Diazoxide

Diazoxide, sold under the brand name Proglycem among others, is a medication used to treat low blood sugar due to a number of specific causes.^[4] This includes islet cell tumors that cannot be removed and leucine sensitivity.^[4] It can also be used in refractory cases of sulfonylurea toxicity.^[5] It is taken by mouth.^[4]

Diazoxide

Clinical data
Trade names	Proglycem, others
AHFS/Drugs.com	Monograph
License data	US DailyMed: Diazoxide
Pregnancy category	AU: C
Routes of administration	By mouth, intravenous
ATC code	C02DA01 (WHO) V03AH01 (WHO)
Legal status
Legal status	CA: ℞-only[1] UK: POM (Prescription only) US: ℞-only[2][3]
Pharmacokinetic data
Protein binding	90%
Metabolism	Liver oxidation and sulfate conjugation
Elimination half-life	21-45 hours
Excretion	Kidney
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
CompTox Dashboard (EPA)	DTXSID7022914
ECHA InfoCard	100.006.063
Chemical and physical data
Formula	C8H7ClN2O2S
Molar mass	230.67 g·mol−1
3D model (JSmol)	Interactive image
Melting point	330 to 331 °C (626 to 628 °F)
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, used as the salt diazoxide choline, and sold under the brand name Vykat XR, is used for the treatment of hyperphagia in people with Prader-Willi syndrome.^[3] It was approved for this use in the United States in March 2025.^[6]

Common side effects include high blood sugar, fluid retention, low blood platelets, a fast heart rate, increased hair growth, and nausea.^[4] Other severe side effects include pulmonary hypertension and heart failure.^[4] It is chemically similar to thiazide diuretics.^[4] It works by decreasing insulin release from the pancreas and increasing glucose release by the liver.^[4]

Diazoxide was approved for medical use in the United States in 1973.^[4] It is on the World Health Organization's List of Essential Medicines.^[7] It is available as a generic medication.^[8]

Medical uses

Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.^[9]

Diazoxide also inhibits the secretion of insulin by opening ATP-sensitive potassium channel of beta cells of the pancreas; thus, it is used to counter hypoglycemia in disease states such as insulinoma (a tumor producing insulin)^[10] or congenital hyperinsulinism.

Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.^[11]

Side effects

Diazoxide interferes with insulin release through its action on potassium channels.^[12] 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.^[5]

The US Food and Drug Administration (FDA) published a safety announcement in July 2015 highlighting the potential for development of pulmonary hypertension in newborns and infants treated with this drug.^[13]

Research

Diazoxide, formulated as its choline salt diazoxide choline, is an experimental antiobesity drug being tested in people with Prader-Willi syndrome^[14][15][16] and monogenic obesity caused by mutations in the SH2B1, PCSK1, or SIM1 genes.^[17]