Glucophage Long
Glucophage Long: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Glucophage long
ATX code: A10BA02
Active ingredient: Metformin (Metformin)
Manufacturer: Merck, KGaA (Germany), Merck Sante, sas (France)
Description and photo update: 2018-23-10
Prices in pharmacies: from 159 rubles.
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Glucophage Long is a drug with hypoglycemic action.
Release form and composition
The dosage form of Glucophage Long is prolonged-release tablets: capsule-shaped, biconvex, almost white or white, engraved on one side "500", "750" or "1000" (depending on the dosage); 750 and 1000 mg each - engraved on the other side "Merck" (7 pcs. in blisters, in a cardboard box 4 or 8 blisters; 10 pcs. in blisters, in a cardboard box 3 or 6 blisters; 15 pcs. in blisters, in a cardboard box 2 or 4 blisters; the symbol "M" is applied to the blister and the cardboard box to protect against falsification).
Composition of 1 tablet:
- active substance: metformin hydrochloride - 500, 750 or 1000 mg;
- auxiliary components (500/750/1000 mg): sodium carmellose - 50 / 37.5 / 50 mg; microcrystalline cellulose - 102/0/0 mg; hypromellose 2208 - 358 / 294.24 / 392.3 mg; hypromellose 2910 - 10/0/0 mg; magnesium stearate - 3.5 / 5.3 / 7 mg.
Pharmacological properties
Pharmacodynamics
Glucophage Long belongs to the group of oral hypoglycemic drugs from the biguanide group, which lower the basal and postprandial plasma glucose levels in the blood.
Metformin does not stimulate insulin secretion and does not lead to the development of hypoglycemia. Increases the sensitivity of peripheral receptors to insulin and glucose utilization by cells. By inhibiting glycogenolysis and gluconeogenesis, it reduces the production of glucose by the liver. Delays the absorption of glucose in the intestine.
Metformin, acting on glycogen synthetase, stimulates glycogen synthesis. Increases the transport capacity of all types of membrane glucose transporters.
The substance has a beneficial effect on lipid metabolism: it lowers the content of triglycerides, low density lipoproteins (LDL) and total cholesterol.
During therapy, the patient's weight either remains stable or decreases moderately.
Pharmacokinetics
Absorption of metformin after oral administration of Glucophage Long versus slow-release conventional-release tablets. T max (time to reach the maximum concentration of the substance) after taking 500 mg is 7 hours (when taking 1500 mg, T max can fluctuate in the range of 4-12 hours), T max for conventional-release tablets - 2.5 hours.
In steady state, C max (maximum concentration of the substance) and AUC (area under the concentration-time curve) increase in a non-proportional manner to the dose. After a single dose of 2000 mg of metformin in the form of sustained-release tablets, the AUC is similar to that after taking 1000 mg of metformin 2 times a day in the form of conventional-release tablets.
In individual patients, fluctuations in C max and AUC in the case of taking Glucophage Long are similar to the same indicators as in the case of taking tablets with a normal release profile.
The absorption of metformin from sustained-release tablets does not depend on food intake.
The binding of the substance to plasma proteins is negligible. C max in blood is lower than plasma C max and is reached after approximately the same time. Average V d (volume of distribution) ranges from 63 to 276 liters.
Cumulation of metformin with repeated administration of up to 2000 mg per day is not observed.
No metabolites were found.
T 1/2 (half-life) after oral administration is about 6.5 hours. It is excreted by the kidneys unchanged. Renal clearance of the substance is> 400 ml / min (metformin is excreted by tubular secretion and glomerular filtration).
The clearance of metformin in patients with impaired renal function decreases in proportion to creatinine clearance, T 1/2 increases in this group of patients, which may cause an increase in its plasma concentration.
Indications for use
Glucophage Long is prescribed for the treatment of type 2 diabetes mellitus in cases of ineffectiveness of diet therapy and physical activity (especially with obesity).
The drug can be used as monotherapy or in combination with other oral hypoglycemic drugs or insulin.
Contraindications
Absolute:
- impaired renal function or renal failure (creatinine clearance <45 ml / min);
- diabetic precoma, diabetic ketoacidosis, coma;
- clinically pronounced manifestations of chronic / acute diseases that can lead to tissue hypoxia (including acute myocardial infarction, acute heart failure, respiratory failure, chronic heart failure with unstable hemodynamic parameters);
- acute conditions, accompanied by the risk of impaired renal function, including dehydration (with severe / chronic diarrhea, repeated bouts of vomiting), shock, infectious diseases in a severe course (in particular, urinary and respiratory tract infections);
- hepatic dysfunction, liver failure;
- trauma and major surgical operations, in which insulin therapy is indicated;
- lactic acidosis, including a burdened history;
- acute alcohol poisoning, chronic alcoholism;
- adherence to a hypocaloric diet (less than 1000 kcal per day);
- radioisotope / X-ray studies with the introduction of an iodine-containing contrast agent (within 48 hours before / after them);
- pregnancy;
- age up to 18 years;
- individual intolerance to the components of the drug.
