Metformin Canon pills 1000mg, 30pcs

Composition

of 1 tab. :

– Metformin hydrochloride 1000 mg;

excipients:

pregelatinized starch 78 mg,

sodium carboxymethyl starch (primogel) 16 mg,

sodium stearyl fumarate 6 mg,

povidone 94 mg, talc 6 mg;

composition of the film shell:

Opadray II white 36 mg, including: polyvinyl alcohol 16,884 mg, macrogol (polyethylene glycol) 8,496 mg, titanium dioxide 4,356 mg, talc 6,264 mg

Pharmacological action

Pharmaceutical group:

hypoglycemic agent of the biguanide group for oral use.

Pharmaceutical action:  

Metformin is an oral hypoglycemic agent from the biguanide group. In patients with diabetes mellitus, it reduces the concentration of glucose in the blood by inhibiting gluconeogenesis in the liver, reducing the absorption of glucose from the gastrointestinal tract (GIT) and increasing its utilization in tissues by increasing their sensitivity to insulin (mainly striated muscles, to a lesser extent-adipose tissue). It stimulates intracellular glycogenesis by activating glycogen synthase.

Unlike sulfonylurea derivatives, it does not stimulate insulin secretion and does not have a hypoglycemic effect in healthy individuals. It has an effect on lipid metabolism-reduces the concentration of triglycerides, cholesterol and low-density lipoproteins in the blood serum. Stabilizes or reduces body weight. It has a fibrinolytic effect by suppressing the tissue-type plasminogen activator inhibitor.

Pharmacokinetics:

After oral use, metformin absorption from the gastrointestinal tract is 48-52%. With simultaneous food intake, the absorption of metformin decreases and is delayed. Absolute bioavailability is 50-60%. The maximum concentration in the blood (Cmax) is 2 micrograms / ml, the time to reach the maximum concentration (TCmax) is 1.81-2.69 hours.

Metformin is rapidly distributed in the tissue. Penetrates red blood cells. It accumulates in the salivary glands, liver, and kidneys. The volume of distribution (for a dose of 850 mg) is 296-1012 liters. The association with plasma proteins is insignificant. It is metabolized to a very weak degree.

It is excreted by the kidneys, mainly in unchanged form. The clearance of metformin in healthy individuals is 400 ml/min. The half-life (T1 / 2) is 6.2 hours (initial T1/2 – from 1.7 to 3 hours, terminal-from 9 to 17 hours). With renal failure, it increases, there is a risk of accumulation of the drug.

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

-Hypersensitivity to metformin or to any excipient of the drug Metformin Canon. – Diabetic ketoacidosis, diabetic precoma, coma. – Renal insufficiency or impaired renal function (creatinine clearance (CC) less than 60 ml / min). – Acute conditions with a risk of developing impaired renal function: – dehydration (with diarrhea, vomiting), fever, severe infectious diseases, – hypoxia (shock, sepsis, kidney infections, bronchopulmonary diseases). – Clinically expressed manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (including heart or respiratory failure, acute myocardial infarction). – Extensive surgical operations and injuries, when insulin therapy is indicated (see the section “Special instructions”). – Hepatic insufficiency, impaired liver function. – Chronic alcoholism, acute alcohol poisoning. – Lactic acidosis, including in the anamnesis. – Use for at least 48 hours before and 48 hours after conducting radioisotope or X-ray studies with the introduction of an iodine-containing contrast agent (see the section “Interaction with other drugs”). – A period of at least 48 hours before and 48 hours after surgery under general anesthesia, spinal or peridural anesthesia. – Compliance with a hypocaloric diet (less than 1000 kcal / day). – Children under 10 years of age.

With caution: In people over the age of 60 who perform heavy physical work (increased risk of lactic acidosis).

Side effects

From the central nervous system: taste disorder (“metallic” taste in the mouth).

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain and lack of appetite.

The occurrence of these side effects is most likely during the initial period of treatment and in most cases they disappear spontaneously. To prevent symptoms, it is recommended to take metformin during or after a meal. Slowly increasing the dose may improve gastrointestinal tolerance.

From the side of the hepatobiliary system: impaired liver function, hepatitis. After discontinuation of metformin, adverse events usually disappear completely.

Allergic reactions: very rare – erythema, pruritus, rash, urticaria.

From the side of metabolism: very rarely – lactic acidosis (requires discontinuation of the drug).

Other: very rare-with prolonged use, hypovitaminosis of B12 (including megaloblastic anemia) and folic acid (malabsorption) develops.

Published data show that in a limited population of children aged 10 to 16 years, side effects are similar in nature and severity to those in adult patients.

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:

With the simultaneous use of metformin with danazol, 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 it, 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.

Adults:

Monotherapy 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 Canon, 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 Canon is 500 mg and 850 mg – 1 tablet 2-3 times a day, Metformin Canon 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 Canon 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 Canon 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 with metformin, it is necessary to regularly monitor the concentration of glucose in the blood on an empty stomach and after meals. The patient should be warned to stop taking the drug and consult a doctor if vomiting, abdominal pain, muscle pain, general weakness or severe malaise occur. These symptoms may be a sign of incipient lactic acidosis.

Metformin should be discontinued 48 hours before and 48 hours after X-ray examination (including urography, intravenous angiography) using radiopaque drugs.

Since metformin is excreted by the kidneys, the creatinine concentration should be determined before starting treatment and regularly thereafter: in patients with preserved renal function 1 time a year; in patients with reduced creatinine clearance and in elderly patients – 2-4 times a year.

Special care should be taken when renal function is impaired, for example, during the initial period of therapy with antihypertensive agents, diuretics, NSAIDs.

The patient should be informed about the need to consult a doctor if symptoms of a bronchopulmonary infection or an infectious disease of the genitourinary organs appear.

When using metformin, you should refrain from taking alcohol due to the increased risk of hypoglycemia and disulfiram-like effect.

Hypovitaminosis B12 when taking metformin is caused by malabsorption and is reversible. When the drug is discontinued, the signs of B12 hypovitaminosis quickly disappear.

Influence on the ability to drive vehicles and mechanisms:

Metformin monotherapy does not cause hypoglycemia and therefore does not affect the ability to drive vehicles and work with mechanisms.

When using metformin with other hypoglycemic agents (sulfonylurea derivatives, insulin, etc. ), 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