In this article we will discuss about the Mechanism of Action (MOA)- Meglitinides. So let’s get started.
Mechanism of Action
Meglitinides bind to the ATP dependent K+ channels on the cell membrane of beta cells of the pancreas in a similar manner to sulphonylureas but have a weaker affinity and faster disassociation from SUR1 binding site. It leads to increase intracellular K+ which causes the membrane to become more positive leading to depolarisation and opening of voltage gated Calcium channels, this rise in intracellular calcium leads to increase fusion of insulin granulae in the cell membrane and therefore increased secretion of pro-insulin. Meglitinides have a short onset of action and short half life. Repaglinide have shown to reduce HbA1c level by 0.5 to 2% whereas FPG level by 65-75 mg/dl.
