Metformin is an antidiabetic drug that promotes better absorption of glucose. The World Health Organization has included this drug in the list of essential drugs.
Metformin (dimethyl biguanide) is an anti-diabetic agent for internal use, which belongs to the class of biguanides. The effectiveness of Metformin is related to the ability of the active substance to inhibit gluconeogenesis in the body. The active substance inhibits the transport of electrons in the respiratory chain of the mitochondria. This leads to a decrease in the concentration of ATP within the cells and stimulation of glycolysis, carried out by anoxic route. As a result, glucose enters the cells from the extracellular space, production of lactate and pyruvate increases in the liver, intestines, fat and muscle tissues. The glycogen stores in the liver cells also decrease. Does not cause hypoglycemic effects, because it does not activate insulin production.
Reduces the processes of fat oxidation and inhibits the production of free fatty acids. Against the background of the use of the drug, there is a change in the pharmacodynamics of insulin due to a decrease in the ratio of insulin bound to insulin free. An increase in the ratio of insulin / proinsulin is also found. Due to the mechanism of action of the drug, a decrease in the level of glucose in the blood serum after eating, also decreases the basic glucose index. Due to the fact that the drug does not stimulate insulin production with beta cells of the pancreas, it suppresses hyperinsulinemia, which is considered one of the most important factors of weight gain in diabetes mellitus and the progression of vascular complications. Reducing glucose levels is due to improved absorption of glucose by muscle cells and an increase in the sensitivity of peripheral receptors to insulin. In healthy people (without diabetes), when taking metformin, a decrease in glucose levels is not observed. Metformin helps to reduce body weight in obesity and diabetes by suppressing appetite, reducing glucose absorption from food in the gastrointestinal tract and stimulating anaerobic glycolysis.
Metformin also has a fibrinolytic effect due to the inhibition of PAI-1 (an inhibitor of tissue-type plasminogen activator) and t-PA (tissue plasminogen activator).
The drug stimulates the process of biotransformation of glucose into glycogen, activates blood circulation in the hepatic tissue. A hypolipidemic property: reduces the level of LDL (low-density lipoproteins), triglycerides (by 10-20% even under the condition of an initial increase of 50%) and VLDLP (very low density lipoproteins). Due to metabolic effects, metformin causes an increase in the level of HDLP (high-density lipoproteins) by 20-30%.
On the part of the system of the digestive system: nausea, vomiting, metallic taste in the mouth, loss of appetite, diarrhea, flatulence, abdominal pain. These symptoms are particularly common at the beginning of treatment and usually disappear on their own. These symptoms can be reduced by the appointment antotsidov derivatives of atropine or antispasmodics.
From a metabolism: in rare cases – lactic acidosis (requires discontinuation of treatment); long-term treatment – In hypovitaminosis 12 (malabsorption).
From the side of hematopoiesis: in some cases – megaloblastic anemia.
From the Endocrine: hypoglycemia.
Allergic reactions: skin rash.