Drug information of Gliclazide
Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM)
Mechanism of effect
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.
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.
Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration. 94%, highly bound to plasma proteins Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%). Half life:10.4 hours
Drug indicationsdiabetes mellitus type2
Drug contraindicationsActive liver disease , bowel obstruction , recent surgery or trauma , Acute or chronic metabolic acidosis , diabetic ketoacidosis , gastric retention
InteractionsAmitriptyline , Erythromycin , Propranolol , Sotalol , Glibenclamide , Aripiprazole , Aprepitant , Olanzapine , Paroxetine , Fluoxetine , Levofloxacin , Warfarin , Metoprolol , Somatropin-Human Growth hormone , Carvedilol , Clozapine , Sitagliptin , Bisoprolol
Points of recommendation
Avoid alcohol. Take without regard to meals. A consistent diet is recommended to reduce the risk of hypoglycemia.