Gliclazide | Genelabs.com

Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).
Brands	Diamicron Diamicron MR Glimicron Mylan-Gliclazide Nordialex PMS-Gliclazide
Categories	Hypoglycemic Agents Sulfonylureas Antidiabetic
Manufacturers	Servier Canada
Synonyms	1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea 1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea Gliclazida [INN-Spanish] Gliclazidum [INN-Latin] N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea

indication

For the treatment of NIDDM in conjunction with diet and exercise.

pharmacology

Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.

mechanism of action

Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells. This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

toxicity

LD₅₀=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.

biotransformation

Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.

absorption

Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.

half life

10.4 hours. Duration of action is 10-24 hours.

route of elimination

Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).

drug interactions

Acebutolol: Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.

Acetylsalicylic acid: Acetylsalicylic acid increases the effect of the sulfonylurea, gliclazide.

Atenolol: The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.

Betaxolol: The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia.

Bevantolol: The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.

Bismuth Subsalicylate: The salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, gliclazide.

Bisoprolol: The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.

Carteolol: The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.

Carvedilol: The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.

Chloramphenicol: Chloramphenicol may increase the effect of sulfonylurea, gliclazide.

Clofibrate: Clofibrate may increase the effect of sulfonylurea, gliclazide.

Dicumarol: Dicumarol may increase the effect of sulfonylurea, gliclazide.

Esmolol: The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.

Glucosamine: Possible hyperglycemia

Labetalol: The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.

Magnesium salicylate: The salicylate, magnesium salicylate, increases the effect of the sulfonylurea, gliclazide.

Metoprolol: The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.

Nadolol: The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.

Oxprenolol: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Penbutolol: The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia.

Phenylbutazone: Phenylbutazone increases the effect of the hypoglycemic agent

Pindolol: The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.

Practolol: The beta-blocker, practolol, may decrease symptoms of hypoglycemia.

Propranolol: The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.

Rifampin: Rifampin may decrease the effect of sulfonylurea, gliclazide.

Salicylate-sodium: The salicylate, salicylate-sodium, increases the effect of the sulfonylurea, gliclazide.

Salsalate: The salicylate, salsalate, increases the effect of the sulfonylurea, gliclazide.

Somatropin recombinant: Somatropin may antagonize the hypoglycemic effect of gliclazide. Monitor for changes in fasting and postprandial blood sugars.

Sotalol: The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.

Timolol: The beta-blocker, timolol, may decrease symptoms of hypoglycemia.

Trisalicylate-choline: The salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, gliclazide.

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