Composition
1 tablet contains:
Active ingredients:
metformin 850 mg
Pharmacological action
Metformin inhibits gluconeogenesis in the liver, reduces glucose absorption from the intestine, increases peripheral glucose utilization, and increases the sensitivity of tissues to insulin.
At the same time, it does not affect the secretion of insulin by beta cells of the pancreas, and does not cause hypoglycemic reactions. Reduces the level of triglycerides and low-density linoproteins in the blood.
Stabilizes or reduces body weight. It has a fibrinolytic effect by suppressing the tissue-type plasminogen activator inhibitor.
After oral use, metformin is absorbed from the gastrointestinal tract. Bioavailability after taking a standard dose is 50-60%. Cmax in blood plasma is reached 2.5 hours after oral use.
Practically does not bind to plasma proteins.
It accumulates in the salivary glands, muscles, liver and kidneys. It is excreted unchanged by the kidneys. T1 / 2 is 9-12 hours. With impaired renal function, accumulation of the drug is possible.
Indications
Type 2 diabetes mellitus in adults (especially in obese patients) when diet therapy and exercise are ineffective, as monotherapy or in combination with other oral hypoglycemic agents or insulin.
Type 2 diabetes mellitus in children from 10 years of age – both as monotherapy and in combination with insulin.
Contraindications
- diabetic ketoacidosis, diabetic precoma, coma;
- the impairment of renal function;
- acute illness with a risk of kidney problems: dehydration (diarrhea, vomiting), fever, severe infectious diseases, the condition of hypoxia (shock, sepsis, kidney infection, chronic lung disease);
- symptomatic manifestations of acute and chronic diseases, which can lead to the development of tissue hypoxia (cardiac or respiratory failure, acute myocardial infarction);
- major surgery or trauma (when shown holding insulin);
- the liver;
- chronic alcoholism, acute alcohol poisoning;
- the application for at least 2 days before and for 2 days after the radioisotope or radiological examinations with the use of iodinated contrast agents;
- lactic acidosis (including history);
- adherence to a reduced-calorie diet (less than 1000 cal/day);
- pregnancy;
- lactation;
- hypersensitivity to the drug.
It is not recommended to use the drug in people over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis.
Side effects
From the side of the digestive system: Â nausea, vomiting, metallic taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain. These symptoms are particularly common at the beginning of treatment and usually resolve on their own. These symptoms can be reduced by prescribing anthocides, atropine derivatives, or antispasmodics.
From the side of metabolism: Â in rare cases – lactic acidosis (requires discontinuation of treatment); with prolonged treatment-hypovitaminosis In 12(malabsorption).
From the side of hematopoietic organs: Â in some cases – megaloblastic anemia.
From the endocrine system: Â hypoglycemia.
Allergic reactions: Â skin rash.
Interaction
Contraindicated combinations
Radiological studies with the use of iodine-containing radiopaque drugs can cause the development of lactic acidosis in patients with diabetes mellitus against the background of functional renal failure. The use of metformin should be discontinued 48 hours before and not resumed earlier than 48 hours after X-ray examination using radiopaque drugs. Not recommended combinations
Concomitant use of metformin with alcohol and ethanol-containing drugs, during acute alcohol intoxication, fasting or following a low-calorie diet, as well as with liver failure increases the risk of lactic acidosis.
Combinations that require extreme caution When metformin is co-administered with danazole, a hyperglycemic effect may develop. If treatment with danazol is necessary and after discontinuation of its use, it is necessary to adjust the dose of metformin under the control of blood glucose concentration.
Chlorpromazine in high doses (100 mg/day) reduces the release of insulin and increases the concentration of glucose in the blood. When used concomitantly with antipsychotics and after discontinuation of their use, it is necessary to adjust the dose of metformin under the control of blood glucose concentration.
Glucocorticosteroids (corticosteroids), when administered parenterally and topically, reduce glucose tolerance and increase blood glucose concentrations, in some cases causing ketosis. If it is necessary to use such a combination and after discontinuation of corticosteroids, it is necessary to adjust the dose of metformin under the control of blood glucose concentration.
With the simultaneous use of loop diuretics and metformin, there is a risk of lactic acidosis due to the possible appearance of functional renal failure.
