Glucofage long 1000mg tbl prolong deist N60

Prescription drug

Manufacturer: Мерк
Рецептурный препарат
глюкофаж лонг 1000мг тбл пролонг дейст n60
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Brief information

Производитель

Мерк

Действующее вещество

Метформин

The appearance of the product may differ from the photos on the site.

General description
Источник:  РЛС

Composition

Long-acting tablets1 table.
active substance: 
Metformin hydrochloride500 mg
excipients: sodium carmellose-50 mg; hypromellose 2910-10 mg; hypromellose 2208-358 mg; MCC-102 mg; magnesium stearate-3.5 mg 
Long-acting tablets1 table.
active substance: 
Metformin hydrochloride750 mg
excipients: sodium carmellose-37.5 mg; hypromellose 2208-294.24 mg; magnesium stearate-5.3 mg 
Long-acting tablets1 table.
active substance: 
Metformin hydrochloride1 g
composition component without quantity 
excipients: sodium carmellose-50 mg; hypromellose 2208-392.3 mg; magnesium stearate-7 mg 

Description of the dosage form

500 mg tablets: capsule-shaped biconvex tablets, white or almost white, with 500 engraved on one side.

750 mg tablets: capsule-shaped biconvex tablets, white or almost white, with 750 engraved on one side and MERCK on the other.

1000 mg tablets: capsule-shaped biconvex tablets of white or almost white color, with 1000 engraving on one side and MERCK on the other.

Pharmacokinetics

Suction

The average T max of Metformin (1214 ng / ml) in blood plasma after a meal is 5 h (in the interval of 4-10 h) after a single oral administration 1 table. the drug Glucofage long in the dosage form of a long-acting tablet, 1000 mg.

500 mg. after oral administration of the drug in the form of a long-acting tablet, the absorption of Metformin is slowed down compared to a tablet with normal Metformin release. The time to reach the maximum concentration (TCmax) is 7 hours. at the same time, TCmax for a tablet with normal release is 2.5 hours.

750 mg. Average time of maximum concentration of Metformin (1193 ng/ml) in plasma after a meal is 5 hours (in between 4-12 hours) after oral intake of 1500 mg Glucophage long in the form of tablets prolonged action, 750 mg.

1000 mg. the Average time to reach the maximum concentration of Metformin (1214 ng / ml) in blood plasma (Tsmach) after a meal is 5 h (in the interval of 4-10 h) after a single oral administration 1 table. the drug Glucofage long in the dosage form of a long-acting tablet 1000 mg.

In an equilibrium state identical to that of Metformin with normal release, C max and AUC increase disproportionately to the dose taken. After a single oral administration 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 normal release 2 times a day.

Intraindividual variability of C max and AUC after taking Metformin in the form of long-acting tablets is similar to that observed after taking Metformin in the form of tablets with normal release.

When taking Metformin in the form of long-acting tablets at a dose of 1000 mg after a meal, the AUC increases by 77% (C max increases by 26% and T max increases by about 1 h).

The absorption of Metformin from long-acting tablets does not change depending on the composition of the food taken. There is no accumulation with repeated administration of up to 2000 mg of Metformin in the form of long-acting tablets at a dose of up to 2000 mg.

Distribution

The Association with plasma proteins is insignificant. The C max in blood is lower than the C max in plasma, and is reached after about the same time. The average V d ranges from 63-276 l.

Metabolism

No metabolites were found in humans.

Breeding

Metformin is excreted unchanged by the kidneys. The renal clearance of Metformin is >400 ml / min, indicating that Metformin is excreted by CF and tubular secretion. After oral administration of T 1/2-about 6.5 hours.

With impaired renal function, Metformin clearance decreases proportionally to creatinine Cl, and T 1/2 increases, which can lead to an increase in the plasma concentration of Metformin.

Pharmacodynamics

Metformin — biguanide with hypoglycemic effect, lowering both basal and postprandial concentration of glucose in the blood plasma. It does not stimulate insulin secretion and therefore does not cause hypoglycemia. Increases the sensitivity of peripheral receptors to insulin and utilization of glucose by cells. Reduces the production of glucose by the liver by inhibiting gluconeogenesis and glycogenolysis. Delays the absorption of glucose in the intestine.

Metformin stimulates glycogen synthesis by acting on glycogen synthase. Increases the transport capacity of all types of membrane glucose carriers.

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, LDL and triglycerides.

Indications of the drug

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

- as monotherapy;

- in combination with other oral hypoglycemic agents or insulin.

