Glucophage Long pills 750mg, 60pcs

Composition

of 1 tab. metformin hydrochloride 750 mg

Auxiliary substances:

carmellose sodium – 37.5 mg,

hypromellose 2208-294.24 mg,

magnesium stearate-5.3 mg

Pharmacological action

An oral hypoglycemic drug from the biguanide group that reduces both basal and postprandial blood glucose levels. It does not stimulate insulin secretion and therefore does not cause hypoglycemia. Increases the sensitivity of peripheral insulin receptors and the utilization of glucose by cells. Reduces liver glucose production by inhibiting gluconeogenesis and glycogenolysis. Delays the absorption of glucose in the intestines.

Metformin stimulates glycogen synthesis by affecting glycogen synthetase. Increases the transport capacity of all types of membrane glucose transporters.

With metformin, the patient’s body weight either remains stable or decreases moderately.

Metformin has a beneficial effect on lipid metabolism: it reduces the content of total cholesterol, LDL and triglycerides.

Pharmacokinetics

Suction

After oral use of the drug in the form of a long-acting tablet, the absorption of metformin is slowed down compared to a tablet with a normal release of metformin. The time to reach the Cmax of metformin when taking Glucophage® Long-acting tablets is 7 hours. At the same time, the Tmax for a normal-release tablet is 2.5 hours.

At steady state, identical to the Css of metformin in tablet form with the usual release profile, Cmax and AUC increase out of proportion to the dose. After a single oral dose of 2000 mg of metformin in the form of long-acting tablets, the AUC is similar to that observed after taking 1000 mg of metformin in the form of tablets with a normal release 2 times/day.

Fluctuations in Cmax and AUC in individual patients when taking metformin in the form of long-acting tablets are similar to the same indicators as when taking tablets with a normal release profile.

The absorption of metformin from long-acting tablets does not change depending on food intake.

Distribution

Binding to plasma proteins is insignificant. Cmax in blood is lower than Cmax in plasma and is reached after approximately the same time. The average Vd ranges from 63-276 liters.

No accumulation is observed with repeated use of up to 2000 mg of metformin in the form of long-acting tablets.

Metabolism

No metabolites were detected in humans.

Deduction

After oral use, T1/2 is about 6.5 hours. Metformin is excreted unchanged by the kidneys. Renal clearance of metformin is >400 ml / min, which indicates that metformin is eliminated by glomerular filtration and tubular secretion.

Pharmacokinetics in special clinical cases

With impaired renal function, metformin clearance decreases in proportion to creatinine clearance, and T1/2 increases, which can lead to an increase in the concentration of metformin in plasma.

Indications

Type 2 diabetes mellitus in adults with ineffective diet therapy and physical activity (especially in obese patients):

• as monotherapy;
• in combination with other oral hypoglycemic drugs, or in combination with insulin.

Use during pregnancy and lactation

Use during pregnancy and lactation

Decompensated diabetes mellitus during pregnancy is associated with an increased risk of birth defects and perinatal mortality.

A limited amount of evidence suggests that the use of metformin in pregnant women does not increase the risk of developing birth defects in children.

When planning pregnancy, as well as in the case of pregnancy with the use of metformin, the drug should be discontinued and insulin therapy should be prescribed. It is necessary to maintain the concentration of glucose in the blood at the level closest to normal to reduce the risk of fetal malformations.

Metformin is excreted in breast milk. No side effects were observed in newborns who were breastfed while taking metformin. However, due to the limited amount of data, the use of the drug during lactation is not recommended. The decision to stop breast-feeding should be made taking into account the benefits of breastfeeding and the potential risk of side effects in the child.

Use in children

It is contraindicated in children and adolescents under 18 years of age due to the lack of data on use.

Contraindications

• diabetic ketoacidosis, diabetic precoma, coma;
• renal failure or impaired renal function (CC
• acute conditions occurring with the risk of developing renal dysfunction, including dehydration (chronic or severe diarrhea, repeated vomiting), severe infections (e. g., infections of respiratory and urinary tract), shock;
• symptomatic manifestations of acute and chronic diseases, which can lead to the development of tissue hypoxia (including cardiac or respiratory failure, acute myocardial infarction);
• extensive surgery and trauma, when shown holding insulin;
• hepatic failure, hepatic impairment;
• chronic alcoholism, acute alcohol poisoning;
• lactic acidosis (including history);
• application of at least 48 hours prior to and within 48 hours after the radioisotope or radiological examinations with use of iodinated contrast agents;
• adherence to a reduced-calorie diet (less than 1000 kcal/day);
• pregnancy;
• children’s and teenage age up to 18 years due to a lack of data on the application;
• hypersensitivity to the components of the drug.

With caution, the drug should be used in patients over the age of 60 years, performing heavy physical work, which is associated with an increased risk of developing lactic acidosis; during lactation (breastfeeding).

Side effects

Determination of the frequency of side effects: very common (≥1/10), common (≥1/100,

From the nervous system: often-a violation of taste (metallic taste in the mouth).

From the digestive system: very often – nausea, vomiting, diarrhea, abdominal pain, lack of appetite. Most often, they occur during the initial period of treatment and in most cases pass spontaneously. To prevent symptoms, it is recommended to take metformin with a meal. Slowly increasing the dose may improve gastrointestinal tolerance.

From the side of the hepatobiliary system: very rarely – impaired liver function or hepatitis; after discontinuation of metformin, adverse events completely disappear.

From the skin: very rarely – erythema, pruritus, urticaria.

From the side of metabolism: very rarely – lactic acidosis. Prolonged use of metformin may reduce the absorption of vitamin B12. If megaloblastic anemia is detected, it is necessary to consider the possibility of such an etiology.

