A comprehensive review of the use of lemborexant in treating insomnia

Abstract

Abstract Lemborexant (LEM), a dual orexin receptor antagonist, represents a significant advancement in treating insomnia, a prevalent sleep disorder affecting a considerable portion of the population, especially older adults in India. LEM has several benefits over conventional sedatives in the treatment of insomnia, such as the selective mechanism of action, lower risk of tolerance and dependence, better sleep architecture, reduced possibility of cognitive impairment, various dosing options, the risk of rebound insomnia, and the risk of drug–drug interactions are also decreased. This thorough examination explores the pharmacological mechanisms, pharmacokinetics, clinical effectiveness, and safety profile of LEM, providing valuable insights into its distinct mode of action compared with traditional medications targeting gamma-aminobutyric acid receptors. By blocking orexin receptors (orexin 1 receptor and orexin 2 receptor), LEM regulates neuropeptides orexin A and orexin B, crucial for controlling wakefulness and arousal. Clinical trials demonstrate its predictable pharmacokinetics, dose-dependent effects, and minimal adverse reactions, confirming its efficacy in improving sleep initiation and maintenance. Long-term studies on LEM’s sustained therapeutic benefits show no signs of rebound insomnia or withdrawal. Its favorable safety profile, including minimal impact on next-day functioning, cognitive abilities, and postural stability, sets it apart from other treatments. The exploration of potential drug interactions underscores the importance of cautious prescribing, especially concerning cytochrome P450 3A inhibitors and inducers. As LEM becomes integrated into healthcare protocols, it promises to be a well-tolerated and effective solution, reshaping standard treatment approaches for insomnia and overcoming the limitations of older medications. In summary, LEM is a valuable addition to the pharmacotherapeutic toolbox, offering a novel strategy for managing sleep disturbances with sustained efficacy and favorable safety features.