Relative (Glucophage Long is prescribed under medical supervision):
- renal failure (creatinine clearance - 45-59 ml / min);
- lactation period;
- age over 60 years against the background of performing heavy physical work (due to an increased likelihood of lactic acidosis).
Instructions for the use of Glucophage Long: method and dosage
Glucophage Long is taken orally with a sufficient amount of liquid, preferably during / after dinner. The tablets should be swallowed whole without chewing.
Frequency rate of admission - 1 time per day.
The drug must be taken daily. In case of termination of admission, the patient must inform the doctor about it.
The dose of the drug is determined individually based on the results of measuring the concentration of glucose in the blood.
At the beginning of treatment, patients who are not taking metformin, when conducting monotherapy or combination therapy with other hypoglycemic agents, are prescribed Glucophage Long 500 mg or Glucophage Long 750 mg. 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 gradual increase in the dose improves the tolerability of therapy from the gastrointestinal tract.
The maximum daily dose is 2000 mg. If glucose control cannot be achieved, you can consider using the daily dose in 2 divided doses (equal parts, during breakfast and dinner). If adequate glycemic control is not achieved in this case, it is possible to switch to metformin in the form of tablets with the usual release profile (in particular, Glucophage) at a maximum daily dose of 3000 mg.
For patients who are already receiving metformin, Glucophage Long is prescribed in the same daily dose as the drug in the form of tablets with a regular release profile.
For patients taking metformin in the form of conventional tablets at a dose higher than 2000 mg per day, switching to Glucophage Long is not recommended.
With renal failure of moderate severity (with creatinine clearance of 45-59 ml / min), metformin can be used only in cases of absence of conditions in which an increase in the likelihood of lactic acidosis is possible. At the beginning of treatment, this group of patients is prescribed Glucophage Long 500 mg or Glucophage Long 750 mg in 1 dose, the maximum daily dose is 1000 mg. Renal function should be monitored every 3–6 months. If creatinine clearance is below 45 ml / min, therapy is interrupted immediately.
In elderly patients, the dose of metformin should be adjusted based on the assessment of renal function, which should be performed regularly (at least twice a year).
If a dose is accidentally missed, it should be taken as soon as possible. Do not take a double dose of the drug.
Side effects
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):
- nervous system: often - metallic taste in the mouth;
- hepatobiliary system: very rarely - hepatitis or abnormal liver function indicators (usually, adverse events after discontinuation of metformin completely disappear);
- digestive system: very often - vomiting, nausea, abdominal pain, diarrhea, lack of appetite (most often disorders develop in the initial period of therapy and subsequently, as a rule, spontaneously disappear; taking Glucophage Long simultaneously with food, as well as a gradual increase in the dose contribute reducing the likelihood of these adverse reactions);
- metabolism: very rarely - lactic acidosis; during a long course - a decrease in the absorption of vitamin B 12 (in cases of diagnosing megaloblastic anemia, this violation must be taken into account);
- skin: very rarely - itching, erythema, urticaria.
Overdose
The main symptoms: when using 85,000 mg of metformin (42.5 times higher than the maximum daily dose), hypoglycemia did not develop, however, in this case, the appearance of lactic acidosis was observed. A significant overdose / presence of associated risk factors can cause lactic acidosis.
If signs of lactic acidosis appear, Glucophage Long should be canceled immediately. The patient should be urgently hospitalized to clarify the diagnosis (after determining the concentration of lactate). The most effective measure for removing metformin and lactate from the body is hemodialysis. It also shows symptomatic treatment.
special instructions
Due to the accumulation of metformin, a rare but serious complication, lactic acidosis, is possible, which is characterized by high mortality in the absence of urgent treatment. Basically, during the use of Glucophage Long, such cases occurred in diabetes mellitus against the background of severe renal failure.
Other associated risk factors should also be considered: ketosis, poorly controlled diabetes, prolonged fasting, liver failure, excessive alcohol consumption and any conditions associated with severe hypoxia.
In addition, it is necessary to take into account the likelihood of lactic acidosis with the appearance of muscle cramps, which are accompanied by abdominal pain, dyspepsia, severe malaise and general weakness.
Lactic acidosis is characterized by abdominal pain, vomiting, acidotic dyspnea, hypothermia, and muscle cramps followed by coma. Diagnostic laboratory parameters - a decrease in blood pH (5 mmol / l, an increased lactate / pyruvate ratio and an increased anion gap. If lactic acidosis is suspected, Glucophage Long is immediately canceled.
The drug should be interrupted 48 hours before scheduled surgery. Resumption of therapy is possible after 48 hours, provided that during the examination, renal function was found to be normal.
