Drug Groups

approved

Description

A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. [PubChem]

Indication

Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma.

Pharmacology

Diazoxide 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 which inhibits the generation of an action potential.

Toxicity

Oral LD₅₀ in rat and mouse: 980 mg/kg and 444 mg/kg, respectively.

Affected Organisms

Biotransformation

Hepatic.

Absorption

Readily absorbed following oral administration.

Half Life

28 ±8.3 hours in normal adults.

Protein Binding

Very high (more than 90%) to serum proteins.

Elimination

Proglycem is extensively bound (more than 90%) to serum proteins, and is excreted in the kidneys.

External Links