Lemborexant, an orexin receptor antagonist, is effective not only for sleep disorders but also for preventing and treating delirium. To date, no complex sleep-related behaviors due to lemborexant have been reported. Herein, we present the case of a 69-year-old male patient who was hospitalized for oral floor and tongue cancer and developed delirium after surgery; however, upon lemborexant dosage increase, used to treat insomnia, he developed abnormal nocturnal behavior. This symptom rapidly improved when lemborexant was discontinued. Distinguishing parasomnia from delirium is important because the treatment of these two conditions differs. Although rapid eye movement sleep behavior or sleepwalking was the cause of this parasomnia, a definitive diagnosis could not be established. If qualitatively distinct abnormal behavior is observed compared to delirium after increasing lemborexant dosage, the possibility of parasomnia should be considered.
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http://dx.doi.org/10.1097/YIC.0000000000000546 | DOI Listing |
J Pharm Sci
December 2024
Janssen Research & Development, LLC, Discovery Pharmaceutics, San Diego, CA, USA.
Rat pharmacokinetic studies are commonly utilized in early discovery to support absorption, distribution, metabolism, and excretion optimization of active pharmaceutical ingredients (APIs). The aim of this work was to compare exposures from fit-for-purpose oral suspension and solution formulations in rats to guidance provided by the refined Developability Classification System (rDCS) with respect to identifying potential limits to oral absorption, formulation strategy selection, and to optimize oral bioavailability (BA). This investigation utilized six diverse APIs covering a large range of biorelevant solubility, metabolic stability, and oral BA in rats.
View Article and Find Full Text PDFNeuropsychopharmacol Rep
March 2025
Eisai Ltd., Hatfield, UK.
J Sleep Res
November 2024
Department of Neurology, Kaohsiung Medical University Hospital, Kaohsiung, Taiwan.
Dual orexin receptor antagonists (DORAs) are indicated for the treatment of insomnia disorder. However, DORAs may change sleep parameters, thus having adverse effects on patients with obstructive sleep apnea (OSA). This meta-analysis clarified the impact of DORAs in OSA treatment on sleep architecture and respiratory parameters.
View Article and Find Full Text PDFAm J Geriatr Psychiatry
February 2025
Department of Neurology, Tufts Medical Center Boston (JO), Boston, MA.
Introduction: The rising prevalence of Alzheimer's disease (AD) and related dementia worldwide underscores the urgent need for effective interventions, particularly for managing neuropsychiatric symptoms (NPS) such as sleep disturbance. This review explores the emerging role of Dual Orexin Receptor Antagonists (DORA) in addressing sleep disturbance in patients with Alzheimer's disease dementia.
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J Pharm Sci
October 2024
Fraunhofer Institute for Translational Medicine and Pharmacology, Frankfurt am Main, Germany. Electronic address:
Lemborexant is a dual orexin receptor antagonist assigned to class II of the Biopharmaceutics Classification System (BCS). Thus, the ICH M9 Guideline excludes immediate-release (IR) solid oral dosage forms containing lemborexant from BCS-based biowaivers, irrespective of their in vitro dissolution behavior. By contrast, classification of lemborexant according to the refined Developability Classification System (rDCS) falls into class I, indicating few biopharmaceutics risks.
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