Glimepiride
China [CN] Glimepirea is a long-acting antidiabetic drug of the third-generation sulfonylurea class. The main mechanism of its hypoglycemic effect is to stimulate pancreatic β cells to secrete insulin and partially increase the sensitivity of surrounding tissues to insulin. This product binds to and dissociates insulin receptors at a faster rate than glibenclamide and causes less severe hypoglycemia. Its mechanism of action is by binding to the sulfonylureas receptor (a protein with a relative molecular mass of 6.5×104) on the surface of pancreatic β -cells. This receptor is coupled with the ATP-sensitive K+ (KATP) channel, promoting the closure of the KATP channel, causing depolarization of the cell membrane, and opening the voltage-dependent calcium channel. Ga2+ influx promotes the release of insulin and inhibits the synthesis of hepatic glucose. Recent studies have shown that different sulfonylurea coal drugs have different affines for KATP. The order is: Euglycemic acid = glimepirea > methylsulfonylurea > chlorosulfonylurea. In addition, glimepiride can also increase cardiac glucose uptake through non-insulin-dependent pathways, which may be caused by the increased expression of two proteins, glucose transporter factor 1 and 4. Because the effect of glimepiride on the cardiovascular KATP channel is weaker than that of glibopiride, gliclazide and lipizide. Therefore, adverse reactions of the cardiovascular system are also very few.
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