Diazoxide

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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.[1] This includes islet cell tumors that cannot be removed and leucine sensitivity.[1] It can also be used in refractory cases of sulfonylurea toxicity.[2] It is taken by mouth.[1]

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.[4]

Common side effects include high blood sugar, fluid retention, low blood platelets, a fast heart rate, increased hair growth, and nausea.[1] Other severe side effects include pulmonary hypertension and heart failure.[1] It is chemically similar to thiazide diuretics.[1] It works by decreasing insulin release from the pancreas and increasing glucose release by the liver.[1]

Diazoxide was approved for medical use in the United States in 1973.[1] It is on the World Health Organization's List of Essential Medicines.[5] It is available as a generic medication.[6]

Medical uses

Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[7]

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)[8] or congenital hyperinsulinism.

Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[9]

Side effects

Diazoxide interferes with insulin release through its action on potassium channels.[10] 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.[2]

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.[11]

Research

Diazoxide, formulated as its choline salt diazoxide choline, is an experimental antiobesity drug being tested in people with Prader-Willi syndrome[12][13][14] and monogenic obesity caused by mutations in the SH2B1, PCSK1, or SIM1 genes.[15]

References

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  15. ↑ Clinical trial number NCT05532020 for "An Open-Label Study of Diazoxide Choline in Patients With Genetic Obesities" at ClinicalTrials.gov

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