Glucophage Long pills 1000mg, 30pcs

Composition

1 tablet contains

Active ingredient:

metformin hydrochloride-1000.0 mg;

Auxiliary substances:

carmellose sodium-50.0 mg,

hypromellose 2208-392.3 mg,

magnesium stearate-7.0 mg

Pharmacological action

Pharmacotherapeutic group hypoglycemic agent of the biguanide group for oral use. ATX code: A 10 BA 02 Pharmacological action Pharmacodynamics methformin is a hypoglycemic biguanide that reduces both basal and postprandial plasma 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 acting on glycogen synthase. Increases the transport capacity of all types of membrane glucose transporters. While taking 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, low-density lipoproteins and triglycerides. Pharmacokineticsabsorption The average time to reach the maximum concentration of metformin (1214 ng/ml) in blood plasma (TCmax) after a meal is 5 hours (in the interval of 4-10 hours) after a single oral use of 1 tablet of Glucophage® Long in the dosage form of a tablet with a prolonged release of 1000 mg. In an equilibrium state identical to that of metformin with normal release, the maximum concentration (Cmax) and area under the concentration-time curve (AUC) increase out of proportion to the dose taken. After a single oral dose of metformin in the form of extended-release tablets at a dose of 2000 mg, the AUC is similar to that observed after taking metformin in the form of tablets with a normal release at a dose of 1000 mg twice a day. Intra-individual variability in Cmax and AUC after taking metformin in the form of extended-release tablets is similar to that observed after taking metformin in the form of tablets with a normal release. When taking metformin in the form of 1000 mg long-release tablets after a meal, AUC increases by 77% (Cmax increases by 26% and TCmax increases by about 1 hour). The absorption of metformin from long-release tablets does not change depending on the composition of the food taken. No accumulation is observed with repeated use of metformin in the form of extended-release tablets at a dose of up to 2000 mg. Distribution The association with plasma proteins is insignificant. Cmax in blood is lower than Cmax in plasma, and is reached after approximately the same time. The average volume of distribution (Vd) varies in the range of 63-276 liters. Metabolism Metabolites were not detected in humans. Elimination 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. After oral use, the elimination half-life is about 6.5 hours. With impaired renal function, metformin clearance decreases in proportion to creatinine clearance, and the elimination half-life increases, which can lead to an increase in the concentration of metformin in plasma.

Indications

Type 2 diabetes mellitus in adults, especially in obese patients, when diet therapy and exercise are ineffective:

• as monotherapy;

• in combination with other oral hypoglycemic agents or with insulin.

Use during pregnancy and lactation

When planning pregnancy, as well as in the case of pregnancy while taking Glucophage® Long, the drug should be discontinued, and insulin therapy should be prescribed. The patient should inform the doctor about the onset of pregnancy while taking Glucophage® Long. Since there are no data on the penetration of metformin into breast milk, this drug is contraindicated during breastfeeding. If it is necessary to use the drug Glucophage® Long prolonged action during lactation, breastfeeding should be discontinued.

Contraindications

• Hypersensitivity to metformin or any excipient.
• Diabetic ketoacidosis, diabetic precoma, coma.
• Renal insufficiency or impaired renal function (creatinine clearance less than 45 ml / min).
• Acute conditions with a risk of developing impaired renal function: dehydration (with chronic or severe diarrhea, repeated attacks of vomiting), severe infectious diseases (for example, respiratory tract infections, urinary tract infections), shock.
• Clinically expressed manifestations of acute or chronic diseases that can lead to the development of tissue hypoxia (including acute heart failure, chronic heart failure with unstable hemodynamic parameters, respiratory failure, acute myocardial infarction).
• Extensive surgical operations and injuries, when insulin therapy is indicated (see the section “Special instructions”).
• Hepatic insufficiency, impaired liver function.
• Chronic alcoholism, acute alcohol poisoning.
• Pregnancy.
• Lactic acidosis (including a history of lactic acidosis).
• Use for less than 48 hours before and 48 hours after radioisotope or X-ray studies with the introduction of an iodine-containing contrast agent (for example, intravenous urography, angiography) (see the section “Interaction with other drugs”);
• Compliance with a hypocaloric diet (less than 1000 kcal / day).
• Children under 18 years of age due to the lack of data on the use.

