Gliclazide Mechanism Of Action
Mechanism of action according to product monograph.
Gliclazide mechanism of action. The molecule contains an azabicyclo octyl group which confers special properties on the basic sulphonylurea moiety. Gliclazide is an oral antihyperglycemic agent used for the treatment of non insulin dependent diabetes mellitus niddm. Sulfonylureas bind to and close atp sensitive k k atp channels on the cell membrane of pancreatic beta cells which depolarizes the cell by preventing potassium from exiting. Mechanism of action gliclazide binds to the β cell sulfonyl urea receptor sur1.
Nathan2 servier research and development fulmer slough u k. The mode of action and clinical pharmacology of gliclazide. Diabetes research and clinical practice 14 1991 s21 s36 1991 elsevier science publishers b v. Gliclazide selectively binds to sulfonylurea receptors sur 1 on the surface of the pancreatic beta cells.
The hypoglycemic action of gliclazide is related to an improvement in insulin secretion from the functioning beta cells of the pancreas. It is extensively metabolised and renal clearance accounts for only 4 of total drug clearance. It potentates the insulin release improves the dynamics of insulin. Extrapancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs.
Gliclazide is a sulphonylurea drug with an intermediate half life of around 11 hours. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of. The primary mode of action of glipizide in experimental animals appears to be the stimulation of insulin secretion from the beta cells of pancreatic islet tissue and is thus dependent on functioning beta cells in the pancreatic islets. Citation needed mechanism of action.
Diagram of glucose reduction and insulin release in the pancreas. And 27ris courbevoie cedex france summary gliclazide is a sulphonylurea drug with an. It has been classified differently according to its drug properties in which based on its chemical structure gliclazide is considered a first generation sulfonylurea due to the structural presence of a sulfonamide group able to release a proton and the presence of one. Blood sugar control persists in some patients for up to 24 hours after a single dose of glucotrol even though plasma levels have declined to a small fraction of peak levels by that time see pharmacokinetics below.
This binding subsequently blocks the atp sensitive potassium channels. Gliclazide overdose may cause severe hypoglycemia requiring urgent administration of glucose by iv and monitoring. 0168 8227 91 03 50 s21 diabet 00563 the mode of action and clinical pharmacology of gliclazide.