Contraindications

hypersensitivity to Metformin or to any auxiliary substance;

diabetic ketoacidosis, diabetic precoma, coma;

renal failure or impaired renal function (CL creatinine <45 ml / min);

acute conditions that occur with the risk of developing kidney function disorders: dehydration (with chronic or severe diarrhea, multiple vomiting attacks), severe infectious diseases (such as 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 Special instructions);

liver failure, impaired liver function;

chronic alcoholism, acute alcohol poisoning;

pregnancy;

lactic acidosis (including history);

use for less than 48 hours before and for 48 hours after radioisotope or x-ray studies with the introduction of an iodine-containing contrast agent (for example, in / in urography, angiography) (see Interaction);

compliance with a hypocaloric diet (<1000 cal/day);

children under 18 years of age, due to the lack of data on the application.

Caution: patients older than 60 years who perform heavy physical work, which is associated with an increased risk of developing lactoacidosis, patients with renal insufficiency (creatinine Cl 45-59 ml/min), breast-feeding period.

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 data suggests that taking Metformin in pregnant women does not increase the risk of developing birth defects in children.

When planning a pregnancy, as well as in the case of pregnancy on the background of Metformin, the drug should be canceled and insulin therapy should be prescribed.

It is necessary to maintain the concentration of glucose in the blood plasma 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 infants 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 breastfeeding should be made taking into account the benefits of breastfeeding and the potential risk of side effects in the child.

Dosage and administration

Inside. Tablets are swallowed whole, without chewing, with a small amount of liquid, 1 time a day during dinner. The dose of the drug Glucofage long in the form of long-acting tablets 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.

For patients who do not take Metformin, the recommended starting dose of Glucofage long is 500, 750 or 1000 mg once a day during dinner.

500 mg. depending on the concentration of glucose in the blood plasma, a slow increase in the dose (by 500 mg) is possible every 10-15 days, until the maximum daily dose is reached (2000 mg). A slow increase in the dose helps reduce the side effects of the gastrointestinal tract.

750 mg. the Recommended dose of the drug Glucofage long is 2 table. 750 mg once a day. If the recommended dose does not achieve adequate control of glycemia, it is possible to increase the dose to the maximum — 3 table. 750 mg of the drug Glucofage long 1 time a day.

1000 mg. the drug Glucofage long 1000 mg is prescribed as a maintenance therapy for patients taking Metformin in the form of tablets with normal release at a dose of 1000 or 2000 mg.

500, 750, and 1000 mg. For patients already receiving Metformin treatment, the initial dose of Glucofage long should be equivalent to the daily dose of regular-release tablets.

Patients taking Metformin in the form of tablets with the usual release of the active ingredient at a dose exceeding 2000 mg are not recommended to switch to long Glucophage.

For patients who do not take Metformin, the recommended starting dose of Glucofage long is 500 mg or 750 mg once a day during dinner (the following release forms of Glucofage long are available: 500 mg and 750 mg long-acting 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.

In the case of switching from another hypoglycemic agent, the dose selection is carried out as described above, starting with the appointment of the drug Glucofage long 500 or 750 mg, with a possible subsequent transition to the drug Glucofage long 1000 mg.

Combination with insulin. To achieve better control of blood glucose, Metformin and insulin can be used as a combination therapy. The usual initial dose of the drug Glucofage long is 1 table. 500 or 750 mg once a day during dinner, while the insulin dose is selected based on the results of measuring the concentration of glucose in the blood. Next, you can switch to the drug Glucofage long 1000 mg.

Daily dose. The maximum recommended dose of the drug Glucofage long — 4 table. 500 mg (2000 mg/day), 3 table. 750 mg per day (2250 mg) or 2 tables. 1000 mg per day (2000 mg). If taking the maximum recommended dose 1 time a day during dinner fails to achieve adequate glycemic control, then the maximum dose can be divided into two doses: 2 table. 500 mg or 1 table. 1000 mg — during Breakfast and 2 tables. 500 mg or 1 table. 1000 mg — during dinner.

If adequate glycemic control is not achieved when taking 2000 mg of the drug Glucofage long, long-acting tablets, it is possible to switch to Metformin with the usual release of the active ingredient (for example, Glucofage, film-coated tablets) with a maximum daily dose of 3000 mg.

