Metformin is an oral antidiabetic medication used as the first line treatment option for type 2 diabetes.
It is also used in the treatment of gestational diabetes, polycystic ovarian syndrome, and for the prevention of diabetes in pre diabetic individuals.
It this video, our primary goal is to explore the mechanism of action of metformin.
Metformin is the only drug belonging to the biguanide class of medications.
Its main action is to reduce blood glucose levels by inhibiting new glucose formation in the liver, which is also called gluconeogenesis.
It does this by increasing the activity of an enzyme called adenosine mono phosphate activated protein kinase, or AMPK for short.
After entering the cells, metformin inhibits the mitochondrial respiratory chain complex, resulting in reduced ATP production, which is the primary stimulus for the activation of AMPK.
AMPK is a key regulator of energy homeostasis within the cells.
Activation of this enzyme causes an increase in overall cellular catabolism, while reducing anabolic mechanisms.
It reduces gluconeogenesis by inhibiting genes responsible for the synthesis of PEP carboxy kinase and glucose 6 phosphatase, which are key enzymes in the gluconeogenesis pathway.
It also increases glucose uptake from peripheral tissues, especially the muscle and fat tissues, by inducing translocation of Glut 4 into the cell membrane.
In addition to these 2 mechanisms, metformin also reduces the intestinal absorption of glucose, which further reduces blood glucose levels.
Furthermore, metformin increases the oxidation of fatty acids, decreases glycogen, protein, fatty acids, and cholesterol synthesis, and reduces LDL levels while increasing HDL, which significantly lowers the cardiovascular risk in patients with type 2 diabetes.

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