Diazoxide

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Diazoxide

Chemical structure of Diazoxide

Diazoxide is a medication primarily used to treat hypoglycemia due to hyperinsulinism, and it is also used as a vasodilator in the management of hypertensive emergencies. It works by inhibiting the release of insulin from the pancreas and by relaxing smooth muscle cells in the blood vessels.

Mechanism of Action

Diazoxide acts by opening potassium channels in the beta cells of the pancreas, which leads to hyperpolarization of the cell membrane and inhibition of insulin release. This action is beneficial in conditions where there is excessive insulin production, such as congenital hyperinsulinism.

As a vasodilator, diazoxide relaxes the smooth muscle in the peripheral arterioles, leading to a decrease in peripheral vascular resistance and a subsequent drop in blood pressure.

Medical Uses

Treatment of Hypoglycemia

Diazoxide is used in the management of hypoglycemia caused by excessive insulin secretion. It is particularly useful in conditions like insulinoma and congenital hyperinsulinism. By reducing insulin secretion, diazoxide helps to maintain normal blood glucose levels.

Hypertensive Emergencies

In the past, diazoxide was used in the treatment of hypertensive emergencies due to its rapid vasodilatory effects. However, its use in this context has decreased with the availability of newer antihypertensive agents.

Side Effects

Common side effects of diazoxide include fluid retention, hyperglycemia, and tachycardia. Due to its effects on blood glucose levels, it can cause significant hyperglycemia, especially in patients with diabetes mellitus.

Pharmacokinetics

Diazoxide is administered orally or intravenously. It is highly protein-bound and has a long half-life, which allows for less frequent dosing. The drug is metabolized in the liver and excreted primarily in the urine.

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Contributors: Prab R. Tumpati, MD