Diazoxide

Diazoxide

Clinical data
Trade names	Proglycem
AHFS/Drugs.com	Monograph
Pregnancy category	AU: C US: C (Risk not ruled out)
Routes of administration	Oral, intravenous
ATC code	C02DA01 (WHO) V03AH01 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Protein binding	90%
Metabolism	Hepatic oxidation and sulfate conjugation
Biological half-life	21-45 hours
Excretion	Renal
Identifiers
IUPAC name 7-Chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
CAS Number	364-98-7 Y
PubChem CID	3019
IUPHAR/BPS	2409
DrugBank	DB01119 Y
ChemSpider	2911 Y
UNII	O5CB12L4FN
KEGG	D00294 Y
ChEBI	CHEBI:4495 Y
ChEMBL	CHEMBL181 Y
ECHA InfoCard	100.006.063
Chemical and physical data
Formula	C8H7ClN2O2S
Molar mass	230.672 g/mol
3D model (Jmol)	Interactive image
SMILES Clc1ccc2c(c1)S(=O)(=O)/N=C(\N2)C
InChI 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) Y Key:GDLBFKVLRPITMI-UHFFFAOYSA-N Y

Diazoxide (INN; brand name Proglycem) 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.

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

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) or congenital hyperinsulinism.

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

Diazoxide interferes with insulin release through its action on potassium channels. Diazoxide is one of the most potent openers of the K+ ATP channels present on the insulin producing beta cells of the pancreas. Opening these channels leads to hyperpolarization of cell membrane, a decrease in calcium influx, and a subsequently reduced release of insulin. This mechanism of action is the mirror opposite of that of Sulfonylureas, a class of medications used to increase insulin release in Type 2 Diabetics. 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.