Diazoxide, sold under the brand name Proglycem and 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 generally taken by mouth.[1]
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Trade names | Proglycem, Balila |
AHFS/Drugs.com | Monograph |
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Routes of administration | By mouth, intravenous |
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Protein binding | 90% |
Metabolism | Liver oxidation and sulfate conjugation |
Elimination half-life | 21-45 hours |
Excretion | Kidney |
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ECHA InfoCard | 100.006.063 |
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Formula | C8H7ClN2O2S |
Molar mass | 230.67 g·mol−1 |
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Melting point | 330 to 331 °C (626 to 628 °F) |
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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.[3][4] It is available as a generic medication.[5]
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[6]
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)[7] or congenital hyperinsulinism.
Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[8]
Diazoxide interferes with insulin release through its action on potassium channels.[9] 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] 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.[10]
Diazoxide, formulated as its choline salt diazoxide choline, is an experimental antiobesity drug being tested in people with Prader-Willi syndrome[11][12][13] and monogenic obesity caused by mutations in the SH2B1, PCSK1, or SIM1 genes.[14]