Novos sedativos hipnóticos

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 tha...

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Detalles Bibliográficos
Autores: Sukys-Claudino, Lucia [UNIFESP], Moraes, Walter André dos Santos [UNIFESP], Tufik, Sergio [UNIFESP], Poyares, Dalva [UNIFESP]
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2010
País:Brasil
Institución:Universidade Federal de São Paulo (UNIFESP)
Repositorio:Repositório Institucional da UNIFESP
Idioma:portugués
OAI Identifier:oai:repositorio.unifesp.br:11600/5938
Acceso en línea:http://dx.doi.org/10.1590/S1516-44462010000300014
http://repositorio.unifesp.br/handle/11600/5938
Access Level:acceso abierto
Palabra clave:Hypnotics and sedatives
Physiological effects of drugs
Receptors, melatonin
Antidepressive agents
Sleep initiation and maintenance disorders
Hipnóticos e sedativos
Efeitos fisiológicos de drogas
Receptores de melatonina
Antidepressivos
Distúrbios do início e da manutenção do sono
Descripción
Sumario: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.