|Metabolism||Hepatic oxidation and sulfate conjugation|
|Elimination half-life||21-45 hours|
|Chemical and physical data|
|Molar mass||230.672 g/mol|
|3D model (JSmol)|
Diazoxide (INN; brand name Proglycem) 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.
In the United States, this agent is only available in the oral form and is typically given in hospital settings.
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.
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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.
- Diazoxide, drugs.com
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[Category:AMPA receptor positive allosteric modulators]