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
Humans and other mammals
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.