Before starting treatment and regularly in the future, it is necessary to determine the creatinine clearance: in the absence of violations - at least 1 time per year, in elderly patients, as well as in patients with creatinine clearance at the lower limit of the norm - from 2 to 4 times a year. With creatinine clearance less than 45 ml / min, the use of Glucophage Long is contraindicated.
In the presence of a possible impairment of renal function against the background of combined use with antihypertensive drugs, diuretics or non-steroidal anti-inflammatory drugs in elderly patients, special care should be taken.
A higher risk of developing hypoxia and renal failure is observed in patients with heart failure. During therapy, this group of patients requires regular monitoring of cardiac function and renal function.
Patients are advised to continue on a diet that consumes even carbohydrates throughout the day.
If you are overweight, you should continue to adhere to a low-calorie diet (but not less than 1000 kcal per day). Also, patients need to exercise regularly.
Any infectious disease (urinary and respiratory tract infections) and treatment should be reported to your doctor.
To control diabetes mellitus, routine laboratory tests are required.
When monotherapy Glucophage Long does not cause hypoglycemia, however, when it is used in combination with insulin or other oral hypoglycemic agents, it is recommended to exercise caution. The main symptoms of hypoglycemia: increased sweating, weakness, dizziness, headache, heart palpitations, impaired concentration or vision.
The inactive components of Glucophage Long can be excreted unchanged through the intestines, which does not affect the therapeutic activity of the drug.
Influence on the ability to drive vehicles and complex mechanisms
When carrying out combination therapy with other hypoglycemic drugs (sulfonylurea derivatives, insulin, repaglinide), hypoglycemia may develop, which must be taken into account when driving.
Application during pregnancy and lactation
- pregnancy: therapy is contraindicated, which is associated with an increased risk of congenital malformations and perinatal mortality;
- lactation period: Glucophage Long can be used with caution after assessing the benefit / risk ratio.
Pediatric use
The drug is not prescribed to patients under the age of 18, since there is no reliable information confirming its effectiveness / safety.
With impaired renal function
- impaired renal function (creatinine clearance less than 60 ml / min), acute conditions occurring with a risk of impaired renal function (including dehydration with severe / chronic diarrhea, repeated bouts of vomiting), severe infectious diseases, shock: the use of Glucophage Long is contraindicated;
- renal impairment (creatinine clearance 45-59 ml / min): therapy should be carried out with caution.
For violations of liver function
According to the instructions, Glucophage Long is not prescribed for violations of liver function and liver failure.
Use in the elderly
Patients over 60 years old, while performing heavy physical work, Glucophage Long is prescribed with caution (due to the increased likelihood of lactic acidosis).
Drug interactions
Radiological examination with the use of iodine-containing X-ray contrast agents for functional renal failure in patients with diabetes mellitus can lead to the development of lactic acidosis. Glucophage Long should be canceled 48 hours before the study. If, during the examination, renal function was found to be normal, therapy can be resumed after 48 hours.
Against the background of ethanol intake, the likelihood of lactic acidosis during acute alcohol intoxication increases, especially in liver failure, as well as in cases of adherence to a low-calorie diet and malnutrition. Medicines containing ethanol should not be used during treatment.
Combinations requiring caution:
- diuretics, danazol, beta 2 -adrenergic agonists, chlorpromazine (in doses of 100 mg per day), drugs with indirect hyperglycemic action (in particular, glucocorticosteroids and tetracosactide for local / systemic use): more frequent monitoring of blood glucose concentration may be required, especially at the beginning of therapy; in cases of need in the course of treatment, the dose of Glucophage Long can be adjusted;
- "Loop" diuretics: the development of lactic acidosis (associated with possible functional renal failure);
- sulfonylurea derivatives, insulin, acarbose, salicylates: development of hypoglycemia;
- nifedipine: increased absorption and C max of metformin;
- colevelam: an increase in the plasma concentration of metformin in the blood (an increase in AUC without a significant increase in C max);
- cationic drugs (quinine, triamterene, ranitidine, quinidine, amiloride, digoxin, procainamide, morphine, vancomycin and trimethoprim) that are secreted in the renal tubules: competing with metformin for tubular transport systems, which may cause an increase in its C max.
Analogs
Analogues of Glucophage Long are: Formetin, Metformin, Metadien, Formin Pliva, Diasfor, Bagomet, Glyformin, Glucophage, Sofamet and others.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25/30 ° C (tablets of 500 and 750 mg / 1000 mg).
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Glucophage Long
According to reviews, Glucophage Long is an effective drug for long-term use. The development of side effects is rarely reported. With overweight, a gradual decrease is noted.
Price for Glucophage Long in pharmacies
The approximate price for Glucophage Long is (30 or 60 tablets per pack):
- 500 mg: 254-287 or 384-455 rubles;
- 750 mg: 283–338 or 569 rubles;
- 1000 mg: 324 or 676 rubles.
Glucophage Long: prices in online pharmacies
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
