Expiration date: 06/2025

Structure and Composition:

Tablets, film-coated. One tablet contains, active substance:

500, 850 or 1000 mg of metformin hydrochloride

Excipients: Povidone - 20, 34 or 40 mg Magnesium stearate - 5, 8.5 or 10 mg

in blister 10 pcs., in a cardboard pack 3 or 5 blisters in a blister pack of 15 pcs., in paper cartons 2 blisters in a blister pack or 20 pcs., in a cardboard pack 3 or 5 blisters (tab. 500 mg)

in blister 15 pcs., in paper cartons 2 blisters in a blister pack or 20 pcs., in a cardboard pack 3 or 5 blisters (tab. 850 mg)

in blister 10 pcs., in a cardboard pack 3, 5, 6 or 12 blisters in a blister pack or 15 pcs., in a cardboard bundle 2, 3 or 4 blisters (Table. 1000 mg).

Description pharmaceutical form:

Glucophage 500 and 850 mg: white, round, biconvex tablets, film-coated. On cross-section - a homogeneous white mass.

Glucophage 1000 mg: white, oval, biconvex tablets, film-coated, scored on both sides and marked "1000" on one side. On cross-section - a homogeneous white mass.

Characteristic:

Biguanide hypoglycemic agent of the group for oral administration.

Pharmacokinetics:

After oral administration, metformin adequately absorbed from the gastrointestinal tract. The absolute bioavailability of 50-60%. Cmax (approximately 2 g / L or 15 mmol) in plasma is reached after 2.5 hours. At the same time taking metformin absorption of food is reduced and delayed.

Metformin is rapidly distributed into the tissue, practically does not bind to plasma proteins. It is metabolised to a very small extent and excreted by the kidneys. Clearance of metformin in normal subjects was 440 ml / minute (4 times greater than creatinine clearance), indicating that the presence of active tubular secretion. T1 / 2 is about 6.5 hours. In renal insufficiency T1 / 2 increases the risk of drug accumulation occurs.

Description of the pharmacological actions:

Glucophage reduces hyperglycemia, without leading to hypoglycemia. Unlike sulfonylureas, it does not stimulate insulin secretion and has no hypoglycemic effect in healthy persons. It increases the sensitivity of peripheral receptors for insulin and disposal of glucose into cells. It inhibits gluconeogenesis in the liver. Delaying the absorption of carbohydrates in the intestine. Moreover, it has a beneficial effect on lipid metabolism: reduces total cholesterol, LDL and triglycerides.

Testimony:

• diabetes type 2 diabetes in adults
  
• in combination with insulin - for diabetes type 2 diabetes, especially in severe degree of obesity, accompanied by secondary insulin resistance
  
• Type 2 diabetes in children with the age of 10 - both in monotherapy and in combination with insulin.
  

Contraindications:

• Hypersensitivity to metformin or any of the excipients
  
• diabetic ketoacidosis, coma and precoma
  
• renal failure (Cl creatinine <60 ml / min)
  
• acute conditions with the risk of renal dysfunction: dehydration (diarrhea, vomiting), fever, severe infections, a condition of hypoxia (shock, sepsis, kidney infections, bronchopulmonary disease)
  
• symptomatic manifestations of acute and chronic diseases, which may lead to the development of tissue hypoxia (cardiac or respiratory failure, acute myocardial infarction, etc.)
  
• major surgery and trauma (when shown holding insulin)
  
• abnormal liver function
  
• chronic alcoholism, acute alcohol poisoning
  
• lactic acidosis (including history)
  
• for a period of at least 2 days before and after the radioisotope or radiological examinations with the introduction of iodine-containing contrast medium
  
• compliance with a hypocaloric diet (less than 1000 calories / day)
  
• pregnancy
  
• breast-feeding
  

Do not use the drug in patients older than 60 years, performing heavy physical work, which is associated with an increased risk of developing lactic acidosis.

Application of pregnancy and breastfeeding:

When planning a pregnancy, or in the event of pregnancy while taking metformin, the drug should be withdrawn and insulin.

For maternal and newborn installed surveillance. Since the data on the penetration into breast milk is not present, the drug is contraindicated in breastfeeding. If necessary, use Glucophage lactation breastfeeding should be discontinued.

Side effect:

The frequency of side effects of the drug is seen as follows: very common - & ge1 / 10 often - & ge1 / 100 <1/10, uncommon - & ge1 / 1000 <1/100, rare - & ge1 / 10,000 <1/1000, very rare - < 1/10 000, it is not known - can not be assessed with the data available.

Side effects are presented in decreasing order of importance.

Nervous system: often - taste disturbance.

Gastrointestinal disorders: very often - nausea, vomiting, diarrhea, abdominal pain, lack of appetite. Most often they occur in the initial period of treatment and in most cases subside spontaneously. To prevent symptoms of metformin is recommended to take 2 or 3 times a day during or after a meal. The slow increase in the dose may improve gastrointestinal tolerability.

Skin and subcutaneous tissue: Very rare - skin reactions such as erythema, pruritus, rash.

Metabolic disorders: very rarely - lactic acidosis (see "Special Instructions" section.).

Patients receiving long-term treatment with metformin, there was a decrease in vitamin B12 absorption, accompanied by a decrease in blood serum concentration. These effects are quickly reversible when canceling metformin and usually not clinically significant (<0.01%). Reduced levels of vitamin B12 must be taken into account in patients with megaloblastic anemia.

