4462-4467.