Blood Glucose Lowering Drug (Sulfonylurea).
Pharmacology: Pharmacodynamics: Gliclazide (Glimyx) is a second-generation oral hypoglycemic sulfonylurea that stimulates the release of insulin from functioning pancreatic β-cells. This is mediated by an increase in the intracellular ratio of ATP/ADP, which inhibits K+-ATP channels. In addition, there is evidence that Gliclazide has action on peripheral tissues. This has been shown to enhance glycogen synthesis and inhibit glycogenolysis and gluconeogenesis in the liver. This may also improve peripheral glucose uptake by muscles. It reduces hepatic glucose output while stimulating insulin release from pancreatic cells by promoting Ca+2 transport across the cell membranes.
Pharmacokinetics: Absorption: Gliclazide is completely absorbed. Food intake does not affect the rate or degree of absorption.
Plasma levels increase progressively during the first 6 hours, reaching a plateau that is maintained from the sixth to the twelfth hour after administration. Intra-individual variability is low.
Distribution: Plasma protein binding is approximately 95%. The volume of distribution is around 30 liters. A single daily intake of Glimyx 60 mg maintains effective gliclazide plasma concentrations over 24 hours.
Metabolism: Gliclazide is mainly metabolized in the liver and excreted in the urine: less than
1% of the unchanged form is found in the urine. No active metabolites have been detected in plasma.
Elimination: The elimination half-life of Gliclazide varies between 12 and 20 hours.
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