Hepatobiliary disorders: there are few reports about the violation of liver function tests or hepatitis after the abolition of metformin adverse events disappear completely.

Published data, post-marketing data, and controlled clinical trials limited to the pediatric population in the age group 10-16 years show that the side effects on the nature and severity are similar to those in adults.

Drug Interactions:

Not recommended combinations

Danazol: not recommended for concomitant use of danazol, given its hyperglycemic effect. If necessary, treatment with danazol and after discontinuation of the last dose of Glucophage required correction under the control of glucose levels.

Alcohol: alcohol intake increases the risk of lactic acidosis in acute alcohol intoxication, particularly against the background of fast and low-calorie diet, as well as liver failure. While receiving the drug should avoid alcohol and drugs containing ethanol.

Combinations requiring special care

Chlorpromazine: when taken in high doses (100mg / day) improves glycemia, reducing the release of insulin. When neuroleptic treatment and after discontinuation of the last dose of Glucophage required correction under the control of blood glucose levels.

SCS: the systemic and topical application of reduced glucose tolerance, increase glycemia, sometimes causing ketosis. In the treatment of corticosteroids and after you stop taking the last dose of Glucophage required correction under the control of blood glucose levels.

Diuretics: while taking loop diuretics may lead to the development of lactic acidosis due to possible functional renal failure. You should not assign Glucophage if Cl creatinine less than 60 mL / min.

Iodine-containing X-ray contrast agents: X-ray examination with the use of iodine-containing contrast media can induce the development of lactic acidosis in diabetic patients on the background of functional renal failure. Purpose Glucophage should be canceled for 48 hours before and 48 hours after study using X-ray contrast media.

Beta2-agonists: when administered parenterally increase glycaemia due to stimulation of beta2-adrenoceptor &. In this case, the need to control blood glucose. If necessary, it recommended the appointment of insulin.

It will be appreciated that ACE inhibitors and other antihypertensive drugs can reduce the blood glucose level. If necessary to adjust the dose of metformin.

With simultaneous use of Glucophage with sulfonylurea, insulin, acarbose, salicylates may increase hypoglycemic effect.

Dosage and administration:

Inside.

Adults - monotherapy and combination therapy in combination with other oral hypoglycemic agents

The usual starting dose is 500 mg 2-3 times a day during or after meals. Perhaps further gradual increase in the dose depending on the level of blood glucose.

The maintenance dose is usually 1500-2000 mg / day. To reduce the side effects from the gastrointestinal tract daily dose should be divided into 2-3 doses. The maximum dose is 3000 mg / day, divided into 3 doses.

The slow increase in the dose may improve gastrointestinal tolerability.

Patients taking metformin in doses of 2000-3000 mg / day may be transferred to receiving Glucophage 1000 mg. The maximum recommended dose of 3000 mg / day, divided into 3 doses.

In the case of transition planning with admission of other hypoglycemic agents to stop taking other means and to start taking the drug at a dose of Glucophage, above.

Adults - a combination with insulin

To achieve better blood glucose control with metformin and insulin may be administered as a combination therapy. The usual starting dose of the drug Glucophage 500 mg, and 850 of Table 1. 2-3 times a day, Glucophage 1000 mg - 1 tablet. 1 time per day, while the dose of insulin is selected based on the results of measurement of blood glucose.

Children and adolescents

Infants with the age of 10 can be used as Glucophage monotherapy, or in combination with insulin. The usual starting dose is 500 mg 2-3 times a day during or after meals. After 10-15 days, the dose should be adjusted based on the results of measurement of blood glucose. The maximum daily dose is 2,000 mg, divided into 2-3 doses.

Elderly patients

Due to a possible reduction in renal function, the dose of metformin should be selected under the control of the regular indicators of renal function (serum creatinine of at least 2-4 times a year).

Overdose:

Symptoms: metformin dose to 85 g of hypoglycaemia was observed. However, in this case, the observed development of lactic acidosis. Early symptoms of lactic acidosis include nausea, vomiting, diarrhea, fever, abdominal pain, pain in the muscles, in the future may be marked shortness of breath, dizziness, impaired consciousness and coma development.

Treatment: In the event of signs of lactic acidosis, treatment with Glucophage must be stopped immediately, the patient hospitalized immediately and determine the concentration of lactate, clarify the diagnosis. The most effective measure for the excretion of lactate and metformin is hemodialysis. Spend as symptomatic treatment.

Special instructions:

If during treatment, patients were vomiting, abdominal pain, muscle pain, weakness and severe malaise, you need to stop taking the drug and consult a doctor immediately. These symptoms may be a sign of incipient lactic acidosis.

For 48 hours before and 48 hours after the X-ray contrast studies (urography, intravenous angiography) should stop taking Glucophage.

Since metformin is excreted by the kidneys, before starting treatment and regularly thereafter, you must determine the level of serum creatinine.

Particular caution should be exercised in cases where renal function may fail, for example during the initial period of antihypertensive therapy, or therapy with diuretics, the initial and NSAID therapy.

The patient must inform the doctor about the appearance of bronchopulmonary infection or infectious disease urinary organs.

During treatment should refrain from drinking alcohol.

Effects on ability to drive and use machines

Glucophage monotherapy does not cause hypoglycaemia and therefore has no effect on ability to drive and use machines. However, patients should be treated with caution in a risk of hypoglycemia with metformin in combination with other hypoglycemic drugs (sulfonylureas, insulin, repaglinide, etc.).