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O papel da orexina para novas abordagens terapêuticas da insónia
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Resumo(s)
O sono representa uma função vital do organismo com múltiplos efeitos
fisiológicos, apresentando-se ainda como fundamental na restauração da actividade cerebral.
A falta de sono tem consequências nefastas para o organismo. Hoje em dia a
insónia apresenta-se como um foco de preocupação crescente, pelo aumento da sua prevalência a nível mundial.
Atualmente existem diversas terapêuticas farmacológicas disponíveis no
mercado, sendo que apresentam várias efeitos secundários e limitações ao seu uso.
A orexina (hipocretina) é um neuropéptido, com efeitos reguladores no ciclo
sono/vigília. O antagonismo dos receptores da orexina (ARO) tem-se revelado um mecanismo de acção promissor no tratamento da insónia.
Este trabalho visa rever as principais características farmacológicas dos fármacos utilizados no tratamento da insónia que atuam nos receptores da orexina. Uma vez que se trata de uma área muito recente de investigação, propõe-se com esse trabalho efectuar uma revisão sobre as principais características clínicas e farmacológicas desta nova classe de fármacos para o tratamento da insónia.
Realizou-se uma revisão não sistemática da literatura, através da pesquisa em
Pubmed (http://www.pubmed.com), Medscape (http://www.medscape.com) e
clinicaltrials (https://www.clinicaltrials.gov), desde Janeiro de 1998 até Janeiro de 2015, recorrendo às seguintes palavras-chave: sleep, insomnia, hipnotics, orexin, hypocretin, orexin antagonists, Suvorexant.
Os ARO são fármacos pioneiros com resultados promissores, mostrando-se
diferentes dos fármacos anteriores por serem eficazes no tratamento da insónia em doses que aparentemente não perturbam as funções cognitivas, sem efeitos secundários significativos, mostrando-se seguros independentemente da idade do paciente. Apesar disso, carecem de uma melhor compreensão do seu funcionamento, assim como das consequências da sua utilização a longo prazo.
O aparecimento desta nova classe terapêutica para o tratamento da insónia veio dar um novo contributo para a prática clínica, alargando a oferta farmacológica para o tratamento da insónia.
Sleep is a vital function with multiple physiological effects, being fundamental in restoring brain activity. Lack of sleep has harmful consequences for the body. Insomnia presents itself as a focus of growing concern, since its prevalence is increasing worldwide. Currently there are many drug therapies available in the market, which have several side effects and limitations on its use. The orexin (hypocretin) is a neuropeptide with regulatory effects on sleep / wake cycle. The antagonism of Orexin receptors (ARO) has proved to be a promising mechanism of action for insomnia treatment. This paper aims to review the main pharmacological characteristics of drugs used in insomnia treatment, that operate in the orexin receptors. Since this is a very new area of research, it is proposed to make a review of the main clinical and pharmacological characteristics of this new class of drugs. It was conducted a non-systematic literature review, through research in Pubmed (http://www.pubmed.com), Medscape (http://www.medscape.com) and clinicaltrials (https: //www.clinicaltrials. gov), from January 1998 to January 2015, using the following key words: sleep, insomnia, hipnotics, orexin, hypocretin, orexin antagonists, Suvorexant. The ARO are pioneers drugs that show promising results , being different from the previous ones by being effective in insomnia treatment, at doses that apparently do not a disrupt cognitive function neither show significant side effects, being also safe regardless patient's age. Nevertheless, they still lack of better understanding of its mechanisms, as well as knowledge of consequences to its long-term use . The revelation of this new therapeutic class to, gave a new contribution to clinical practice, extending the possibilities of pharmacological treatment.
Sleep is a vital function with multiple physiological effects, being fundamental in restoring brain activity. Lack of sleep has harmful consequences for the body. Insomnia presents itself as a focus of growing concern, since its prevalence is increasing worldwide. Currently there are many drug therapies available in the market, which have several side effects and limitations on its use. The orexin (hypocretin) is a neuropeptide with regulatory effects on sleep / wake cycle. The antagonism of Orexin receptors (ARO) has proved to be a promising mechanism of action for insomnia treatment. This paper aims to review the main pharmacological characteristics of drugs used in insomnia treatment, that operate in the orexin receptors. Since this is a very new area of research, it is proposed to make a review of the main clinical and pharmacological characteristics of this new class of drugs. It was conducted a non-systematic literature review, through research in Pubmed (http://www.pubmed.com), Medscape (http://www.medscape.com) and clinicaltrials (https: //www.clinicaltrials. gov), from January 1998 to January 2015, using the following key words: sleep, insomnia, hipnotics, orexin, hypocretin, orexin antagonists, Suvorexant. The ARO are pioneers drugs that show promising results , being different from the previous ones by being effective in insomnia treatment, at doses that apparently do not a disrupt cognitive function neither show significant side effects, being also safe regardless patient's age. Nevertheless, they still lack of better understanding of its mechanisms, as well as knowledge of consequences to its long-term use . The revelation of this new therapeutic class to, gave a new contribution to clinical practice, extending the possibilities of pharmacological treatment.
Descrição
Trabalho Final do Curso de Mestrado Integrado em Medicina, Faculdade de Medicina, Universidade de Lisboa, 2015
Palavras-chave
Orexinas Antagonistas dos receptores de orexina Insónia Terapêutica