Diazoxide
Medication used to treat low blood sugar and high blood pressure
From Wikipedia, the free encyclopedia
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.[5] This includes islet cell tumors that cannot be removed and leucine sensitivity.[5] It can also be used in refractory cases of sulfonylurea toxicity.[6] It is taken by mouth.[5]
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- AU: C
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| Trade names | Proglycem, Vykat XR, others |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Oral, intravenous |
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| Protein binding | >90%[4] |
| Metabolism | Liver oxidation and sulfate conjugation |
| Elimination half-life | Adults: 24–36 hours[4] Children: 9.5–24 hours[4] |
| Excretion | Kidney |
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| ECHA InfoCard | 100.006.063 |
| Chemical and physical data | |
| 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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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 (PWS).[3] It was approved for this use in the United States in March 2025.[7]
Common side effects include high blood sugar, fluid retention, low blood platelets, a fast heart rate, increased hair growth, and nausea.[5] Other severe side effects include pulmonary hypertension and heart failure.[5] It is chemically similar to thiazide diuretics.[5] It works by decreasing insulin release from the pancreas and increasing glucose release by the liver.[5]
Diazoxide was approved for medical use in the United States in 1973.[5] It is on the World Health Organization's List of Essential Medicines.[8] It is available as a generic medication.[9]
Medical uses
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[10]
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)[11] or congenital hyperinsulinism.
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.[6]
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]
Diazoxide has been associated with development of hypertrichosis and stimulation of scalp hair growth.[14][15]
Pharmacology
Pharmacodynamics
Diazoxide acts as a ATP-sensitive potassium channel (KATP) opener.[16]
It has been found to act as a positive allosteric modulator of the ionotropic glutamate AMPA and kainate receptors.[17]
Pharmacokinetics
The elimination half-life of diazoxide has been reported to be 24 to 36 hours in adults and 9.5 to 24 hours in children.[4]
Research
Diazoxide was under development by Lakatos-Topol and Proanagen as a topical solution for the treatment of androgenic alopecia (pattern hair loss) and alopecia areata in the 1980s but was ultimately never marketed.[18][19] It was intended as a competitor and alternative to minoxidil (Rogaine) for such purposes.[18][19] The drug applied topically was found to promote scalp hair growth in balding stump-tailed macaques.[20][21][22][23]
Under the name Vykat XR, diazoxide choline is an approved therapy for Prader-Willi syndrome[3][24][25][26] and is under investigation for monogenic obesity caused by mutations in the SH2B1, PCSK1, or SIM1 genes.[27]