The use of beta-2-adrenomimetics in the form of injections reduces the hypoglycemic effect of metformin due to stimulation of beta-2-adrenergic receptors. In this case, you should monitor the concentration of glucose in the blood and, if necessary, use insulin. Angiotensin-converting enzyme inhibitors and other antihypertensive medications may reduce blood glucose concentrations. If necessary, the metformin dose should be adjusted.
Concomitant use of metformin with sulfonylurea derivatives, insulin, acarbose and salicylates may increase the hypoglycemic effect.
Nifedipine increases the absorption and Cmax of metformin, which should be taken into account when using them simultaneously. Loop diuretics and nonsteroidal anti-inflammatory drugs (NSAIDs) increase the risk of decreased kidney function. In this case, caution should be exercised when using metformin.
How to take, course of use and dosage
Tablets should be taken orally, swallowed whole, without chewing, during or immediately after a meal, with a sufficient amount of water.
AdultsMonotherapy and combination therapy with other oral hypoglycemic agents
The recommended starting dose is 1000-1500 mg / day. To reduce side effects from the gastrointestinal tract, the dose should be divided into 2-3 doses. After 10-15 days, in the absence of adverse effects from the gastrointestinal tract, a further gradual increase in the dose is possible, depending on the concentration of glucose in the blood. A slow increase in the dose may improve the gastrointestinal tolerance of the drug.
The maintenance daily dose is 1500-2000 mg. The maximum daily dose is 3000 mg, divided into 3 doses. When planning to switch from taking another oral hypoglycemic agent to Metformin, it is necessary to stop taking another hypoglycemic agent and start taking Metformin Canon in the above doses. Combination therapy with insulin
The recommended initial dose of Metformin is 500 mg and 850 mg – 1 tablet 2-3 times a day, Metformin 1000 mg-1 tablet 1 time a day, the dose of insulin is selected based on blood glucose concentration indicators.
Children over 10 years of age
Metformin Canon is used in monotherapy and in combination therapy with insulin. The recommended starting dose of Metformin is 500 mg once a day in the evening with meals. After 10-15 days, the dose of the drug should be adjusted based on the concentration of glucose in the blood. The maintenance dose is 1000-1500 mg / day in 2-3 divided doses. The maximum daily dose is 2000 mg in 3 divided doses.
Elderly patients Due to a possible decrease in renal function, the dose of Metformin should be selected under regular monitoring of renal function indicators (monitoring of serum creatinine concentrations at least 2-4 times a year). The duration of treatment is determined by the doctor. It is not recommended to stop taking the drug without the instructions of the attending physician.
Overdose
Symptoms: when using metformin at a dose of 85 g, hypoglycemia was not observed, but lactic acidosis was observed. Early symptoms of lactic acidosis include nausea, vomiting, diarrhea, a decrease in body temperature, abdominal pain, muscle pain, and later rapid breathing, dizziness, impaired consciousness, and coma may occur.
Treatment: In case of signs of lactic acidosis, treatment with the drug should be stopped immediately, the patient should be urgently hospitalized and, having determined 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
During treatment, it is necessary to monitor kidney function. At least 2 times a year, as well as when myalgia occurs, the plasma lactate content should be determined. In addition, once every 6 months, it is necessary to monitor the level of creatinine in the blood serum (especially in patients, the elderly). Metformin should not be used if the blood creatinine level is higher than 135 mmol / l in men and 110 mmol/L in women.
It is possible to use Metformin in combination with sulfonylurea derivatives. In this case, especially careful monitoring of blood glucose levels is necessary.
Metformin should be discontinued 48 hours before and 48 hours after radiopaque radiography (urography, IV angiography).
If a patient has a bronchopulmonary infection or an infectious disease of the genitourinary organs, you should immediately inform your doctor about this.
During treatment, you should refrain from taking alcohol and medications containing ethanol..
Influence on the ability to drive motor vehicles and manage mechanisms
The use of the drug in monotherapy does not affect the ability to drive vehicles and work with mechanisms.
When Metformin is combined with other hypoglycemic agents (sulfonylureas, insulin), hypoglycemic conditions may develop, in which the ability to drive vehicles and engage in other potentially dangerous activities that require increased attention and rapid psychomotor reactions deteriorates.
Storage conditions
Store in a dry place protected from light at a temperature not exceeding 25 °C. Keep out of reach of children.
Active ingredient
Metformin
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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