Heptaminol

Heptaminol
Alerta sobre risco à saúde
Nome IUPAC (RS)-6-amino-2-methylheptan-2-ol
Identificadores
Número CAS 372-66-7
PubChem 3590
ChemSpider 3464
MeSH Heptaminol
Código ATC C01DX08
SMILES
InChI
1/C8H19NO/c1-7(9)5-4-6-8(2,3)10/h7,10H,4-6,9H2,1-3H3
Propriedades
Fórmula química C8H19NO
Massa molar 145.24 g mol-1
Farmacologia
Via(s) de administração Oral,
Excreção Renal
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.

O Heptaminol é um alcanolamina cardiotóxico classificado como vasodilatador (C01DX08). Às vezes usa-se no tratamento da hipotensão ortoestática.[1][2]

Comercializa-se sobre as nomes de Clinadil compositum, Diclamina, Denubil e Largotrex.[3]

Mecanismo de acção

Estimula a circulação sanguínea cerebral pelo que também se utiliza como nootrópico facilitador da aprendizagem. É um agente inotrópico positivo que atua mediante a libertação de norepinefrina periférica o que ocasiona um aumento da contratilidade cardíaca, aumento da frequência cardíaca e vasodilatação. Também atua bloqueando os neurotransmisores pré- e pós-sinápticos o que afeta à amplitude das contracções musculares.

Farmacocinética

Em humanos, após a sua administração oral, o heptaminol absorve-se rápida e completamente. Após a administração oral de 300 mg de heptaminol as concentrações máximas atingem-se às 1,8 horas sendo a Cmax de 1,6 mg/ml. Tem uma meia-vida de eliminação de 2,5 horas. Se metaboliza por hidroxilação e elimina-se na urina em forma não conjugada.

Toxicidade

Em roedores, a dose letal 50 do heptaminol por via intraperitoneal é de 1250 mg/kg. Em humanos empregou-se desde faz muitas décadas sem que se tenham informado de efeitos negativos.

Doping

O heptaminol é uma substância dopante. O ciclista Dmitri Fofonov deu positivo na Volta a França.[4] Em junho de 2010 o nadador Frédérick Bousquet também deu positivo pela substância, supostamente por comprar um medicamento farmacêutico.[5]

Referências

  1. ↑ «Heptaminol» 
  2. ↑ (en francés) «Heptaminol Chlorhydrate» 
  3. ↑ Thierry Soucca. GUÍA DE LOS NUEVOS ESTIMULANTES. [S.l.: s.n.] 
  4. ↑ «Tour rider Fofonov tests positive» 
  5. ↑ «France swimmer Bousquet suspended in doping scandal» 

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