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Diazoxide

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Diazoxide
File:Diazoxide Structural Formula V.1.svg
Systematic (IUPAC) name
7-Chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Clinical data
Trade names Proglycem
AHFS/Drugs.com monograph
  • AU: C
  • US: C (Risk not ruled out)
Oral, intravenous
Pharmacokinetic data
Protein binding 90%
Metabolism Hepatic oxidation and sulfate conjugation
Half-life 21-45 hours
Excretion Renal
Identifiers
364-98-7 7pxY
C02DA01 V03AH01
PubChem CID 3019
IUPHAR ligand 2409
DrugBank DB01119 7pxY
ChemSpider 2911 7pxY
UNII O5CB12L4FN 7pxY
KEGG D00294 7pxY
ChEBI CHEBI:4495 7pxY
ChEMBL CHEMBL181 7pxY
Chemical data
Formula C8H7ClN2O2S
230.672 g/mol
 14pxY (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, preventing calcium flux across the sarcolemma and activation of the contractile apparatus.

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.

Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[4]

Side effects

Diazoxide interferes with insulin release through its action on potassium channels.[citation needed] The efflux of potassium, as an effect of diazoxide, will lead to hyperpolarization of cell membrane that leads to decrease calcium influx. The low calcium will decrease the release of insulin. Therefore this medicine is not given to non-insulin dependent diabetic patients.

See also

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. doi:10.1097/00004872-199608000-00016. 
  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. PMID 17053028. doi:10.1210/en.2006-0738. 
  4. ^ Randle, J. C.; Biton, C; Lepagnol, J. M. (1993). "Allosteric potentiation by diazoxide of AMPA receptor currents and synaptic potentials". European journal of pharmacology 247 (3): 257–65. PMID 8307099.  edit