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Equihua AC, De La Herrán-Arita AK, Drucker-Colin R. Orexin receptor antagonists as therapeutic agents for insomnia. Front Pharmacol. 2013;4:163doi: 10.3389/fphar.2013.00163.
Equihua, A. C., De La Herrán-Arita, A. K., & Drucker-Colin, R. (2013). Orexin receptor antagonists as therapeutic agents for insomnia. Frontiers in pharmacology, 4163. https://doi.org/10.3389/fphar.2013.00163
Equihua, Ana C, et al. "Orexin receptor antagonists as therapeutic agents for insomnia." Frontiers in pharmacology vol. 4 (2013): 163. doi: https://doi.org/10.3389/fphar.2013.00163
Equihua AC, De La Herrán-Arita AK, Drucker-Colin R. Orexin receptor antagonists as therapeutic agents for insomnia. Front Pharmacol. 2013 Dec 25;4:163. doi: 10.3389/fphar.2013.00163. PMID: 24416019; PMCID: PMC3872321.
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Front Pharmacol. 2013 Dec 25;4:163. doi: 10.3389/fphar.2013.00163.

Orexin receptor antagonists as therapeutic agents for insomnia.

Frontiers in pharmacology

Ana C Equihua, Alberto K De La Herrán-Arita, Rene Drucker-Colin

Affiliations

  1. Neuropatología Molecular, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México Mexico City, México.
  2. Center for Sleep Sciences and Medicine, Stanford University Palo Alto, CA, USA.

PMID: 24416019 PMCID: PMC3872321 DOI: 10.3389/fphar.2013.00163

Abstract

Insomnia is a common clinical condition characterized by difficulty initiating or maintaining sleep, or non-restorative sleep with impairment of daytime functioning. Currently, treatment for insomnia involves a combination of cognitive behavioral therapy (CBTi) and pharmacological therapy. Among pharmacological interventions, the most evidence exists for benzodiazepine (BZD) receptor agonist drugs (GABAA receptor), although concerns persist regarding their safety and their limited efficacy. The use of these hypnotic medications must be carefully monitored for adverse effects. Orexin (hypocretin) neuropeptides have been shown to regulate transitions between wakefulness and sleep by promoting cholinergic/monoaminergic neural pathways. This has led to the development of a new class of pharmacological agents that antagonize the physiological effects of orexin. The development of these agents may lead to novel therapies for insomnia without the side effect profile of hypnotics (e.g., impaired cognition, disturbed arousal, and motor balance difficulties). However, antagonizing a system that regulates the sleep-wake cycle may create an entirely different side effect profile. In this review, we discuss the role of orexin and its receptors on the sleep-wake cycle and that of orexin antagonists in the treatment of insomnia.

Keywords: hypocretins/orexins; insomnia; orexin receptor antagonist; sleep disorders; therapy-related

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