Diazóxido

Diazóxido
Nombre (IUPAC) sistemático
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Identificadores
Número CAS 364-98-7
Código ATC C02DA01 V03AH01
PubChem 3019
DrugBank DB01119
ChemSpider 2911
UNII O5CB12L4FN
KEGG D00294
ChEBI 4495
ChEMBL 181
Datos químicos
Fórmula C8H7N2ClO2S 
Peso mol. 230.672 g/mol
Clc1ccc2c(c1)S(=O)(=O)/N=C(\N2)C
InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
Key: GDLBFKVLRPITMI-UHFFFAOYSA-N
Farmacocinética
Unión proteica 90%
Metabolismo Oxidación hepática y conjugación de sulfato
Vida media 21-45 horas
Excreción Renal
Datos clínicos
Cat. embarazo C (AU) No hay estudios en humanos. El fármaco solo debe utilizarse cuando los beneficios potenciales justifican los posibles riesgos para el feto. Queda a criterio del médico tratante. (EUA)
Vías de adm. Oral, intravenosa
[editar datos en Wikidata]

El Diazóxido (INN; nombre comercial Proglycem)[1]​ es un activador de los canales de potasio, que causa una relajación local el músculo liso a través de un incremento de la permeabilidad membranosa hacia los iones de potasio. Esto cambia los canales iónicos voltaje-dependientes de calcio que inhiben la generación de un potencial de acción.

Usos

Este fármaco es utilizado como un vasodilatador en el tratamiento de la hipertensión aguda o la hipertensión maligna.[2]​ Además, inhibe la secreción de insulina desde el páncreas, por lo que se utiliza para contrarrestar la hipoglicemia en varios estados de la enfermedad, tales como la insulinoma (un tumor productor de insulina)[3]​ o el hiperinsulinismo congénito.

Química

El diazóxido puede ser preparado desde el dicloronitrobenceno:[4]​

Referencias

  1. ↑ drugs.com (ed.). «Diazoxide» (en inglés). Consultado el 14 de mayo de 2012. 
  2. ↑ van Hamersvelt HW, Kloke HJ, de Jong DJ, Koene RA, Huysmans FT (agosto de 1996). «Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?». J. Hypertens. (en inglés) 14 (8): 1041-5. PMID 8884561. 
  3. ↑ Huang Q, Bu S, Yu Y, et al. (enero de 2007). «Diazoxide prevents diabetes through inhibiting pancreatic beta-cells from apoptosis via Bcl-2/Bax rate and p38-beta mitogen-activated protein kinase». Endocrinology (en inglés) 148 (1): 81-91. PMID 17053028. doi:10.1210/en.2006-0738. 
  4. ↑ Rubin, A. A.; Roth, F. E.; Winbury, M. M.; Topliss, J. G.; Sherlock, M. H.; Sperber, N.; Black, J. (1961). «New Class of Antihypertensive Agents». Science (en inglés) 133 (3470): 2067. doi:10.1126/science.133.3470.2067. 

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