Patients with kidney failure. Metformin can be used in patients with moderate renal insufficiency (creatinine Cl 45-59 ml / min) only in the absence of conditions that may increase the risk of lactic acidosis. The initial dose is 500 or 750 mg once a day. The maximum dose is 1000 mg/day. Kidney function should be carefully monitored every 3-6 months.

If the creatinine Cl is below 45 ml / min, the drug should be stopped immediately.

Patients of advanced age. Due to a possible decrease in kidney function, the Metformin dose is adjusted based on an assessment of kidney function, which should be performed regularly, at least 2 times a year.

Duration of treatment. Glucofage long should be taken daily, without interruption. If treatment is discontinued, the patient must inform the doctor.

Skipping a dose. If you skip the next dose, the patient should take the next dose at the usual time. Do not take a double dose of Glucofage long.

Side effect

The frequency of side effects of the drug is estimated as follows: very often (≥1/10); often (≥ 1/100, <1/10); infrequently (≥1/1000, <1/100); rarely (≥1/10000, <1/1000); very rare (<1/10000).

From the metabolic: very rarely — lactic acidosis (see Special instructions).

With long-term use of Metformin, there may be a decrease in the absorption of vitamin B 12 . When detecting megaloblastic anemia, it is necessary to consider the possibility of such an etiology.

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

From the digestive tract: very often — nausea, vomiting, diarrhea, abdominal pain and lack of appetite. Most often they occur in the initial period of treatment and in most cases spontaneously pass. To prevent symptoms, it is recommended to take Metformin during or after a meal. A slow increase in the dose may improve gastrointestinal tolerance.

On the part of the liver and biliary tract: very rarely — violation of liver function indicators and hepatitis; after the cancellation of Metformin, undesirable phenomena completely disappear.

From the skin and subcutaneous tissues: very rarely — skin reactions such as erythema (redness of the skin), itching, hives.

If any of the side effects listed in the description have worsened or there are other side effects not listed in the description, you must inform your doctor.

Interaction

Contraindicated in combination

Iodine-containing radiopaque agents: against the background of functional renal failure in patients with diabetes mellitus, radiological research using iodine-containing radiopaque agents can cause the development of lactoacidosis. Treatment with Glucofage long should be canceled, depending on kidney function, 48 hours before or during x-ray examination using iodine-containing radiopaque agents and resumed no earlier than 48 hours after, provided that during the examination, renal function was recognized as normal.

Recommended combinations

Alcohol. With acute alcohol intoxication, the risk of developing lactoacidosis increases, especially in the case of insufficient nutrition, compliance with a low-calorie diet, and liver failure.

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

Combinations that require caution

Drugs with indirect hyperglycemic action (for example, GCS and tetracosactide (systemic and local action), β 2-adrenomimetics, danazol, chlorpromazine when taken in high doses (100 mg per day) and diuretics: more frequent monitoring of blood glucose concentration may be required, especially at the beginning of treatment. If necessary, the dose of the drug Glucofage long can be adjusted during treatment and after its termination, based on the level of glycemia.

Diuretics: concurrent administration with loop diuretics may lead to the development of lactic acidosis due to possible renal failure.

With simultaneous use of the drug Glucofage long with sulfonylurea derivatives, insulin, acarbose, salicylates, hypoglycemia may develop.

Nifedipine increases the absorption and C max 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 C max .

Kolesevelam when used simultaneously with Metformin in the form of long-acting tablets increases the concentration of Metformin in the blood plasma (increase in AUC without a significant increase in C max).

Overdose

When Metformin was administered at a dose of up to 85 g (42.5 times the maximum daily dose), hypoglycemia was not observed. However, in this case observed the development of lactic acidosis. Significant overdose or associated risk factors may lead to lactic acidosis (see Special instructions).

Treatment: if signs of lactoacidosis appear, treatment with the drug should be stopped immediately, the patient should be urgently hospitalized and, having determined the concentration of lactate, clarify the diagnosis. The most effective measure for removing lactate and Metformin from the body is hemodialysis. Symptomatic treatment is also performed.

Special instruction

Lactic acidosis

Lactoacidosis is a rare but serious (high mortality in the absence of emergency treatment) complication that can occur due to Metformin accumulation. Cases of lactic acidosis when taking Metformin occurred mainly in patients with diabetes mellitus and 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 to reduce the frequency of occurrence of lactic acidosis.

The risk of developing lactoacidosis should be taken into account when non-specific signs appear, such as muscle cramps accompanied by dyspeptic disorders, abdominal pain and severe asthenia.

