Composition
Active ingredients:
metformin 500 mg
Excipients:
povidone K 90;
corn starch;
crospovidone;
magnesium stearate;
talc
 Shell composition:
methacrylic acid and methyl methacrylate copolymer (eudragite L 100-55); macrogol 6000; titanium dioxide; talc
Pharmacological action
Metformin inhibits gluconeogenesis in the liver, reduces glucose absorption from the intestine, enhances peripheral glucose utilization, and also 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.
PHARMACOKINETICS
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 without a tendency to ketoacidosis (especially in obese patients) when diet therapy is ineffective; in combination with insulin – in type 2 diabetes mellitus, especially with a pronounced degree of obesity, accompanied by secondary insulin resistance.
Use during pregnancy and lactation
When planning pregnancy, as well as in the case of pregnancy while taking Metformin, it should be canceled and insulin therapy should be prescribed.
Since there are no data on penetration into breast milk, this drug is contraindicated during breastfeeding.
If it is necessary to use Metformip during breastfeeding, breast-feeding should be discontinued.
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
Simultaneous use of danazol is not recommended in order to avoid the hyperglycemic effect of the latter. If treatment with danazol is necessary and after discontinuation of the latter, it is necessary to adjust the dose of metformin and monitor the level of glycemia.
Combinations that require special caution: chlorpromazine-when taken in large doses (100 mg/day) increases glycemia, reducing the release of insulin.
During treatment with neuroleptics and after discontinuation of the latter, it is necessary to adjust the dose of metformin under the control of the level of glycemia.
When used concomitantly with sulfonylureas, acarbose, insulin, NSAIDs, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate derivatives, cyclophosphamide, and beta-blockers, the hypoglycemic effect of metformin may be enhanced.
When used concomitantly with corticosteroids, oral contraceptives, epinephrine, sympathomimetics, glucagon, thyroid hormones, thiazide and loop diuretics, phenothiazine derivatives, nicotinic acid derivatives, the hypoglycemic effect of metformin may decrease.
Cimetidine slows down the elimination of metformin, which increases the risk of lactic acidosis.
Metformin may weaken the effect of anticoagulants (coumarin derivatives).
Alcohol consumption increases the risk of lactic acidosis during acute alcohol intoxication, especially in cases of fasting or following a low-calorie diet, as well as in cases of liver failure.
How to take, course of use and dosage
The dose of the drug is set by the doctor individually, depending on the level of glucose in the blood.
The initial dose is 500-1000 mg per day (1-2 tablets). After 10-15 days, a further gradual increase in the dose is possible, depending on the blood glucose level.
The maintenance dose of the drug is usually 1500-2000 mg per day. (3-4 tablets) The maximum dose is 3000 mg per day (6 tablets).
In elderly patients, the recommended daily dose should not exceed 1 g (2 tablets).
Metformin tablets should be taken whole during or immediately after a meal, with a small amount of liquid (a glass of water). To reduce side effects from the gastrointestinal tract, the daily dose should be divided into 2-3 doses.
Due to the increased risk of lactic acidosis, the dose of the drug should be reduced in severe metabolic disorders.
Overdose
If Metformin is overdosed, lactic acidosis may develop with a fatal outcome. The cause of lactic acidosis may also be the accumulation of the drug due to impaired renal function.
Symptoms of lactic acidosis include nausea, vomiting, diarrhea, low body temperature, abdominal pain, muscle pain, and later rapid breathing, dizziness, impaired consciousness, and coma.
Treatment: Â if signs of lactic acidosis appear, treatment with Metformin should be stopped immediately, the patient should be urgently hospitalized and the diagnosis should be confirmed by determining the lactate concentration. The most effective measure for removing lactate and metformin from the body is hemodialysis. Symptomatic treatment is also performed.
Hypoglycemia may occur when Metformin is combined with sulfonylureas.
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.
Form of production
Tablets
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C
Shelf life
2 years
Active ingredient
Metformin
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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