Acarbose

Acarbose
Alerta sobre risco à saúde
Nome IUPAC (2R,3R,4R,5S,6R)-5-{[(2R,3R,4R,5S,6R)-5- {[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6 methyl- 5-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3- (hydroxymethyl)cyclohex-2-en-1-yl]amino} tetrahydro-2H-pyran-2-yl]oxy}-3,4 dihydroxy- 6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}- 6-(hydroxymethyl)tetrahydro-2H-pyran-2,3,4-triol
Identificadores
Número CAS 56180-94-0
PubChem 444254
ChEBI 2668
Código ATC A10BF01
SMILES
Propriedades
Fórmula química C25H43NO18
Massa molar 645.51 g mol-1
Farmacologia
Biodisponibilidade baixa
Via(s) de administração via oral
Metabolismo intestinal
Meia-vida biológica 2h
Ligação plasmática pouco
Excreção Inalterado em fezes, 2% renal
Riscos na gravidez
e lactação 		B3(AU) B (EUA)
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.

Acarbose é um fármaco utilizado pela medicina como redutor da glicemia,[1] hipoglicemiante. Retarda a absorção de amido e carboidratos grandes pela glicosidase alfa. É uma biotecnologia obtida através de filtrados de fungos, do grupo actinomicetos.

Mecanismo de ação

O fármaco é inibidor da enzima alfaglicosidase. Quando ingere-se carboidrato, com esta enzima inibida, é possível diminuir a quantidade de glicose no sangue. A alfa-glicosidase ajuda na absorção da glicose ingerida nas refeições promovendo uma maior concentração no sangue. Com a inibição desta enzima, além de reduzir a hiperglicemia o alimento leva mais tempo para concluir a digestão diminuindo a necessidade de novas refeições.

Administração

Deve ser tomada antes das refeições, 3 a 4 vezes por dia. Adultos podem tomar doses de 25 a 50mg. Doses mais altas causam maior produção de gases e diarreia. Mesmo tomando a acarbose deve-se continuar fazendo controle glicêmico regularmente.[2]

Indicações

A acarbose é indicada no tratamento de diabetes mellitus tipo 2 e também tipo 1 em associação com a insulina. Pode ser usado no pré-diabetes. Provavelmente é segura na gravidez, mas faltam mais estudos (categoria B).

Contra indicações

É contra indicada em caso de[3]:

Efeitos colaterais

Como a acarbose previne a degradação de carboidratos complexos em glicose, mais carboidratos permanecem no intestino e chegam ao cólon. No cólon as bactérias digerem carboidratos complexos causando efeitos secundários gastrointestinais como flatulência (em 78% dos pacientes) e diarreia (em 14% dos pacientes). Estes efeitos são relacionados com a dose sendo, em geral, aconselhável começar com uma dose baixa e aumentar gradualmente até a quantidade desejada. Um estudo descobriu que os efeitos colaterais reduzem significativamente reduz ao longo de 24 semanas (de 50 a 15%), mesmo com dosagem constante.[4]

Notas e referências

  1. ↑ P.R.Vade-mécum ABIMIP 2006/2007
  2. ↑ http://www.mayoclinic.org/drugs-supplements/acarbose-oral-route/proper-use/drg-20067949
  3. ↑ http://www.mayoclinic.org/drugs-supplements/acarbose-oral-route/before-using/drg-20067949
  4. ↑ "Efficacy of 24-week monotherapy with acarbose, metformin, or placebo in dietary-treated NIDDM patients: the Essen-II Study". Am. J. Med. 103 (6): 483–90. December 1997. doi:10.1016/S0002-9343(97)00252-0. PMID 9428831.

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