2011-04-25

Hyperstat

Diazoxide

Diazoxide
Systematic (IUPAC) name
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Identifiers
CAS number 364-98-7
ATC code C02DA01 V03AH01
PubChem CID 3019
IUPHAR ligand 2409
DrugBank APRD00914
ChemSpider 2911
UNII O5CB12L4FN
KEGG D00294
ChEMBL CHEMBL181
Chemical data
Formula C8H7ClN2O2S
Mol. mass 230.672 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Protein binding 90%
Metabolism Hepatic oxidation and sulfate conjugation
Half-life 21-45 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat. C(AU) C(US)
Legal status POM (UK) -only (US)
Routes Oral, intravenous
Yes(what is this?) (verify)

Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.

Uses

It is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.

It is also used to decrease hypoglycemia due to the secretion of insulin in disease states such as insulinoma (a tumor producing insulin) or congenital hyperinsulinism.

Chemistry

Diazoxide.png

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 133: 2067. doi:10.1126/science.133.3470.2067.

References






Retrieved from : http://en.wikipedia.org/wiki/Diazoxide