Metformin-Akrikhin
Metformin-Akrikhin: 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 Metformine-Akrikhin
- 19. Price in pharmacies
Latin name: Metformin-Akrikhin
ATX code: A10BA02
Active ingredient: metformin (Metformin)
Manufacturer: JSC "Akrikhin" (Russia)
Description and photo update: 09.10.2019
Prices in pharmacies: from 119 rubles.
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Metformin-Akrikhin is an oral hypoglycemic drug of the biguanide group.
Release form and composition
Dosage forms:
- film-coated tablets: from white to white with a cream or gray shade of color, oval, biconvex (10 pcs. in blisters, in a cardboard box 3 or 6 packs; 30 or 60 pcs. in polypropylene / polyethylene cans, in a cardboard box 1 can);
- tablets: almost white or white, round, flat-cylindrical, with a chamfer and a dividing line (10 pcs. in blister strip packs, in a cardboard box of 3, 6 or 10 packs).
Each pack also contains instructions for the use of Metformin-Akrikhin.
1 film-coated tablet contains:
- active substance: metformin hydrochloride in terms of 100% substance - 0.85 g or 1 g;
- auxiliary components: potato starch, stearic acid, povidone (type K90), colloidal silicon dioxide, glycerol;
- film shell: macrogol-6000, hypromellose-2910, talc.
1 tablet contains:
- active substance: metformin hydrochloride in terms of 100% substance - 0.5 g;
- auxiliary components: sorbitol, povidone (type K90), macrogol-6000, calcium hydrogen phosphate dihydrate, crospovidone (type B), stearic acid.
Pharmacological properties
Pharmacodynamics
Metformin-Akrikhin is an oral hypoglycemic drug of the biguanide group. Its active substance, metformin, differs from sulfonylurea derivatives in that it does not stimulate insulin secretion. The action of metformin is aimed at increasing the sensitivity of peripheral receptors to insulin and stimulating the utilization of glucose by cells, reducing the production of glucose by the liver by inhibiting glycogenolysis and gluconeogenesis, and slowing down the absorption of carbohydrates in the intestine. Taking the drug by healthy individuals does not show a hypoglycemic effect and does not lead to the development of hypoglycemia. Promotes an increase in the transport capacity of all types of membrane glucose transporters. As a result of the effect on glycogen synthase, glycogen synthesis is potentiated.
Metformin-Akrikhin has a beneficial effect on lipid metabolism, lowering the content of low density lipoproteins, total cholesterol and triglycerides.
Against the background of the use of the drug, the patient's body weight remains stable or moderately decreases.
In addition, the results of clinical trials indicate the efficacy of using metformin to prevent the development of type 2 diabetes mellitus in patients with prediabetes and additional risk factors if lifestyle changes do not allow them to achieve adequate glycemic control.
Pharmacokinetics
After oral administration, the proportion of absorbed metformin from the gastrointestinal tract (GIT) is 70-80%. Absolute bioavailability is 50-60%. The maximum concentration (C max) of metformin in the blood plasma is reached after 2.5 hours. To achieve an equilibrium concentration in the blood plasma against the background of the use of metformin in therapeutic doses, it takes 24-28 hours, usually it does not exceed 0.001 mg / ml. Simultaneous food intake lowers and delays the absorption of the drug.
The pharmacokinetics of absorption is not linear, the process is characterized by saturation.
Metformin practically does not bind to plasma proteins. For the same period C max in blood is lower than in blood plasma.
It is quickly distributed into tissues, penetrates into erythrocytes. It is assumed that erythrocytes are the secondary compartment of metformin distribution. The volume of distribution can be from 63 to 276 liters.
Metformin is not actually metabolized, its metabolites are not found in the body.
It is excreted mainly through the kidneys unchanged. The clearance of metformin is 4 times greater than the clearance of creatinine, and is more than 400 ml / min. This indicates the presence of active tubular secretion.
The half-life (T 1/2) is about 6.5 hours.
In case of impaired renal function, a decrease in metformin clearance is observed in proportion to creatinine clearance (CC), which leads to an increase in T 1/2, the level of metformin concentration in blood plasma and increases the risk of cumulation.
The pharmacokinetic parameters of metformin in children after a single dose of 0.5 g are similar to those in healthy adults.
Indications for use
The use of Metformin-Akrikhin is indicated for the treatment of type 2 diabetes mellitus (non-insulin dependent) in patients over the age of 10 years as monotherapy or in combination with insulin if diet therapy and physical activity do not provide sufficient glycemic control, especially in obesity.
For adults, the drug can also be prescribed in combination with other oral hypoglycemic agents.
In addition, the use of film-coated tablets is indicated for the prevention of the development of type 2 diabetes mellitus in patients with prediabetes and additional risk factors for the development of type 2 diabetes mellitus, with the ineffectiveness of diet therapy and physical activity.
