Metformin, tablets 850 mg 60 pcs

Metformin inhibits gluconeogenesis in liver, decreases glucose absorption from intestine, increases peripheral glucose utilization, and increases tissue sensitivity to insulin. At the same time it has no effect on insulin secretion by the beta cells of the pancreas and does not cause hypoglycemic reactions.

Limits triglycerides and low-density linoproteins in the blood. Stabilizes or reduces body weight. Has a fibrinolytic effect by inhibiting tissue-type plasminogen activator inhibitor.

After oral administration metformin is absorbed from the gastrointestinal tract. Bioavailability after a standard dose is 50-60%. Cmax in plasma is reached 2.5 hours after oral administration. Practically does not bind with plasma proteins. It accumulates in salivary glands, muscles, liver and kidneys.

Indications

Type 2 diabetes mellitus in adults (especially in patients with obesity) with ineffectiveness of diet therapy and physical activity, as monotherapy or in combination with other oral hypoglycemic agents or insulin.

Type 2 diabetes mellitus in children from the age of 10 years – both as monotherapy and in combination with insulin.

Active ingredient

Composition

1 tablet contains:

The active ingredients:

metformin 850 mg

Excipients:

Povidone K-30 59.5 mg;

Magnesium stearate 8.5 mg.

Composition of the film coating (white to almost white film coating mixture “Vivacote PC-1P-058”) 27.2 including.Including: Hypromellose 16.32 mg; Talc 5.44 mg; Titanium dioxide 2.992 mg; MacroGol 4000 (polyethylene glycol 4000) 2.448 mg.

How to take, the dosage

The tablets should be taken orally, swallowed whole, without chewing, during or immediately after a meal, with plenty of water.

Adults

Monotherapy and combination therapy with other oral hypoglycemic agents

The recommended starting dose is 1000-1500 mg/day. The dose should be divided into 2-3 doses to reduce gastrointestinal side effects. In 10-15 days in absence of gastrointestinal adverse effects further gradual dose increase depending on blood glucose concentration is possible. Slow increase in dose may improve gastrointestinal tolerance of the drug.

The maintenance daily dose is 1500-2000 mg. The maximum daily dose is 3000 mg divided into 3 doses.

If planning to switch from another oral hypoglycemic drug to Metformin, discontinue the other hypoglycemic drug and start Metformin Canon at the above doses.

Combination therapy with insulin

The recommended starting dose of Metformin 500 mg and 850 mg is 1 tablet 2-3 times daily; Metformin 1000 mg is 1 tablet once daily; the dose of insulin is adjusted on the basis of blood glucose values.

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 daily in the evening with a meal. After 10-15 days the dose of the drug should be adjusted on the basis of blood glucose concentration. The maintenance dose is 1000-1500 mg/day in 2-3 doses. The maximum daily dose is 2000 mg in 3 doses.

Patients of Elderly People

Because of possible decrease of renal function, Metformin dose should be adjusted with regular control of renal function parameters (serum creatinine concentration control at least 2-4 times per year).
The duration of treatment is determined by the doctor. It is not recommended to interrupt the drug without the guidance of the attending physician.

Interaction

Contraindicated combinations

Radiological studies with the use of iodine-containing radiopaque agents may cause lactoacidosis in diabetic patients with functional renal insufficiency. Metformin administration should be discontinued 48 hours before and not resumed until 48 hours after radiological examination with contrast agents.

Unrecommended combinations

The simultaneous use of metformin with alcohol and ethanol-containing drugs, during acute alcohol intoxication, when fasting or following a low-calorie diet, as well as liver failure increases the risk of lactoacidosis.

Combinations requiring special caution

The simultaneous use of metformin with danazol may result in hyperglycemic effects. If treatment with danazolol is necessary and after discontinuation of danazolol, metformin dose adjustment is required with monitoring of blood glucose concentrations.

Chlorpromazine at high doses (100 mg/day) decreases insulin release and increases blood glucose concentrations. When concomitant use with neuroleptics and after discontinuation of their use, correction of metformin dose is required under control of blood glucose concentration.

Glucocorticosteroids (GCS) when used parenterally and topically decrease glucose tolerance and increase blood glucose concentrations, in some cases causing ketosis.

If this combination is necessary and after discontinuation of GCS, metformin dose adjustment is required with control of blood glucose concentration.
Simultaneous use of loop diuretics and metformin carries a risk of lactoacidosis due to possible functional renal failure.

The use of beta2-adrenomimetics in the form of injections reduces the hypoglycemic effect of metformin due to stimulation of beta2-adrenoreceptors. In this case, blood glucose concentration should be monitored and insulin should be used if necessary.

Angiotensin-converting enzyme inhibitors and other antihypertensive drugs may decrease blood glucose concentration. If necessary, the dose of metformin should be adjusted.

Concomitant use of metformin with sulfonylurea derivatives, insulin, acarbose and salicylates may increase the hypoglycemic effect.

Nifedipine increases absorption and Cmax of metformin, which should be considered when using them concomitantly.

“Loop” diuretics and nonsteroidal anti-inflammatory drugs (NSAIDs) increase the risk of decreased renal function. In this case, caution should be exercised when using metformin.

Special Instructions

Key kidney function should be monitored during treatment. Plasma lactate should be determined at least twice a year, as well as in case of myalgia. In addition, serum creatinine level should be controlled once every 6 months (especially in elderly patients). Metformin should not be prescribed if blood creatinine level is higher than 135 μmol/l in men and 110 μmol/l in women.

Metformin may be used in combination with sulfonylurea derivatives. In this case, particularly careful monitoring of blood glucose levels is necessary.

For 48 hours before and for 48 hours after X-ray contrast (urography, IV angiography), Metformin should be discontinued.

If a patient has a bronchopulmonary infection or a urinary tract infection, the attending physician should be informed immediately.

Alcohol and medications containing ethanol should be avoided during treatment.

Influence on driving and operating machinery

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

When combining Metformin with other hypoglycemic agents (sulfonylurea derivatives, insulin) hypoglycemic states may occur, which impair the ability to drive vehicles and engage in other potentially dangerous activities that require increased attention and quick psychomotor reactions.

Contraindications

The drug is not recommended for persons older than 60 years of age who perform strenuous physical labor, due to the increased risk of lactic acidosis in them.

Side effects

Gastrointestinal system disorders: nausea, vomiting, metallic taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain. These symptoms are especially common at the beginning of treatment and usually go away on their own. These symptoms may be reduced by administration of antacids, atropine derivatives, or antispasmodics.

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

Hematopoietic organs: in rare cases – megaloblastic anemia.

Endocrine system: hypoglycemia.

Allergic reactions: skin rash.

Overdose

Symptoms: when using metformin at a dose of 85 g, no hypoglycemia was observed, but the development of lactoacidosis was noted. Early symptoms of lactoacidosis are nausea, vomiting, diarrhea, decreased body temperature, abdominal pain, muscle pain; later there may be rapid breathing, dizziness, impaired consciousness and development of coma.

Treatment: If signs of lactocidosis occur the drug treatment should be stopped immediately, the patient should be urgently hospitalized and after determining the lactate concentration the diagnosis should be specified. The most effective measure for lactate and metformin elimination from the body is hemodialysis. Symptomatic treatment is also carried out.

Similarities