Belsomra

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==Relationship to Insomnia==
==Relationship to Insomnia==
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Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal.
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Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system<ref>Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.</ref>. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal<ref>doi:10.2174/157015908787386050</ref>.
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With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.
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With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder<ref>doi: 10.2147/DDDT.S73224</ref>.
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.
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== References ==
== References ==
<references/>
<references/>
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Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.
 
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Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050
 
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Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224
 

Revision as of 21:57, 4 December 2016

PDB ID 4S0V

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References

  1. 1.0 1.1 1.2 Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35.
  2. Stahl SM. Mechanism of action of suvorexant. CNS Spectr. 2016 Jun;21(3):215-8. doi: 10.1017/S1092852916000225. PMID:27322687 doi:http://dx.doi.org/10.1017/S1092852916000225
  3. 3.0 3.1 Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry. 2013;74 Suppl 1:3-20. doi: 10.4088/JCP.13011su1c. PMID:24107804 doi:http://dx.doi.org/10.4088/JCP.13011su1c
  4. Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli RM, Tanaka H, Williams SC, Richardson JA, Kozlowski GP, Wilson S, Arch JR, Buckingham RE, Haynes AC, Carr SA, Annan RS, McNulty DE, Liu WS, Terrett JA, Elshourbagy NA, Bergsma DJ, Yanagisawa M. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85. PMID:9491897
  5. Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.
  6. Schwartz JR, Roth T. Neurophysiology of sleep and wakefulness: basic science and clinical implications. Curr Neuropharmacol. 2008 Dec;6(4):367-78. doi: 10.2174/157015908787386050. PMID:19587857 doi:http://dx.doi.org/10.2174/157015908787386050
  7. Sutton EL. Profile of suvorexant in the management of insomnia. Drug Des Devel Ther. 2015 Nov 11;9:6035-42. doi: 10.2147/DDDT.S73224. eCollection, 2015. PMID:26648692 doi:http://dx.doi.org/10.2147/DDDT.S73224
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