Metformin Long Canon sustained release pills 500mg, 60pcs

Composition

Tablets with prolonged release are white or almost white in color, oval, biconvex.

Auxiliary substances:

hypromellose 2208 (hydroxypropylmethylcellulose 2208),

hypromellose (hydroxypropylmethylcellulose) 2910,

colloidal silicon dioxide,

magnesium stearate,

microcrystalline cellulose.

Pharmacological action

Oral hypoglycemic agent from the biguanide group (dimethylbiguanide). The mechanism of action of metformin is related to its ability to inhibit gluconeogenesis, as well as the formation of free fatty acids and fat oxidation. Increases the sensitivity of peripheral insulin receptors and the utilization of glucose by cells. Metformin does not affect the amount of insulin in the blood, but changes its Pharmacodynamics by reducing the ratio of bound to free insulin and increasing the ratio of insulin to proinsulin.

Metformin stimulates glycogen synthesis by affecting glycogen synthetase. Increases the transport capacity of all types of membrane glucose transporters. Delays the absorption of glucose in the intestines.

Reduces the level of triglycerides, LDL, VLDL. Metformin improves the fibrinolytic properties of blood by suppressing the tissue-type plasminogen activator inhibitor.

While taking metformin, the patient’s body weight either remains stable or decreases moderately.

Pharmacokinetics

After oral use, metformin is slowly and incompletely absorbed from the gastrointestinal tract. Cmax in plasma is reached after approximately 2.5 hours. With a single dose of 500 mg, absolute bioavailability is 50-60%. With simultaneous food intake, the absorption of metformin decreases and is delayed.

Metformin is rapidly distributed to the body’s tissues. Practically does not bind to plasma proteins. It accumulates in the salivary glands, liver, and kidneys.

It is excreted unchanged by the kidneys. T1 / 2 from plasma is 2-6 hours.

Accumulation of metformin is possible in patients with impaired renal function.

Indications

Type 2 diabetes mellitus (non-insulin-dependent) with ineffectiveness of diet therapy and physical activity, in obese patients: in adults – as monotherapy or in combination with other oral hypoglycemic agents or with insulin;in children aged 10 years and older – as monotherapy or in combination with insulin.

Contraindications

Acute or chronic metabolic acidosis, diabetic ketoacidosis, diabetic precoma and coma; renal failure, impaired renal function (creatinine clearance less than 60 ml/min);dehydration, severe infection, hypoglycemic shock, which can lead to impaired renal function;clinically expressed symptoms of acute and chronic diseases that can lead to the development of tissue hypoxia (including heart failure, acute myocardial infarction, respiratory failure);use of the drug in patients with acute or chronic diseases, which can lead to the development of tissue hypoxia (including heart failure, acute myocardial infarction, respiratory failure). contrast iodine-containing substances for intravascular use (including during intravenous urography, intravenous cholangiography, angiography, CT); acute alcohol intoxication, chronic alcoholism;hypersensitivity to metformin.

Side effects

On the part of the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal discomfort are possible (usually at the beginning of treatment); in isolated cases – impaired liver function, hepatitis (disappear after stopping treatment).

From the side of metabolism: very rarely – lactate acidosis (discontinuation of treatment is required).

From the hematopoietic system: very rarely – malabsorption of vitamin B12.

The profile of adverse reactions in children aged 10 years and older is the same as in adults.

Interaction

Concomitant use with sulfonylurea derivatives, acarbose, insulin, salicylates, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate, cyclophosphamide may increase the hypoglycemic effect of metformin.

When used concomitantly with corticosteroids, oral contraceptives, danazol, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, thiazide diuretics, and nicotinic acid derivatives, the hypoglycemic effect of metformin may decrease.

In patients receiving metformin, the use of iodine-containing contrast agents for diagnostic studies (including intravenous urography, intravenous cholangiography, angiography, CT) increases the risk of acute renal failure and lactate acidosis. These combinations are contraindicated.

Beta-2-adrenomimetics in the form of injections increase the concentration of glucose in the blood due to stimulation of beta-2-adrenergic receptors. In this case, it is necessary to monitor the concentration of glucose in the blood. If necessary, it is recommended to prescribe insulin.

Concomitant use of cimetidine may increase the risk of developing lactic acidosis.

Concomitant use of loop diuretics may lead to the development of lactate acidosis due to possible functional renal failure.

When taken concomitantly with ethanol, the risk of developing lactate acidosis increases.

Nifedipine increases the absorption and Cmax of metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, and vancomycin) secreted in the renal tubules compete with metformin for tubular transport systems and can lead to an increase in its Cmax.

How to take, course of use and dosage

Take orally, during or after a meal.

The dose and frequency of use depends on the dosage form used.

With monotherapy, the initial single dose for adults is 500 mg, depending on the dosage form used, the frequency of use is 1-3 times/day. It is possible to use 850 mg 1-2 times/day. If necessary, the dose is gradually increased at intervals of 1 week. up to 2-3 g / day.

In monotherapy for children aged 10 years and older, the initial dose is 500 mg or 850 1 time/day or 500 mg 2 times/day. If necessary, with an interval of at least 1 week, the dose can be increased to a maximum of 2 g / day in 2-3 doses.

After 10-15 days, the dose should be adjusted based on the results of blood glucose determination.

In combination therapy with insulin, the initial dose of metformin is 500-850 mg 2-3 times a day. The dose of insulin is selected based on the results of blood glucose determination.

Special instructions

It is not recommended for use in acute infections, exacerbation of chronic infectious and inflammatory diseases, injuries, acute surgical diseases, and the risk of dehydration.

Do not apply before surgical operations and within 2 days after they are performed.

Metformin should be used with caution in elderly patients and those who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis. Senile patients often have asymptomatic renal dysfunction. Special care is required if renal dysfunction is caused by taking antihypertensive drugs or diuretics, as well as NSAIDs.

If during treatment the patient has muscle cramps, digestive disorders (abdominal pain) and severe asthenia, then it should be borne in mind that these symptoms may indicate the beginning of lactic acidosis.

During treatment, it is necessary to monitor renal function; determination of the content of lactate in plasma should be carried out at least 2 times a year, as well as when myalgia occurs.

When metformin is used as monotherapy in accordance with the dosage regimen, hypoglycemia usually does not occur. However, when combined with insulin or with sulfonylureas, there is a risk of hypoglycemia. In such cases, especially careful monitoring of the concentration of glucose in the blood is necessary.

During treatment, patients should avoid alcohol consumption due to the risk of developing lactate acidosis.

Preclinical studies have shown that metformin has no carcinogenic potential.

Active ingredient

Metformin

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets