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Mechanism of Action. Metformin, classified as a biguanide drug, effectively lowers blood glucose levels by decreasing glucose production in the liver, diminishing intestinal absorption, and enhancing insulin sensitivity. As a result, metformin effectively lowers both basal and postprandial blood glucose levels.
Mechanism of action. Metformin's mechanisms of action are unique from other classes of oral antihyperglycemic drugs.
In this Review, we highlight the latest advances in our understanding of the mechanisms of action of metformin and discuss potential emerging novel therapeutic uses.
Metformin is an oral antihyperglycemic agent that lowers both basal and post-prandial plasma glucose in T2D. In addition to increasing insulin sensitivity, it acts by decreasing hepatic glucose synthesis and intestinal glucose absorption.
Considerable efforts have been made since the 1950s to better understand the cellular and molecular mechanisms of action of metformin, a potent antihyperglycemic agent now recommended as the first line oral therapy for type 2 diabetes (T2D).
Metformin has been shown to act via both AMP-activated protein kinase (AMPK)-dependent and AMPK-independent mechanisms; by inhibition of mitochondrial respiration but also perhaps by inhibition of mitochondrial glycerophosphate dehydrogenase, and a mechanism involving the lysosome.
Metformin is a complex drug with multiple sites of action and multiple molecular mechanisms. Physiologically, metformin acts directly or indirectly on the liver to lower glucose production, and acts on the gut to increase glucose utilisation, increase GLP-1 and alter the microbiome.