Metformin, tablets 1000 mg 60 pcs

Metformin inhibits gluconeogenesis in the liver, reduces glucose absorption from the intestine, increases peripheral glucose utilization, and increases tissue sensitivity to insulin.

With this it has no effect on insulin secretion by beta cells of the pancreas, does not cause hypoglycemic reactions. Reduces the level of triglycerides and low-density linoproteins in the blood. Stabilizes or reduces body weight. Has a fibrinolytic effect due to the inhibition of tissue-type plasminogen activator inhibitor.

PHARMACOKINETICS

After oral administration, metformin is absorbed from the GI tract.

The bioavailability after a standard dose is 50-60%. Cmax in plasma is reached 2.5 h after oral administration.

It practically does not bind with plasma proteins. It accumulates in salivary glands, muscles, liver and kidneys. It is excreted unchanged by kidneys. T1/2 is 9-12 hours.

In case of impaired renal function the drug may be cumulated.

Indications

Diabetes mellitus type 2 without a tendency to ketoacidosis (especially in obese patients) with ineffective diet therapy; in combination with insulin – for type 2 diabetes mellitus, especially with severe obesity, accompanied by secondary insulin resistance.

Pharmacological effect

Metformin inhibits gluconeogenesis in the liver, reduces the absorption of glucose from the intestine, enhances peripheral glucose utilization, and also increases tissue sensitivity 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 due to the suppression of tissue-type plasminogen activator inhibitor.

PHARMACOKINETICS

After oral administration, metformin is absorbed from the gastrointestinal tract.

Bioavailability after taking a standard dose is 50-60%. Cmax in blood plasma is achieved 2.5 hours after oral administration.

Practically does not bind to plasma proteins. Accumulates in the salivary glands, muscles, liver and kidneys. It is excreted unchanged by the kidneys. T1/2 is 9-12 hours

In case of impaired renal function, accumulation of the drug is possible.

Special instructions

During treatment, it is necessary to monitor kidney function. At least 2 times a year, and also when myalgia appears, the lactate content in plasma should be determined. In addition, once every 6 months it is necessary to monitor the level of creatinine in the blood serum (especially in elderly patients). Metformin should not be prescribed if the blood creatinine level is above 135 µmol/L in men and 110 µmol/L in women.

It is possible to use the drug Metformin in combination with sulfonylurea derivatives. In this case, particularly careful monitoring of blood glucose levels is necessary.

Metformin should be stopped 48 hours before and 48 hours after X-ray contrast (urography, intravenous angiography).

If a patient develops a bronchopulmonary infection or an infectious disease of the genitourinary organs, you should immediately inform your doctor.

During treatment, you should refrain from drinking alcohol and medications containing ethanol. .

Impact on the ability to drive vehicles and operate machinery

The use of the drug in monotherapy does not affect the ability to drive vehicles or operate machinery.

When Metformin is combined with other hypoglycemic agents (sulfonylurea derivatives, insulin), hypoglycemic conditions may develop, which impair the ability to drive vehicles and engage in other potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Active ingredient

Metformin

Composition

Active ingredients:

metformin 1000 mg

Excipients:

povidone K 90;

cornstarch;

crospovidone;

magnesium stearate;

talc

Shell composition:

methacrylic acid and methyl methacrylate copolymer (eudragit L 100-55); macrogol 6000; titanium dioxide; talc

Contraindications

diabetic ketoacidosis, diabetic precoma, coma;
renal dysfunction;
acute diseases that occur with the risk of developing renal dysfunction: dehydration (with diarrhea, vomiting), fever, severe infectious diseases, hypoxia conditions (shock, sepsis, kidney infections, bronchopulmonary diseases);
clinically pronounced manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (heart or respiratory failure, acute myocardial infarction);
serious surgical operations and injuries (when insulin therapy is indicated);
liver dysfunction;
chronic alcoholism, acute alcohol poisoning;
use for at least 2 days before and for 2 days after radioisotope or x-ray studies with the introduction of an iodine-containing contrast agent;
lactic acidosis (including history);
following a hypocaloric diet (less than 1000 cal/day);
pregnancy;
lactation period;
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 digestive system: nausea, vomiting, metallic taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain. These symptoms occur especially often at the beginning of treatment and, as a rule, go away on their own. These symptoms can be reduced by the use of anthocides, atropine derivatives or antispasmodics.

Metabolic disorders: in rare cases – lactic acidosis (requires cessation of treatment); with long-term treatment – hypovitaminosis B12 (malabsorption).

From the hematopoietic organs: in some cases – megaloblastic anemia.

From the endocrine system: hypoglycemia.

Allergic reactions: skin rash.

Interaction

Concomitant use of danazol is not recommended to avoid the hyperglycemic effect of the latter. If treatment with danazol is necessary and after stopping the latter, dose adjustment of metformin and iodine monitoring of glycemic levels is required.

Combinations that require special caution: chlorpromazine – when taken in large doses (100 mg/day) increases glycemia, reducing insulin release.

When treated with antipsychotics and after stopping the latter, dose adjustment of metformin is required under the control of glycemic levels.

When used simultaneously with sulfonylurea derivatives, acarbose, insulin, NSAIDs, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate derivatives, cyclophosphamide, beta-blockers, the hypoglycemic effect of metformin may be enhanced.

When used simultaneously with corticosteroids, oral contraceptives, epinephrine, sympathomimetics, glucagon, thyroid hormones, thiazide and loop diuretics, phenothiazine derivatives, nicotinic acid derivatives, the hypoglycemic effect of metformin may be reduced.

Cimetidine slows down the elimination of metformin, thereby increasing the risk of developing lactic acidosis.

Metformin may weaken the effect of anticoagulants (coumarin derivatives).

Alcohol intake increases the risk of developing lactic acidosis during acute alcohol intoxication, especially in cases of fasting or following a low-calorie diet, as well as in liver failure.

Overdose

In case of an overdose of Metformin, the development of lactic acidosis with a fatal outcome is possible. The cause of lactic acidosis may also be the accumulation of the drug due to impaired renal function.

Symptoms of lactic acidosis: nausea, vomiting, diarrhea, low body temperature, abdominal pain, muscle pain, and further rapid breathing, dizziness, impaired consciousness and the development of coma may occur.

Treatment: 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 carried out.

When combined with Metformin and sulfonylureas, hypoglycemia may develop.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life

2 years

Manufacturer

Ozone/Ozone Pharm, Russia