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Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Lemborexant is currently in Phase II trial and other molecules like MIN-202, SB-649868, and ACT-462206 are other drugs in the group in Phase I clinical trials. These drugs were proved to reduce latency to sleep, have sleep efficiency (SE), to decrease the phenomenon of wake after sleep onset (ASO), and increased the total sleep time (TST) or duration in relation to “Z” drugs and placebo. These drugs have better safety profile as compared with suvorexant (Misra and Sharma, 2017).
Evaluating lemborexant for the treatment of insomnia
Published in Expert Opinion on Pharmacotherapy, 2021
In rats and monkeys, LEM is rapidly absorbed (blood concentration peaked at 0.83 to 1.8 hours after administration) and primarily eliminated by a metabolism pathway [53]. In healthy adults, LEM exposure increased with increasing dose: time to maximum concentration ranged from approximately 1 to 3 hours and effective half-life ranged from 17 to 19 hours, and there was no evidence of effects of age, sex, or race [54]. In adults with insomnia, LEM pharmacokinetics were described by a three-compartment model with combined first- and zero-order absorption with lag time and linear elimination [55]. In this study, no clinically significant differences in the pharmacokinetics of lemborexant were observed based on age, sex, race/ethnicity, or body mass index [55]. In adults with moderate hepatic impairment, LEM exposure is increased and a dose limit of 5 mg is recommended. No dose adjustment is recommended for patients with mild, moderate, or severe renal impairment [51].
Selecting a pharmacotherapy regimen for patients with chronic insomnia
Published in Expert Opinion on Pharmacotherapy, 2020
Amanda B. Hassinger, Nikolas Bletnisky, Rizwan Dudekula, Ali A. El-Solh
A representative of a new class of hypnotics, the orexin receptor antagonists, suvorexant, has been approved by the FDA in August 2014 for the treatment of primary insomnia of the sleep-onset and sleep-maintenance subtypes. However, suvorexant increases nocturnal sleep mainly by reducing wake after sleep onset (WASO) [47,48]. Suvorexant effect on sleep onset is substantially weaker compared to other short-acting hypnotics like zaleplon or triazolam. Despite the limited safety data on its prolonged use, our approach still favors the use of this agent for coexisting sleep onset and sleep-maintenance insomnia because difficulty staying asleep is more common than difficulty falling asleep particularly for patients over the age of 40 [49]. The current recommended dose is 10 mg to 20 mg daily. Like most hypnotics, suvorexant can be responsible for daytime sleepiness, fatigue, narcolepsy-like symptoms, and in rare instances suicidal ideation [49]. Lemborexant is the most recent drug in the orexin receptor antagonists class to receive approval from the FDA for the treatment of sleep onset and or sleep-maintenance insomnia [50]. Its mechanism of action parallels that of suvorexant. Similar to non-benzodiazepine benzodiazepine-receptor agonists, both suvorexant and lemborexant are a schedule IV controlled substance.
Lack of residual morning effects of lemborexant treatment for insomnia: summary of findings across 9 clinical trials
Published in Postgraduate Medicine, 2021
Margaret Moline, Gary Zammit, Jane Yardley, Kate Pinner, Dinesh Kumar, Carlos Perdomo, Jocelyn Y. Cheng
This article reports findings from lemborexant clinical studies conducted by Eisai Inc. as part of the clinical development program for the registration of lemborexant for the treatment of insomnia. Findings from 9 studies are included (Table 1); these 9 studies included next-morning or across-the-day assessments of residual drug effects. Results are reported for subjects treated with lemborexant 5 mg/day or 10 mg/day (the doses studied in phase 3, based on a phase 2 dose-finding study) [15], placebo, and comparator or active control treatments (zolpidem and zopiclone) before bedtime.