An oral rapid and short-acting anti-diabetic drug of the sulfonylurea class.
A second generation sulfonylurea agent.
Undergoes enterohepatic circulation.
Second-generation sulfonylureas are more potent and have shorter half-lives than the first-generation agents.
Mechanism of action is by blocking potassium channels in the beta cells of the islets of Langerhans, causing cells to remain depolarized, increasing the time of calcium release, which results in calcium influx signaling.
Increasing intracellular calcium initiates greater insulin release from each beta cell.
It may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues.
Brand name Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL in doses of 2.5, 5, and 10 milligrams.