Lactoacidosis is characterized by severe malaise with General weakness, acidotic shortness of breath and vomiting, abdominal pain, muscle cramps and hypothermia followed by coma. Diagnostic laboratory indicators are a decrease in blood pH (less than 7.25), the concentration of lactate in blood plasma over 5 mmol / l, increased anion gap and the ratio of lactate/pyruvate. If you suspect lactic acidosis, stop taking the drug and immediately consult a doctor.

Surgery

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

Kidney function

Since Metformin is excreted by the kidneys, it is necessary to determine the serum content of creatinine and/or Cl in the serum at least once a year in patients with normal kidney function and 2-4 times a year in elderly patients, as well as in patients with creatinine Cl on NGN.

In the case of CL creatinine less than 45 ml / min, the use of the drug is contraindicated.

Special care should be taken when possible renal dysfunction in elderly patients, while using antihypertensive drugs, diuretics or NSAIDs.

Heart failure

Patients with heart failure have a higher risk of hypoxia and kidney failure. Patients with CHF should regularly monitor heart and kidney function while taking Metformin. Metformin is contraindicated in acute heart failure and CHF with unstable hemodynamic parameters.

Other precautions

Patients are advised to continue to follow a diet with an even intake of carbohydrates throughout the day. Patients who are overweight 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 treatment being performed and any infectious diseases such as colds, respiratory tract infections, or urinary tract infections.

It is recommended to regularly conduct standard laboratory tests to control diabetes.

Metformin does not cause hypoglycemia in monotherapy, but caution is recommended when using it in combination with insulin or other oral hypoglycemic agents (for example, sulfonylurea derivatives or Repaglinide). Symptoms of hypoglycemia include weakness, headache, dizziness, increased sweating, rapid heartbeat, impaired vision, or impaired concentration. It is necessary to warn the patient that inactive components of the drug Glucofage long can be released unchanged through the intestine, which does not affect the therapeutic activity of the drug.

Influence on the ability to drive vehicles and mechanisms. Monotherapy with Glucofage long does not cause hypoglycemia, so it does not affect the ability to drive vehicles and mechanisms.

However, hypoglycemia may develop when Metformin is used in combination with other hypoglycemic drugs (including sulfonylurea derivatives, insulin, and Repaglinide). If you experience symptoms of hypoglycemia, do not drive vehicles or machinery.

Form release

Tablets of prolonged action, 500 mg, 750 mg.15 table. in a blister made of PVC/pvdh and aluminum foil, 2 or 4 blisters in a pack of cardboard. The m symbol is applied to the blister and the cardboard package to protect it from falsification.

Extended-release tablets, 1000 mg. For 7 table. in a blister of PVC / pvdh / aluminum foil, 4 or 8 BL. placed in a cardboard box.

10 table. in a blister of PVC/PVDC/aluminium foil, for 3 or 6 BL. placed in a cardboard box.

The m symbol is applied to the blister and the cardboard package to protect it from falsification.

Conditions of supply of pharmacies

By prescription.

Manufacturer

All stages of production, including production quality control. Merck Sante S. A. S., France. Centre de produccion Semois, 2 Rue du Pressoir Ver-45400 Semois, France.

Or in the case of packaging of the Drug nanolek LLC

Production of the finished dosage form and packaging (primary packaging): Merck Sante S. a. s., France, centre de produccion Semois, 2 Rue du Pressoir Ver, 45400 Semois, France.

Secondary (consumer packaging) and manufacturing quality control: Nanolek LLC, Russia. 612079, Kirov region, orichevsky district, village. Levintsy, nanolek biomedical complex.

for 750 mg and 1000 mg

Or manufacturer

All stages of production, including production quality control. Merck KGaA, Germany Frankfurter Strasse 250, 64293, Darmstadt, Germany.

Registration certificate holder: Merck Sante S. a. s., France. Legal address: 37, Rue Saint-Romain, 69379, Lyon sedex, 08, France.

Consumer complaints and information about undesirable phenomena should be sent to Merck LLC: 35, Valovaya street, Moscow, 115054.

Tel.: (495) 937-33-04; (495) 937-33-05.

e-mail: safety@merck.ru

The appearance of the product may differ from the photos on the site.

Information about prescription drugs is for professionals only. The information provided should not be used by patients to make an independent decision on the use of the presented drugs and cannot serve as a substitute for a full-time consultation with a doctor.

A description of the active substances of the drug is provided. The scientific information provided is generalized and cannot be used to decide on the possibility of using a specific drug.

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