Use the drug with caution:

• in patients over 60 years of age who perform heavy physical work, which is associated with an increased risk of lactic acidosis;
• in patients with renal insufficiency (creatinine clearance 45-59 ml / min)
• during breastfeeding.

Side effects

The frequency of side effects of the drug is estimated as follows: Very frequent: ≥ 1/10 Frequent: ≥ 1/100, < 1/10 Infrequent: ≥ 1/1000, Rare: ≥ 1/10 000, Very rare: < 1/10 000 Metabolic and nutritional disorders: Very rare: lactic acidosis (see “Special instructions”). With prolonged use of metformin, there may be a decrease in the absorption of vitamin B12. If megaloblastic anemia is detected, it is necessary to consider the possibility of such an etiology. Nervous system disorders: Common: taste disorder (metallic taste in the mouth). Disorders of the gastrointestinal tract:  Very common: nausea, vomiting, diarrhea, abdominal pain, and 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 during or after a meal. Slowly increasing the dose may improve gastrointestinal tolerance. Liver and biliary tract disorders: Very rare: impaired liver function and hepatitis; after discontinuation of metformin, these adverse events completely disappear. Skin and subcutaneous tissue disorders: Very rare: skin reactions such as erythema (redness of the skin), pruritus, urticaria. If any of the side effects listed in the instructions get worse, or other side effects that are not listed in the instructions are noticed, you should inform your doctor.

Interaction

Contraindicated combinations

of iodine-containing radiopaque agents: against the background of functional renal failure in patients with diabetes mellitus, radiological examination with the use of iodine-containing radiopaque agents may cause the development of lactic acidosis. Treatment with Glucophage®Long-term therapy should be discontinued depending on renal function 48 hours before or during the X-ray examination with the use of iodine-containing radiopaque drugs and renewed no earlier than 48 hours after, provided that the renal function was found to be normal after the examination.

Not recommended combinations

Alcohol: acute alcohol intoxication increases the risk of developing lactic acidosis, especially if:

• insufficient nutrition, compliance with a low-calorie diet•

* liver failure.

While taking the drug, you should avoid taking alcohol and drugs containing ethanol.

Combinations that require caution

Medications with indirect hyperglycemic effects (for example, glucocorticosteroids (corticosteroids) and tetracosactide (systemic and local action), beta_-2-adrenomimetics, danazol, chlorpromazine in large doses (100 mg per day) and diuretics): more frequent monitoring of blood glucose levels may be required, especially at the beginning of treatment. If necessary, the dose of the drug Glucophage® Long can be adjusted during treatment and after its termination, based on the level of glycemia.

Diuretics: concomitant use of loop diuretics may lead to lactic acidosis due to possible functional renal failure.

With simultaneous use of the drug Glucophage® Long with sulfonylurea derivatives, insulin, acarbose, salicylates, hypoglycemia may develop.

Nifedipine increases the absorption and_cmaxof 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 may increase its_cmax.

Colesevelam, when used concomitantly with metformin in the form of extended-release tablets, increases the concentration of metformin in blood plasma (an increase in AUC without a significant increase in_cmax).

How to take, course of use and dosage

Glucophage® Long 1000 mg is taken orally. Tablets are swallowed whole, without chewing, with a sufficient amount of liquid,1 time a day during or after dinner. The dose of Glucophage® Long 1000 mg is selected by the doctor individually for each patient based on the results of measuring the concentration of glucose in the blood. Monotherapy and combination therapy in combination with other hypoglycemic agents

• Glucophage® Long 1000 mg should be taken once a day during or after dinner.
• Glucophage® Long 1000 mg is prescribed as maintenance therapy for patients taking metformin in the form of tablets with a normal release at a dose of 1000 mg or 2000 mg. To switch to Glucophage® Long 1000 mg, the daily dose should be equivalent to the daily dose of metformin with a normal release.
• Switching to Glucophage® Long 1000 mg is not recommended for patients taking metformin in the usual release tablet form at a dose exceeding 2000 mg.
• For patients who do not take metformin, the recommended starting dose of Glucophage® Long is 500 mg or 750 mg once daily with dinner (the following forms of release of Glucophage® Long are available: 500 mg and 750 mg long-release tablets). Every 10-15 days, it is recommended to adjust the dose based on the results of measuring the concentration of glucose in the blood. A slow increase in the dose contributes to better tolerability on the part of the gastrointestinal tract.
• In case of switching from another hypoglycemic agent, the dose selection is carried out as described above, starting with the appointment of the drug Glucophage® Long 500 mg or 750 mg, with a possible subsequent transition to the drug Glucophage® Long 1000 mg.

