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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)
Legal status
Routes of
Oral, intravenous
Pharmacokinetic data
Protein binding 90%
Metabolism Hepatic oxidation and sulfate conjugation
Biological half-life 21-45 hours
Excretion Renal
CAS Number 364-98-7 YesY
ATC code C02DA01 V03AH01
PubChem CID: 3019
DrugBank DB01119 YesY
ChemSpider 2911 YesY
KEGG D00294 YesY
Chemical data
Formula C8H7ClN2O2S
Molecular mass 230.672 g/mol
 YesY (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.

In the United States, this agent is typically given in hospital.[2]


Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[3]

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)[4] or congenital hyperinsulinism.

Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[5]

Side effects[edit]

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.

The Food and Drug Administration published a Safety Announcement in July 2015 highlighting the potential for development of pulmonary hypertension in newborns and infants treated with this drug.[2]

See also[edit]


  1. ^ Diazoxide, drugs.com
  2. ^ a b "FDA Drug Safety Communication: FDA warns about a serious lung condition in infants and newborns treated with Proglycem (diazoxide)" (Press release). Food and Drug Administration. July 16, 2015. Retrieved 2015-07-19. 
  3. ^ 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?". Journal of Hypertension 14 (8): 1041–5. doi:10.1097/00004872-199608000-00016. PMID 8884561. Closed access
  4. ^ 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. open access publication - free to read
  5. ^ Randle, John C.R.; Biton, Catherine; Lepagnol, Jean M. (15 November 1993). "Allosteric potentiation by diazoxide of AMPA receptor currents and synaptic potentials". European Journal of Pharmacology 247 (3): 257–65. doi:10.1016/0922-4106(93)90193-D. PMID 8307099. Closed access