Contraindications
Absolute:
- diabetic ketoacidosis, diabetic precoma, or coma;
- renal failure;
- impaired renal function with CC less than 30 ml / min;
- impaired liver function, liver failure;
- acute conditions (including severe infectious diseases, dehydration against the background of diarrhea or vomiting, shock) that increase the risk of developing renal dysfunction;
- clinically pronounced manifestations of respiratory failure, acute heart failure, chronic heart failure with unstable hemodynamic parameters, acute myocardial infarction and other acute or chronic diseases that can cause the development of tissue hypoxia;
- extensive trauma and surgery involving the transition to insulin therapy;
- chronic alcoholism, acute alcohol poisoning;
- lactic acidosis (including history);
- a period of less than 48 hours before and after the administration of an iodine-containing contrast agent for radioisotope and X-ray studies;
- adherence to a hypocaloric diet (less than 1000 kcal / day);
- period of pregnancy;
- breast-feeding;
- age up to 10 years;
- hypersensitivity to the components of the drug.
Care should be taken to prescribe Metformin-Akrikhin for renal failure (CC 30-59 ml / min), children aged 10 to 12 years, patients over 60 years old, engaged in heavy physical work, which is associated with heavy loads.
Particular care should be taken with heart failure; the simultaneous use of the drug with insulin, sulfonylurea derivatives, repaglinide or other hypoglycemic agents, antihypertensive drugs, non-steroidal anti-inflammatory drugs or diuretics; with chronic or severe diarrhea, repeated bouts of vomiting and other conditions that can cause dehydration.
Metformin-Akrikhin, instructions for use: method and dosage
Metformin-Akrikhin tablets are taken orally, swallowing whole, during or immediately after a meal, with a sufficient amount of water.
Since it is impossible to violate the integrity of the film shell, if it is necessary to use an initial dose of 0.5 g, a dosage form of metformin of the appropriate dosage should be used.
The duration of treatment is determined by the attending physician; without his appointment, it is impossible to interrupt the drug intake.
Recommended dosage for adults in monotherapy and in combination with other oral hypoglycemic agents:
- initial dose: 0.5 or 0.85 g 2-3 times a day. Taking into account the level of glucose in the blood, it can be gradually increased;
- maintenance dose: 1.5–2.0 g per day, divided into 2–3 doses;
- maximum dose: 3.0 g per day, divided into 3 doses.
To reduce side effects from the gastrointestinal tract, the daily dose should be increased slowly and always divided into 2-3 doses.
In case of switching from another hypoglycemic agent to Metformin-Akrikhin tablets, therapy should be started after discontinuation of treatment with the previous agent, using the recommended dosing regimen.
When combined with insulin, the initial dose of the drug is 0.5 or 0.85 g 2-3 times a day, the dose of insulin is determined in accordance with the level of glucose concentration in the blood.
Recommended dosage of Metformin-Akrikhin for children over the age of 10 years with monotherapy and in combination with insulin:
- initial dose: 0.5 or 0.85 g. After 10-15 days of therapy, dose adjustment is required taking into account glycemic control;
- maximum daily dose: 2.0 g, divided into 2-3 doses.
The recommended dosage for monotherapy in prediabetes is 1.0 to 1.7 g per day, divided into 2 doses. Treatment must be accompanied by regular glycemic control to assess the need to continue the course.
For patients with moderate renal failure (CC 30-59 ml / min), Metformin-Akrikhin is indicated (provided that there are no conditions that increase the risk of lactic acidosis) at an initial dose of 0.5 or 0.85 g 1 time per day. The maximum daily dose is 1 g, divided into 2 doses. The maximum maintenance daily dose is divided into 2–3 doses and, taking into account the degree of impairment of renal function, can be: with CC 45–59 ml / min - 2 g; with CC 30-44 ml / min - 1 g.
In patients with renal impairment, renal function should be carefully assessed at 90–180 days intervals. With CC below 30 ml / min, the use of the drug should be discontinued.
Elderly patients need regular (at intervals of 90 days) studies to determine the concentration of creatinine in the blood serum. The selection and correction of the dose of Metformin-Akrikhin is performed in accordance with the indicators of renal function.
Side effects
- from the nervous system: often - the appearance of a metallic taste in the mouth;
- from the side of metabolism and nutrition: very rarely - lactic acidosis; possibly - against the background of prolonged use, a decrease in the absorption of vitamin B 12, megaloblastic anemia;
- from the gastrointestinal tract: very often - lack of appetite, nausea, abdominal pain, vomiting, diarrhea, flatulence;
- from the hepatobiliary system: very rarely - impaired liver function indicators, hepatitis (completely disappear after discontinuation of the drug);
- from the skin and subcutaneous tissues: very rarely - skin reactions in the form of itching, rash, erythema, urticaria.
