Trade names Proglycem CAS ID 364-98-7 | AHFS/Drugs.com Monograph Molar mass 230.672 g/mol Protein binding 90% | |
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Pregnancycategory AU: CUS: C (Risk not ruled out) ATC code C02DA01 (WHO) V03AH01 (WHO) Legal status UK: POM (Prescription only)US: ℞-only | ||
Treating congenital hyperinsulinism chi with diazoxide
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.
Contents
In the United States, this agent is typically given in hospital.
Uses
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.
Diazoxide also inhibits the secretion of insulin from the pancreas, thus it is used to counter hypoglycemia in disease states such as insulinoma (a tumor producing insulin) or congenital hyperinsulinism.
Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.
Side effects
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.
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.