Diazoxide

Diazoxide
Diazoxide
Systematic (IUPAC) name
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Clinical data
Trade names Proglycem
AHFS/Drugs.com monograph
Pregnancy cat. C(AU) C(US)
Legal status POM (UK) -only (US)
Routes Oral, intravenous
Pharmacokinetic data
Protein binding 90%
Metabolism Hepatic oxidation and sulfate conjugation
Half-life 21-45 hours
Excretion Renal
Identifiers
CAS number 364-98-7 YesY
ATC code C02DA01 V03AH01
PubChem CID 3019
IUPHAR ligand 2409
DrugBank APRD00914
ChemSpider 2911 YesY
UNII O5CB12L4FN YesY
KEGG D00294 YesY
ChEBI CHEBI:4495 YesY
ChEMBL CHEMBL181 YesY
Chemical data
Formula C8H7ClN2O2S 
Mol. mass 230.672 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Diazoxide (INN; brand name Proglycem[1]) 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

Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[2]

Diazoxide also inhibits the secretion of insulin from the pancreas, thus it is used to counter hypoglycemia in disease states such as insulinoma (a tumor producing insulin)[3] or congenital hyperinsulinism.

Chemistry

Diazoxide can be prepared from dichloronitrobenzene:[4] Diazoxide.png

References

  1. ^ Diazoxide, drugs.com
  2. ^ van Hamersvelt HW, Kloke HJ, de Jong DJ, Koene RA, Huysmans FT (August 1996). "Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?". J. Hypertens. 14 (8): 1041–5. PMID 8884561. 
  3. ^ Huang Q, Bu S, Yu Y, et al. (January 2007). "Diazoxide prevents diabetes through inhibiting pancreatic beta-cells from apoptosis via Bcl-2/Bax rate and p38-beta mitogen-activated protein kinase". Endocrinology 148 (1): 81–91. doi:10.1210/en.2006-0738. PMID 17053028. http://endo.endojournals.org/cgi/pmidlookup?view=long&pmid=17053028. 
  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 133 (3470): 2067. doi:10.1126/science.133.3470.2067. 

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  • diazoxide — di·az·ox·ide …   English syllables

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  • Congenital hyperinsulinism — is a medical term referring to a variety of congenital disorders in which hypoglycemia is caused by excessive insulin secretion. Congenital forms of hyperinsulinemic hypoglycemia can be transient or persistent, mild or severe. These conditions… …   Wikipedia

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