Overdose
Symptoms: the development of lactic acidosis with the following characteristic features: acidotic shortness of breath, abdominal pain, hypothermia, coma. Diagnostic laboratory indicators include a decrease in blood acidity (pH less than 7.35), a plasma lactate concentration of more than 5 mmol / L, an increased anion gap and a lactate / pyruvate ratio.
A case of taking metformin at a dose of 85 g once was registered, which exceeds the maximum daily dose by 42.5 times. Such an overdose did not cause the development of hypoglycemia.
Treatment: if signs of lactic acidosis appear, immediate hospitalization of the patient is required. In order to clarify the diagnosis, the concentration of lactate should be determined. For the rapid elimination of lactate and metformin from the body, the most effective is the use of hemodialysis. The appointment of symptomatic therapy is shown.
special instructions
When treating with Metformin-Akrikhin, it is recommended to continue adhering to a diet with a uniform intake of carbohydrates throughout the day. A low-calorie diet in overweight patients should provide at least 1000 kcal per day.
To control diabetes mellitus, routine laboratory tests are required.
A serious complication of the cumulation of metformin is lactic acidosis, in the absence of urgent therapy, it can be fatal. Due to the risk of lactic acidosis, special care should be taken when prescribing metformin to patients with the following risk factors: decompensated diabetes mellitus, renal and / or hepatic failure, alcoholism, ketosis, prolonged fasting, severe infectious disease, severe hypoxia, concomitant therapy with other drugs. Non-specific signs of lactic acidosis include muscle cramps with abdominal pain, dyspeptic disorders, and severe asthenia. If you suspect the development of lactic acidosis, you must stop taking Metformin-Akrikhin and immediately consult a doctor.
During the period of treatment, you should not drink alcoholic beverages and take ethanol-containing medicines.
When carrying out planned surgical interventions in patients with normal renal function, the drug should be discontinued 48 hours before the onset of anesthesia and resumed no earlier than 48 hours after the operation.
In addition, the state of renal function should be established before the administration of the drug, it should be regularly monitored during treatment. In patients with normal renal function, the CC index should be determined at least once every 12 months, with an initial CC of 45-59 ml / min - with an interval of 3-6 months, with CC 30-44 ml / min - every 3 months.
Due to the high risk of hypoxia and impaired renal function in patients with heart failure, this category of patients should be treated with metformin with regular monitoring of cardiac activity and monitoring of renal function.
Despite the fact that the results of clinical studies conducted for 12 months in children and adolescents indicate the absence of the effect of metformin on their growth and puberty, it is recommended to carefully monitor these parameters in children with a long course of therapy. According to the survey results, in the age group from 10 to 16 years, the nature and severity of side effects in children is similar to those in adult patients.
In patients with prediabetes, the use of Metformin-Akrikhin is indicated in the presence of the following additional risk factors for the development of type 2 diabetes mellitus: age up to 60 years, BMI (body mass index) 30 kg per 1 m 2 or more, arterial hypertension, increased concentration of triglycerides, a reduced concentration of high-density lipoprotein cholesterol, an indication in the history of gestational diabetes mellitus or the presence of diabetes mellitus in first-line relatives.
Influence on the ability to drive vehicles and complex mechanisms
Monotherapy with Metformin-Akrikhin does not affect the patient's ability to drive vehicles or complex mechanisms.
The use of the drug in combination with other hypoglycemic agents (insulin, sulfonylurea derivatives, repaglinide) increases the risk of hypoglycemia, therefore, when performing types of work that require increased concentration of attention and high speed of psychomotor reactions, care should be taken.
Application during pregnancy and lactation
The use of Metformin-Akrikhin during pregnancy and lactation is contraindicated.
When planning pregnancy or conception during therapy with the drug, metformin should be discontinued. Patients with type 2 diabetes mellitus are recommended to be transferred to insulin therapy.
Pediatric use
The appointment of Metformin-Akrikhin under the age of 10 is contraindicated.
The drug should be used with caution for the treatment of children from 10 to 12 years old.
With impaired renal function
The appointment of Metformin-Akrikhin is contraindicated in case of renal dysfunction with CC less than 30 ml / min, renal failure or conditions that increase the risk of renal dysfunction (acute period of severe infectious diseases, dehydration against the background of diarrhea or vomiting, shock).
The drug should be taken with caution in renal failure with a CC of 30–59 ml / min.
For violations of liver function
The use of Metformin-Akrikhin for the treatment of patients with impaired liver function, liver failure is contraindicated.
Use in the elderly
Care should be taken to prescribe Metformin-Akrikhin to patients over the age of 60 years.
The selection and adjustment of the dose should be made taking into account the indicators of renal function.
