Active ingredient: Gliclazide - Basic Profile / Key Facts

Basic Profile / Key Facts

Drug Category

• Hypoglycemic Agents
• Sulfonylureas

Dosage Forms

• Tablet

Indications

For the treatment of Diabetes mellitus

Pharmacology

Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates beta 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 beta 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 beta cells. This opens voltage-dependent calcium channels in the beta cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

Absorption

Rapidly and well absorbed but may have wide inter- and intra-individual variability.

Toxicity

LD₅₀=3000 mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Not Available

Drug Interactions

Not Available