Rufinamida

Rufinamida
Alerta sobre risco à saúde
Nome IUPAC 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
Identificadores
Número CAS 106308-44-5
PubChem 129228
Código ATC N03AF03
SMILES
Propriedades
Fórmula química C10H8F2N4O
Massa molar 238.19 g mol-1
Página de dados suplementares
Estrutura e propriedades n, εr, etc.
Dados termodinâmicos Phase behaviour
Solid, liquid, gas
Dados espectrais UV, IV, RMN, EM
Exceto onde denotado, os dados referem-se a
materiais sob condições normais de temperatura e pressão
Referências e avisos gerais sobre esta caixa.
Alerta sobre risco à saúde.

Rufinamida (nomes comerciais: Banzel, Inovelon, entre outros)[1][2] é um anticonvulsivante usado em combinação com outros medicamentos para tratar convulsões relacionadas à síndrome de Lennox-Gastaut[3] e outros transtornos convulsivos. A rufinamida é um derivado de triazol e foi desenvolvida pela Novartis em 2004.

Nos Estados Unidos, a rufinamida foi aprovada pela agência reguladora Food and Drug Administration (FDA) em 14 de novembro de 2008 para o tratamento adjuvante de convulsões associadas à síndrome de Lennox-Gastaut em adultos e crianças a partir dos 4 anos. Apesar de não ter sido aprovada para o tratamento de convulsões parciais, ensaios clínicos sugerem que a rufinamida seja eficaz para o tratamento de convulsões parciais.[4]

O mecanismo de ação da rufinamida não é completamente conhecido. Algunas evidências sugerem que a rufinamida atua modulando o bloqueio dos canais de sódio dependentes de voltagem,[5][6] um alvo comum para drogas anticonvulsivantes e antiepilépticas.[7] Um estudo de 2014 descreveu os os efeitos da rufinamida sobre os canais de sódio dependente de voltagem, sugerindo que a inativação de algumas isoformas do canal de sódio que pode reduzir a excitabilidade neuronal.[8] No entanto, esta ação não pode explicar o espectro completo da atividade da rufinamida.

Referências

  1. ↑ Brodie MJ, Rosenfeld WE, Vazquez B, Sachdeo R, Perdomo C, Mann A, Arroyo S (agosto de 2009). «Rufinamide for the adjunctive treatment of partial seizures in adults and adolescents: a randomized placebo-controlled trial». Epilepsia. 50 (8): 1899–909. PMID 19490053. doi:10.1111/j.1528-1167.2009.02160.x 
  2. ↑ European Public Assessment Report for rufinamide (INOVELON)
  3. ↑ Hakimian S, Cheng-Hakimian A, Anderson GD, Miller JW (agosto de 2007). «Rufinamide: a new anti-epileptic medication». Expert Opin Pharmacother. 8 (12): 1931–40. PMID 17696794. doi:10.1517/14656566.8.12.1931 
  4. ↑ Brodie MJ, Rosenfeld WE, Vazquez B, Sachdeo R, Perdomo C, Mann A, Arroyo S (agosto de 2009). «Rufinamide for the adjunctive treatment of partial seizures in adults and adolescents: a randomized placebo-controlled trial». Epilepsia. 50 (8): 1899–909. PMID 19490053. doi:10.1111/j.1528-1167.2009.02160.x 
  5. ↑ Rogawski, M. A. (2006). «Diverse mechanisms of antiepileptic drugs in the development pipeline». Epilepsy Research. 69 (3): 273–94. PMC 1562526Acessível livremente. PMID 16621450. doi:10.1016/j.eplepsyres.2006.02.004 
  6. ↑ Striano, P.; McMurray, R.; Santamarina, E.; Falip, M. (2018). «Rufinamide for the treatment of Lennox-Gastaut syndrome: Evidence from clinical trials and clinical practice». Epileptic Disorders. 20 (1): 13–29. PMID 29313492. doi:10.1684/epd.2017.0950Acessível livremente 
  7. ↑ Rogawski, A.; Löscher, W. (julho de 2004). «The neurobiology of antiepileptic drugs». Nature Reviews. Neuroscience. 5 (7): 553–564. ISSN 1471-003X. PMID 15208697. doi:10.1038/nrn1430 
  8. ↑ Gilchrist, J; Dutton, S; Diaz-Bustamante, M; McPherson, A; Olivares, N; Kalia, J; Escayg, A; Bosmans, F (2014). «Nav1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodents». ACS Chemical Biology. 9 (5): 1204–12. PMC 4027953Acessível livremente. PMID 24635129. doi:10.1021/cb500108p 

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