The drug is prescribed for type 2 diabetes mellitus (insulin-independent) when diet therapy and exercise regimen are ineffective. Glucophage is prescribed as a monotherapy or in combination with other hypoglycemic drugs
Gliucofaj XR Composition and form of release:
tab. prolong. act. 500 mg, No. 30, No. 60
Gliucofaj XR Pharmacological properties:
Metformin is an antiglycemic agent of the biguanide group. Reduces both baseline plasma glucose and postprandial blood glucose levels. Unlike sulfonylurea derivatives, it does not stimulate the secretion of insulin and does not lead to a hypoglycemic effect in healthy individuals.
Metformin has a triple mechanism of action:
causes a decrease in glucose production in the liver by inhibiting gluconeogenesis and glycogenolysis
improves the uptake and utilization of glucose in the blood, muscles by increasing insulin sensitivity
delays the absorption of glucose in the intestine.
Metformin stimulates intracellular glycogen synthesis by affecting glycogen synthetase. Increases the transport capacity of all types of membrane glucose transporters.
Regardless of its effect on the level of glycemia, metformin has a positive effect on lipid metabolism: it reduces the content of total cholesterol, LDL and TG.
Increases the sensitivity of peripheral receptors to insulin and glucose utilization by cells. Inhibits gluconeogenesis in the liver. Delays the absorption of carbohydrates in the intestines.
After oral administration of a sustained-release tablet, the absorption of metformin is significantly slowed down compared to that of a rapid-release tablet. The time to reach Cmax in serum is 7 hours. For a quick-release tablet, 2.5 hours.
The absorption of metformin from an extended-release tablet does not change with food intake. Cumulation was not noted with repeated administration of up to 2000 mg of metformin in the form of a sustained-release tablet.
Metformin is excreted from the body unchanged in the urine. No metabolites have been identified in humans. Renal clearance is 400 ml / min, which indicates that metformin is excreted by glomerular filtration and tubular secretion. After oral administration of the dose, T1 / 2 is about 6.5 hours. With a decrease in renal function, renal clearance decreases in proportion to creatinine clearance and therefore T increases, which leads to an increase in the level of metformin in the blood plasma.
Gliucofaj XR Indications:
type II diabetes mellitus in adults with ineffective diet therapy (especially in obese patients) as monotherapy, in combination with other oral antidiabetic agents or insulin.
both monotherapy and in combination with other oral antidiabetic agents, as well as insulin.