If any of the side effects indicated in the instructions are aggravated, or other side effects are noted that are not specified in the instructions, the patient should inform the doctor about this.

Interaction

Contraindicated combinations

Against the background of functional renal failure in patients with diabetes mellitus, radiological examination with the use of iodine-containing radiopaque agents can cause the development of lactic acidosis. Glucophage® Long should be discontinued 48 hours before and not resumed earlier than 48 hours after X-ray examination using iodine-containing radiopaque agents, provided that renal function was found to be normal during the examination.

Not recommended combinations

Taking ethanol increases the risk of lactic acidosis during acute alcohol intoxication, especially in cases of malnutrition, low-calorie diet, and liver failure. Medications containing ethanol should not be used during treatment.

Combinations that require caution

Medications with indirect hyperglycemic effects (for example, corticosteroids and tetracosactide for systemic and topical use), beta-2-adrenomimetics, danazol, chlorpromazine at high doses (100 mg / day) and diuretics: more frequent monitoring of blood glucose concentration may be required, especially at the beginning of treatment. If necessary, the dose of Glucophage® Long can be adjusted during treatment and after its termination, based on the level of glycemia.

Concomitant use of loop diuretics may lead to lactic acidosis due to possible functional renal failure. Glucophage® Long should not be prescribed if the creatinine clearance is less than 60 ml / min.

Antihypertensive drugs of the ACE inhibitor class can reduce the concentration of glucose in the blood. If necessary, the metformin dose should be adjusted.

Concomitant use of Glucophage® Long with sulfonylurea derivatives, insulin, acarbose, and salicylates may lead to hypoglycemia.

Nifedipine increases the absorption and Cmax of metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, and vancomycin) secreted in the renal tubules compete with metformin for tubular transport systems and can lead to an increase in its Cmax.

How to take it, course of use and dosage

The drug is taken orally 1 time/day, during dinner. Tablets are swallowed whole, without chewing, with a sufficient amount of liquid.

The dose of Glucophage® Long should be selected individually for each patient based on the results of measuring the concentration of glucose in the blood.

Glucophage® Long should be taken daily, without interruption. In case of discontinuation of treatment, the patient should inform the doctor about this.

If the next dose is missed, the next dose should be taken at the usual time. Do not double the dose of Glucophage® Long.

Overdose

Symptoms: when using metformin at a dose of 85 g (42.5 times the maximum daily dose), the development of hypoglycemia was not observed, but in this case the development of lactic acidosis was observed. Significant overdose or associated risk factors can lead to lactic acidosis.

Treatment: if signs of lactic acidosis appear, treatment with the drug should be stopped immediately, the patient should be urgently hospitalized and, after determining the lactate concentration, the diagnosis should be clarified. The most effective measure for removing lactate and metformin from the body is hemodialysis. Symptomatic treatment is also performed.

Special instructions

Lactic acidosis

Lactic acidosis is an extremely rare but serious complication (high mortality in the absence of urgent treatment) that can occur due to the accumulation of metformin. Cases of lactic acidosis in patients treated with metformin occurred mainly in diabetic patients with severe renal insufficiency.

Other associated risk factors should also be considered, such as poorly controlled diabetes, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, and any condition associated with severe hypoxia. This can help reduce the incidence of lactic acidosis.

The risk of developing lactic acidosis should be considered if there are non-specific signs such as muscle cramps accompanied by dyspepsia, abdominal pain, general weakness and severe malaise.

Lactic acidosis is characterized by acidotic dyspnea, vomiting, abdominal pain, muscle cramps, and hypothermia followed by coma. Diagnostic laboratory indicators are a decrease in blood pH (5 mmol / l, increased anion gap and the ratio of lactate/pyruvate. If lactic acidosis is suspected, stop taking the drug and immediately consult a doctor.

Surgical operations

The use of metformin should be discontinued 48 hours before elective surgery and may be continued no earlier than 48 hours after, provided that renal function was found to be normal during the examination.

Kidney function

Since metformin is excreted by the kidneys, before starting treatment, and regularly thereafter, it is necessary to determine the creatinine clearance: at least once a year in patients with normal renal function, and 2-4 times a year in elderly patients, as well as in patients with creatinine clearance at the lower limit of normal.

Special care should be taken in the event of possible renal impairment in elderly patients, with the simultaneous use of antihypertensive drugs, diuretics or NSAIDs.

Other safety measures

Patients are advised to continue to follow a diet with a uniform intake of carbohydrates throughout the day.

Overweight patients are recommended to continue to follow a hypocaloric diet (but not less than 1000 kcal / day). Patients should also exercise regularly.

Patients should inform their doctor about any ongoing treatment and any infectious diseases, such as respiratory and urinary tract infections.

Routine laboratory tests should be performed regularly to control diabetes mellitus.

Metformin alone does not cause hypoglycemia, but caution is recommended when used in combination with insulin or other oral hypoglycemic agents (for example, sulfonylureas or repaglinide). Symptoms of hypoglycemia include weakness, headache, dizziness, increased sweating, rapid heartbeat, visual impairment, or impaired concentration.

It is necessary to warn the patient that inactive components of the drug Glucophage® Long may be excreted unchanged through the intestine, which does not affect the therapeutic activity of the drug.

Influence on the ability to drive motor vehicles and manage mechanisms

Monotherapy with Glucophage® Long does not cause hypoglycemia, and therefore does not affect the ability to drive a car and work with mechanisms.

However, patients should be warned about the risk of hypoglycemia when using metformin in combination with other hypoglycemic drugs (sulfonylureas, insulin, repaglinide).

Form of production

Glucophage Long tablets.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Metformin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Type 2 Diabetes