Metformin-Canon - instructions for use, dose, side effects, contraindications

Composition:Dosage 500 mg
1 tablet, film-coated, contains: active substance: metformin hydrochloride 500 mg;
auxiliary substances: pregelatinized starch 27 mg, sodium carboxymethyl starch 8 mg, sodium stearyl fumarate 3 mg, povidone 47 mg, talc 3 mg, macrogol (polyethylene glycol 6000) 12 mg; the composition of the film shell: Opadrai II white 18 mg, including: polyvinyl alcohol 8.442 mg, macrogol (polyethylene glycol) 4.248 mg, titanium dioxide 2.178 mg, talc 3.132 mg.
The dosage of 850 mg
1 tablet, film-coated, contains: active substance: metformin hydrochloride 850 mg; auxiliary substances: pregelatinized starch 45.9 mg, sodium carboxymethyl starch (primogel) 13.6 mg, sodium stearyl fumarate 5.1 mg, povidone 79.9 mg, talc 5.1 mg,macrogol (polyethylene glycol 6000) 20.4 mg; composition of the film shell: Opadrai II white 30 mg, including: polyvinyl alcohol 14.07 mg, macrogol (polyethylene glycol) 7.08 mg, titanium dioxide 3.63 mg, talc 5.22 mg.
Dosage of 1000 mg
1 tablet, film-coated, contains: active substance: metformin hydrochloride 1000 mg; auxiliary substances: pregelatinized starch 54 mg, sodium carboxymethyl starch (primogel) 16 mg, sodium stearyl fumarate 6 mg, povidone 94 mg, talc 6 mg, macrogol (polyethylene glycol 6000) 24 mg; composition of the film shell: Opadrai 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.

Description:Dosage 500 mg: Tablets are round, biconvex, covered with a film coat of white or almost white color. On a cross-section of white or almost white color.
Dosage of 850 mg and 1000 mg: Tablets are oval, biconcave, covered with a film coat of white or almost white color. On a cross-section of white or almost white color.

Pharmacotherapeutic group:Hypoglycemic agent of the biguanide group for oral administration.

ATX: & nbsp

A.10.B.A.02 Metformin

Pharmacodynamics:Metformin - oral hypoglycemic agent from the biguanide group. In patients with diabetes mellitus, it reduces the concentration of glucose in the blood by suppressing 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 (predominantly striated muscle, to a lesser extent - fat tissue). Stimulates intracellular glycogenesis, activating glycogen synthase. Unlike derivatives of sulfonylureas, it does not stimulate insulin secretion and does not have a hypoglycemic effect in healthy individuals. Has an effect on lipid metabolism - reduces the concentration in the blood serum of triglycerides, cholesterol and low density lipoproteins. Stabilizes or reduces body weight. Has a fibrinolytic effect due to inhibition of the inhibitor of tissue-type plasminogen activator.

Pharmacokinetics:After oral administration, the absorption of metformin from the gastrointestinal tract is 48-52%. With simultaneous intake of food, absorption of metformin is reduced and delayed. Absolute bioavailability is 50-60%.The maximum concentration in the blood (Cmax) is 2 μg / ml, the time to reach the maximum concentration (TCmax) is 1.81-2.69 h. Metformin quickly distributed into tissues. Penetrates into 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 connection with plasma proteins is insignificant. Exposed to a very weak degree of metabolism. It is excreted by the kidneys, mostly unchanged. The clearance of metformin in healthy individuals is 400 ml / min. The half-life period (T1 / 2) is 6.2 hours (the initial T1 / 2 is from 1.7 to 3 hours, the terminal one is from 9 to 17 hours). With renal insufficiency, it increases, there is a risk of cumulation of the drug.

Indications:Diabetes mellitus type 2 in adults (especially in obese patients) with ineffectiveness of diet and exercise, as a monotherapy or in combination with other oral hypoglycemic agents or insulin. Diabetes mellitus type 2 in children from 10 years of age - both as a monotherapy, and in combination with insulin.

Contraindications:- Hypersensitivity to metformin or to any auxiliary substance.
- Diabetic ketoacidosis, diabetic precoma, coma.
- Renal failure or renal dysfunction (creatinine clearance (CC) less than 60 ml / min).
- Acute conditions that occur with a risk of developing renal dysfunction:
- dehydration (with diarrhea, vomiting), fever, severe infectious diseases,
- the state of hypoxia (shock, sepsis, kidney infections, bronchopulmonary diseases).
- Clinically expressed manifestations of acute and chronic diseases, which can lead to the development of tissue hypoxia (including - cardiac or respiratory failure, acute myocardial infarction).
- Extensive surgery and trauma, when insulin therapy is indicated (see section "Special instructions").
- Hepatic failure, a violation of the liver.
- Chronic alcoholism, acute alcohol poisoning.
- Lactic acidosis, including, in the anamnesis.
- Use for at least 48 hours before and 48 hours after carrying out radioisotope or radiographic studies with the introduction of iodine-containing contrast medium (see section "Interaction with other drugs").
- Period not less than 48 hours before and 48 hours after surgery under general anesthesia, spinal or epidural anesthesia.
- Compliance with a hypocaloric diet (less than 1000 kcal / day).
- Children under 10 years old.

