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Glucophage SR (Metformin)
Oral hypoglycemic drug of biguanide group (dimethylbiguanide). The mechanism of action of metformin is related to its ability to inhibit gluconeogenesis, as well as the formation of free fatty acids and fat oxidation. It increases the sensitivity of peripheral receptors to insulin and glucose utilization by cells. Metformin does not affect the amount of insulin in blood, but changes its pharmacodynamics by reducing the ratio of bound to free insulin and increasing the ratio of insulin to proinsulin.
Metformin stimulates glycogen synthesis by acting on glycogen synthetase. Increases transport capacity of all types of membrane glucose transporters. Delays glucose absorption in the intestine.
Reduces triglycerides, LDL, LDLNP. Metformin improves blood fibrinolytic properties by inhibiting tissue-type plasminogen activator inhibitor.
Against the background of metformin administration, the patient's body weight either remains stable or decreases moderately.
Contraindications to use
Acute or chronic metabolic acidosis, diabetic ketoacidosis, diabetic precoma and coma; renal failure, renal dysfunction (CK<60 ml/min); dehydration, severe infection, hypoglycemic shock, which may lead to renal dysfunction; clinically expressed symptoms of acute and chronic diseases that may lead to the development of tissue hypoxia (including cardiac failure, acute myocardial infarction, respiratory failure); use of contrast iodine-containing substances for intravascular administration (including cardiac insufficiency, acute myocardial infarction, hypoxia). including heart failure, acute myocardial infarction, respiratory failure); use of iodine contrast agents for intravascular administration (including during IV urography, IV cholangiography, angiography, CT); acute alcohol intoxication, chronic alcoholism; hypersensitivity to metformin.
Use in pregnancy and lactation
Adequate and strictly controlled safety studies of metformin use in pregnancy have not been conducted. Administration in pregnancy is possible in cases of extreme necessity, when the expected benefits of therapy for the mother exceed the possible risk to the fetus. Glucophage SR (Metformin) crosses the placental barrier.
Glucophage SR (Metformin) is excreted in small amounts with breast milk, and the concentration of metformin in breast milk may be 1/3 of the concentration in mother's plasma. Side effects in newborns during breastfeeding against the background of metformin administration have not been observed. However, due to the limited data, its use during breastfeeding is not recommended. The decision to stop breastfeeding should be made taking into account the benefits of breastfeeding and the potential risk of side effects in the child.
Preclinical studies have shown that metformin has no teratogenic effect at doses that are 2-3 times higher than the therapeutic doses used in humans. Glucophage SR (Metformin) has no mutagenic potential and has no effect on fertility.
Use in elderly patients
Glucophage SR (Metformin) is not recommended for use in patients over 60 years of age, which is associated with an increased risk of lactic acidosis.
Glucophage SR (Metformin) active ingredient indications
Type 2 diabetes mellitus (insulin-independent) in ineffective diet therapy and physical activity, in patients with obesity: in adults - as monotherapy or in combination with other oral hypoglycemic agents or with insulin; in children aged 10 years and older - as monotherapy or in combination with insulin.
It is taken orally, during or after meals.
The dose and frequency of administration depend on the therapy regimen, the patient's age and the dosage form used.