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 category	AU: C US: C (Risk not ruled out)
Legal status	UK: POM (Prescription only) US: ℞-only
Routes of administration	Oral, intravenous
Pharmacokinetic data
Protein binding	90%
Metabolism	Hepatic oxidation and sulfate conjugation
Biological half-life	21-45 hours
Excretion	Renal
Identifiers
CAS Number	364-98-7 Y
ATC code	C02DA01 (WHO) V03AH01
PubChem	CID: 3019
IUPHAR/BPS	2409
DrugBank	DB01119 Y
ChemSpider	2911 Y
UNII	O5CB12L4FN Y
KEGG	D00294 Y
ChEBI	CHEBI:4495 Y
ChEMBL	CHEMBL181 Y
Chemical data
Formula	C8H7ClN2O2S
Molecular mass	230.672 g/mol
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
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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.

Uses

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.

Side effects

Diazoxide interferes with insulin release through its action on potassium channels. 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.

See also

• Hydrochlorothiazide (HCTZ)