Drug interactions
With the simultaneous use of Metformin-Akrikhin:
- iodine-containing X-ray contrast agents: the use of iodine-containing X-ray contrast agents increases the risk of lactic acidosis, especially in patients with diabetes mellitus complicated by functional renal failure. If it is necessary to conduct a radiological study using iodine-containing X-ray contrast agents in patients with normal renal function, treatment with the drug should be temporarily interrupted for about 96 hours (canceled 48 hours before and resumed no earlier than 48 hours after the procedure);
- ethanol: against the background of acute alcohol intoxication, the risk of lactic acidosis increases, especially in patients with malnutrition, liver failure, or on a low-calorie diet;
- danazol: with combined use and after discontinuation of danazol, a dose adjustment of metformin and careful monitoring of blood glucose concentration are required due to the risk of hyperglycemic action of danazol;
- chlorpromazine: caution should be exercised if concomitant therapy with antipsychotics is required or immediately after their withdrawal. Taking chlorpromazine in a daily dose of 0.1 g helps to reduce the release of insulin and increase blood glucose levels, therefore, a dose adjustment of the hypoglycemic drug is required;
- glucocorticosteroids (GCS): the use of GCS of systemic and local action or after its termination causes the need to adjust the dose of metformin under the control of the concentration of glucose in the blood, because GCS reduce glucose tolerance and increase its concentration in the blood, up to the development of ketosis;
- diuretics: in patients with functional renal failure, concomitant therapy with loop diuretics can lead to the development of lactic acidosis, therefore, with CC less than 60 ml / min, this combination cannot be used;
- beta2-adrenergic agonists: injectable beta2-adrenergic agonists stimulate beta2-adrenergic receptors and increase the concentration of glucose in the blood, which may require additional insulin administration;
- antihypertensive drugs, including angiotensin-converting enzyme inhibitors: can cause a decrease in blood glucose, therefore, it may be necessary to adjust the dose of Metformin-Akrikhin;
- insulin, sulfonylurea derivatives, acarbose, salicylates: these drugs increase the risk of hypoglycemia;
- nifedipine: against the background of concomitant therapy with nifedipine, the absorption and C max of metformin increase;
- amiloride, digoxin, procainamide, morphine, quinidine, quinine, triamterene, trimethoprim, vancomycin, ranitidine: cationic drugs compete with metformin for transport systems in the renal tubules, which can lead to an increase in its C max;
- phenothiazides, glucagon, oral contraceptives, estrogens, phenytoin, sympathomimetics, nicotinic acid, isoniazid, BMCK (slow calcium channel blockers), sodium levothyroxine: a combination with the listed agents can reduce the hypoglycemic effect of Metformin-Akrikhin;
- cimetidine: reduces the rate of excretion of metformin, as a result of which the risk of developing lactic acidosis increases;
- indirect anticoagulants: it is possible to reduce the therapeutic effect of indirect anticoagulants;
- verapamil and other inhibitors of organic cation transporters1 (OCT1): a decrease in the hypoglycemic effect of Metformin-Akrikhin is possible;
- rifampicin and other OCT1 inducers: increase the absorption of metformin in the gastrointestinal tract and enhance its action;
- OCT2 inhibitors (including cimetidine, dolutegravir, ranolazine, trimethoprim, vandetanib, isavuconazole): with concomitant therapy with these agents, the risk of an increase in the concentration of metformin in blood plasma increases;
- crizotinib, olaparib (OCT1 and OCT2 inhibitors): when combined with metformin, cause a decrease in its hypoglycemic effect.
Analogs
Metformin-Akrikhin analogs are Metformin, Metformin Zentiva, Metformin Long Canon, Metformin MS, Metformin-Richter, Metformin-Teva, Baghomet, Glucophage, Glucophage Long, Diasfor, Diaformin OD, Merifatin, Metadien, Metfogamma, Sigduforong, Longioforvel Sopamet, Formetin, Formin Pliva, Formetin Long.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
Shelf life: film-coated tablets - 2 years, tablets - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Metformin-Akrikhin
Reviews of Metformin-Akrikhin are often negative. Patients report that taking the drug does not provide sufficient clinical effect. In addition, they often complain that it causes side reactions in the form of diarrhea, dry mouth.
Price for Metformin-Akrikhin in pharmacies
The price of Metformin-Akrikhin for a package containing 60 tablets, depending on the dosage, can be: 0.5 g - from 113 rubles; 0.85 g - from 180 rubles; 1 g - from 335 rubles.
Metformin-Akrikhin: prices in online pharmacies
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Drug name Price Pharmacy |
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Metformin-Akrikhin 500mg tablets 60 pcs. 119 RUB Buy |
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Metformin-Akrikhin 500 mg tablets 60 pcs. 119 RUB Buy |
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Metformin-Akrikhin 850 mg film-coated tablets 60 pcs. 204 RUB Buy |
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Metformin-Akrikhin 1000 mg film-coated tablets 60 pcs. 267 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