Combination with insulin To achieve better glycemic control, metformin and insulin can be used as a combination therapy. The usual starting dose of Glucophage® Long is one tablet of 500 mg or 750 mg once a day with dinner, while the insulin dose is selected based on the results of measuring the concentration of glucose in the blood. Then you can switch to Glucophage® Long 1000 mg. The maximum recommended dose of Glucophage® Long 1000 mg is 2 tablets per day (2000 mg). If taking the maximum recommended dose once a day does not achieve adequate glycemic control, the maximum dose can be divided into two doses: one 1000 mg tablet at breakfast and one 1000 mg tablet at dinner. If adequate glycaemic control is not achieved in this case, it is possible to switch to metformin with a normal release (for example, Glucophage®, film-coated tablets) with a maximum daily dose of 3000 mg. Patients with renal insufficiency Metformin can be used in patients with moderate renal insufficiency (creatinine clearance 45-59 ml/min) only in the absence of conditions that may increase the risk of lactic acidosis. The initial dose is 500 mg or 750 mg once a day. The maximum dose is 1000 mg per day. Renal function should be carefully monitored every 3-6 months. If the creatinine clearance is below 45 ml / min, the drug should be discontinued immediately. Elderly patients: In elderly patients, the metformin dose is adjusted based on a regular assessment of renal function (see “Special Instructions”). Duration of treatment: Glucophage® Long should be taken daily, without interruption. If treatment is discontinued, the patient should inform the doctor. Skipping a dose If you miss the next dose, the patient should take the next dose at the usual time. Do not take a double dose of Glucophage® Long.

Overdose

Hypoglycemia was not observed when metformin was administered at a dose of 85 g (42.5 times the maximum daily dose). However, in this case, the development of lactic acidosis was observed. Significant overdose or associated risk factors may lead to lactic acidosis (see “Special instructions”). 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 a rare but serious complication (high mortality in the absence of urgent treatment) that can occur due to accumulation of metformin. Cases of lactic acidosis during metformin use occurred mainly in patients with diabetes mellitus with severe renal insufficiency. Other associated risk factors should also be considered, such as decompensated diabetes mellitus, ketosis, prolonged fasting, alcoholism, 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 dyspeptic disorders, abdominal pain and severe asthenia. Lactic acidosis is characterized by severe malaise with general weakness, acidotic dyspnea, vomiting, abdominal pain, muscle cramps, and hypothermia followed by coma. Diagnostic laboratory indicators are a decrease in blood pH (less than 7.25), a concentration of lactate in blood plasma over 5 mmol / l, an increased anion gap and the ratio of lactate/pyruvate. If lactic acidosis is suspected, stop taking the drug and immediately consult a doctor. Surgical operationsapplication of metformin should be discontinued 48 hours prior to elective surgery and may be continued no earlier than 48 hours after, provided that renal function was found to be normal during the examination. Renal function Since metformin is excreted by the kidneys, creatinine clearance should be determined before starting treatment and regularly thereafter: 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 nonsteroidal anti-inflammatory drugs. Heart Failure Patients with heart failure have a higher risk of developing hypoxia and kidney failure. Patients with chronic heart failure should be regularly monitored for cardiac and renal function while taking metformin. Metformin is contraindicated in patients with acute heart failure and chronic heart failure with unstable hemodynamic parameters. 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 the doctor about any ongoing treatment and any infectious diseases, such as colds, respiratory tract infections, or urinary tract infections.
• It is recommended to regularly perform standard laboratory tests 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, etc. ). 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.

Effects on the ability to drive vehicles and mechanicsmi Monotherapy with Glucophage® Long does not cause hypoglycemia, so it does not affect the ability to drive vehicles and mechanisms. However, hypoglycemia may occur when metformin is used in combination with other hypoglycemic drugs (sulfonylureas, insulin, repaglinide, etc. ). If symptoms of hypoglycemia occur, do not drive vehicles and mechanisms.

Form of production

Long-acting tablets are white or almost white in color, capsule-shaped, biconvex, with the inscription “1000” on one side and “Megsk” on the other.

Storage conditions

Store at a temperature not exceeding 30 °C. Keep out of reach of children.

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