[The newer sedative-hypnotics].

Abstract

There has been a search for more effective and safe hypnotic drugs in the last decades. Zolpidem, zaleplon, zopiclone, eszopiclone (the z-drugs) and indiplon are GABA-A modulators which bind selectively α1 subunits, thus, exhibiting similar mechanisms of action, although recent evidence suggests that eszopiclone is not as selective for α1 subunit as zolpidem is. Ramelteon and tasimelteon are new chrono-hypnotic agents, selective for melatonin MT1 and MT2 receptors. On the other hand, the consumption of sedative antidepressant drugs is significantly increasing for the treatment of insomnia, in the last years. As an experimental drug, eplivanserin is being tested as a potent antagonist of serotonin 2-A receptors (ASTAR) with a potential use in sleep maintenance difficulty. Another recent pharmacological agent for insomnia is almorexant, which new mechanism of action involves antagonism of hypocretinergic system, thus inducing sleep. Finally we also discuss the potential role of other gabaergic drugs for insomnia.

• Authors: Lucia Sukys-Claudino, Walter André dos Santos Moraes, Sergio Tufik, Dalva Poyares
• Journal: Revista brasileira de psiquiatria (Sao Paulo, Brazil : 1999) (Braz J Psychiatry) Vol. 32 Issue 3 Pg. 288-93 (Sep 2010) ISSN: 1516-4446 [Print] Brazil
• Vernacular Title: Novos sedativos hipnóticos.
• PMID: 20945020 (Publication Type: English Abstract, Journal Article, Review)

Chemical References

• Antidepressive Agents
• GABA Agonists
• Hypnotics and Sedatives
• Receptor, Melatonin, MT1
• Receptor, Melatonin, MT2

Topics

• Antidepressive Agents (therapeutic use)
• GABA Agonists (therapeutic use)
• Humans
• Hypnotics and Sedatives (therapeutic use)
• Receptor, Melatonin, MT1 (agonists)
• Receptor, Melatonin, MT2 (agonists)
• Sleep Initiation and Maintenance Disorders (drug therapy)