extended-release Tablets.

drug description

Oral hypoglycemic agents, except insulin. Biguanides. PBX code A10V A02.


diabetes mellitus type 2 (insulin-independent) in adults (especially in patients with excess body weight) with poor diet and exercise, as monotherapy or in combination with other oral hypoglycemic drugs or with insulin.



  • hypersensitivity to Metformin or to any other component of the drug;
  • diabetic ketoacidosis, diabetic coma;
  • renal failure or impaired renal function (creatinine clearance
  • acute conditions at risk of developing renal impairment, such as:

dehydration, severe infectious diseases, shock


  • The


  • acute and chronic diseases that can lead to the development of hypoxia:

heart or respiratory failure, recent myocardial infarction, shock


  • The

    sumption, liver failure or any condition associated with hypoxia.

lactic Acidosis can occur in the form of muscle cramps with abdominal pain and s

  • patients with normal kidney function at least once a year;
  • in patients with impaired renal function and in elderly patients aged at least 2-4 times a year.

caution Should be exercised in cases where kidney function may be impaired, for

Interaction with other medicinal products and other forms of interaction

Combinations that are not recommended.

Acute alcohol intoxicationis associated with an increased risk of lactic acidosis, especially in cases of starvation or low-calorie diet, as well as liver failure. In the treatment of drug Glucophage XR avoid drinking alcohol and medicines containing alcohol.

Iodinated x-ray contrast agentscan lead to the development of lactic acidosis in patients with diabetes mellitus at the background of functional renal failure. The use of xr Glucophage should be discontinued prior to research and should not be resumed earlier than 48 hours after x-ray examination and evaluation of kidney function.

Combinations that should be used with caution.

Medicines, providing gipoglikemisirutee action (corticosteroids systemic and local action, sympathomimetics, chlorpromazine). It is necessary to constantly monitor blood glucose levels, especially at the beginning of treatment. During and after the termination of such joint therapy, it is necessary to adjust the dose of Glucophage XR under the control of glycemic level.

ACE Inhibitorscan reduce the level of glucose in the blood. If necessary, you should adjust the dosage of the drug during joint therapy.

Diuretics, especially loop diuretics,may increase the risk of lactic acidosis.


Pharmacological properties


Metformin – biguanide with antihyperglycemic effect. Reduces blood plasma as the initial level of glucose and glucose levels after meals. It does not stimulate insulin secretion and does not cause hypoglycemic effect.

Metformin acts in three ways:



  • leads to a decrease in glucose production in the liver by inhibiting gluconeogenesis and glycogenolysis;
  • improves insulin sensitivity in the muscles by improving the capture and utilization of peripheral glucose
  • delays the absorption of glucose in the intestine.

Metformin stimulates intracellular glycogen synthesis by acting on glycogen. Increases transport capacity of all types of membrane glucose transporters (GLUT).

Regardless of its effect on blood glucose levels, Metformin has a positive effect on lipid metabolism: it reduces the content of total cholesterol, low density lipoproteins and triglycerides.



.after taking long-release xr Glucophage tablets, the time to reach the maximum plasma concentration (Tmax) is 7:00 (Tmaxfor fast-release tablets is 2.5 hours).

At the equilibrium state, as the use of tablets with quick release, maximum concentration (max) and area under the curve AUC increase disproportionately ingested dose. AUC after a single oral administration of 2000 mg of Metformin in the form of prolonged release tablets similar to AUC, observed after taking 1000 mg of Metformin in the form of rapid release tablets twice a day.

Fluctuations WITHmaxand AUC in individual subjects in the case of taking Metformin tablets with prolonged release compared to the fluctuations observed in the case of taking Metformin tablets with rapid release.

After taking the tablets with extended release on an empty stomach was observed a decrease in AUC by 30% (Cmaxand Tmaxremained unchanged).

the Absorption of Metformin from prolonged release tablets does not change depending on the composition of the food. There is no cumulation with repeated intake of up to 2000 mg of Metformin in the form of tablets with prolonged release.

Distribution.Linking blood plasma proteins is negligible. Metformin penetrates the red blood cells. The maximum concentration in the blood is lower than the maximum concentration in the blood plasma, and is achieved through the same time. Red blood cells most likely represent a secondary compartment of distribution. The average volume of distribution (Vd) ranges from 63-276 l.

Metabolism.Metformin is excreted unchanged in the urine. Metabolites in humans have not been found.

Output.the Renal clearance of Metformin is>400 ml/min, indicating that Metformin is excreted by glomerular filtration and tubular secretion. After dose, the half-life is about 6.5 hours. Renal clearance decreases in proportion to creatinine clearance and therefore the half-life period increases, which leads to an increase in the level of Metformin in blood plasma.

Basic physical and chemical properties

white or almost white, capsule-shaped biconvex with an engraving of “500” on one side.


shelf Life

3 years.

storage Conditions

Store at a temperature not exceeding 25isC. Keep out of reach of children.



15 tablets in a blister. 2 or 4 blisters in a cardboard box.


Category vacation

According to the recipe.



merc Santa S. A. s … France/Merck Sante sas, France.



2 Rue du Pressoir Saint, 45400 Semois, France/2 rue du Pressoir Vert, 45400 Semoy, France.


Glucophage XR 500mg it is used to lower blood sugar levels. Despite the trade mark of the drug as Glucophage XR, in the international classification it is designated as “Metformin”.

intended use:


  • TheSide effects

At the beginning of the course, perhaps the lack of appetite, slight stomach aches and nausea. After a few days of taking the drug symptoms disappear.