|By mouth, intravenous|
|Metabolism||Liver oxidation and sulfate conjugation|
|Elimination half-life||21-45 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||230.672 g/mol g·mol−1|
|3D model (JSmol)|
Diazoxide, sold under the brand name Proglycem, is a medication used to treat low blood sugar due to a number of specific causes. This includes islet cell tumors that cannot be removed and leucine sensitivity. It can also be used in refractory cases of sulfonylurea toxicity. It is generally taken by mouth.
Common side effects include high blood sugar, low blood platelets, a fast heart rate, and nausea. It 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.
Diazoxide was approved for medical use in the United States in 1973. It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system. In the United States as of 2019 it costs about US$1500 per month.
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) or congenital hyperinsulinism.
Diazoxide interferes with insulin release through its action on potassium channels. 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. 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.
Typical dose is 3mg/kg * 70 kg * 30 days = 6,300 mg at 11.58 per 50 mg