Drug information of Gliclazide

Gliclazide

Drug group: blood sugar

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.

Pharmacodynamic

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.

Pharmacokinetics

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 indications

diabetes mellitus type2

Points of recommendation

Avoid alcohol. Take without regard to meals. A consistent diet is recommended to reduce the risk of hypoglycemia.

Pregnancy level

C

Related drugs

Glimepiride


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