Diazoxide

DB01119ApprovedInvestigationalSmall moleculeDirect Vasodilators

Diazoxide is a non diuretic benzothiadiazine indicated for the management of hypoglycemia in patients who produce an excess of insulin caused by a variety of conditions. Diazoxide is a non-diuretic benzothiadiazine derivative that activates ATP-sensitive potassium channels.

Mechanism: Diazoxide is a nondiuretic benzothiadiazine derivative used for the management of symptomatic hypoglycemia. By binding to the sulfonylurea receptor (SUR) subunit of the ATP-sensitive potassium channel (KATP) on the membrane of pancreatic beta‐cells, diazoxide promotes a potassium efflux from beta-cells. This hyperpolarizes the cell membrane and prevents the influx of calcium to the pancreatic beta‐cells. Without a sufficient amount of calcium in the cell, insulin release is inhibited. Therefore, the use of diazoxide produces an increase in glucose levels. Diazoxide is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity. It also exhibits hypotensive activity by reducing arteriolar smooth muscle and vascular resistance. The mechanism of action of its hypotensive effect has not been fully elucidated; however, it is possible that it involves the antagonism of calcium.
Curator reviewed · 5 references
Primary indication: Oral diazoxide is indicated to manage hypoglycemia due to hyperinsulinism associated with conditions such as inoperable islet cell adenoma or carcinoma, and extrapancreatic malignancy in adults, or leucine sensitivity, islet cell hyperplasia, nesidioblastosis, extrapancreatic malignancy,...Curator reviewed · 10 structured indications
Formula / weight: C₈H₇ClN₂O₂S · 230.671 g/mol (avg)
First approval: Canada, 2011 · United States, 1973
Code names: NSC-64198 · NSC-76130 · SCH-6783 · SRG-95213
Brand names: Proglycem
Vykat