Carefully:In persons over the age of 60, performing heavy physical work (increased risk of lactic acidosis).

Pregnancy and lactation:The drug is contraindicated for use during pregnancy and during breastfeeding.
When planning or developing a pregnancy, Metformin canon should be discontinued and insulin therapy applied. The patient should be warned about the need to inform the doctor if a pregnancy occurs. Mother and child should be monitored.
It is not known whether metformin with breast milk. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:Tablets should be taken orally, swallowing whole, without chewing, during or immediately after eating, with plenty of water.
Adults
Monotherapy and combination therapy with other oral hypoglycemic agents
The recommended initial dose is 1000-1500 mg / day. To reduce side effects from the GIT, the dose should be divided into 2-3 doses.After 10-15 days in the absence of adverse effects on the part of the gastrointestinal tract, a further gradual increase in the dose, depending on the concentration of glucose in the blood, is possible. A slow increase in the dose may help 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 the transition from taking another oral hypoglycemic agent to Metformin canon, stop taking another hypoglycemic agent and start taking Metformin Kanon in the above doses.
Combination therapy with insulin
Recommended initial dose of the drug Metformin Canon 500 mg and 850 mg - 1 tablet 2-3 times a day, Metformin Kanon 1000 mg - 1 tablet 1 time per day, the dose of insulin is selected on the basis of blood glucose concentrations.
Children over 10 years old
Metformin canon is used in monotherapy and in combination therapy with insulin.
The recommended initial dose of the drug Metformin Canon is 500 mg 1 time per 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 doses.The maximum daily dose is 2000 mg in 3 divided doses.
Elderly patients
Because of a possible reduction in renal function, the dose of Metformin canon should be selected under regular monitoring of renal function indicators, (monitoring serum creatinine concentration at least 2-4 times per year).
The duration of treatment is determined by the doctor. It is not recommended to interrupt the use of the drug without the indication of the attending physician.

Side effects:From the central nervous system: a taste disorder ("metallic" taste in the mouth).
From the digestive tract: nausea, vomiting, diarrhea, abdominal pain and lack of appetite.
The occurrence of these side effects is most likely in the initial treatment period and in. In most cases, they spontaneously pass. To prevent symptoms, it is recommended to take metformin during or after a meal. Slow increase in dose may improve gastrointestinal tolerance.
From the hepatobiliary system: violation of liver function, hepatitis. After the withdrawal of metformin, undesirable phenomena, as a rule, completely disappear.
Allergic reactions: very rarely - erythema, itching, rash, hives.
From the side of metabolism: very rarely - lactic acidosis (requires withdrawal of the drug).
Other: very rarely - with prolonged use develops hypovitaminosis B12 (including megaloblastic anemia) and folic acid (impaired absorption). Published data show that in a limited child population aged 10 to 16 years, side effects by nature and severity are similar to those in adult patients.

Overdose:Symptoms: when metformin was used at a dose of 85 g, hypoglycemia was not observed, but lactoacidosis was noted. The early symptoms of lactic acidosis are nausea, vomiting, diarrhea, lower body temperature, abdominal pain, muscle pain, there may be more rapid breathing, dizziness, impaired consciousness and coma development.
Treatment: If signs of lactic acidosis drug treatment must be stopped immediately, the patient hospitalized immediately and determine the concentration of lactate, clarify the diagnosis. The most effective measure for excretion from the body of lactate and metformin is hemodialysis. Conduct also symptomatic treatment.

Interaction:Contraindicated combinations
Radiological studies using iodine-containing radiocontrast preparations can cause the development of lactic acidosis in diabetic patients on the background of functional renal failure. The use of metformin should be discontinued 48 hours before and not resumed earlier 48 hours after radiologic examination using radiopaque preparations.
Unrecommended combinations
With the simultaneous 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, the risk of developing lactic acidosis increases.
Combinations requiring special care
With the simultaneous use of metformin with danazol may develop a hyperglycemic effect. If it is necessary to treat danazol and after stopping its intake, a dose adjustment of metformin is required under the control of the glucose concentration in the blood.
Chlorpromazine in high doses (100 mg / day) reduces the release of insulin and increases the concentration of glucose in the blood.When used simultaneously with neuroleptics and after stopping their intake, a dose adjustment of metformin is required under the control of the glucose concentration in the blood.
Glucocorticosteroids (GCS) for parenteral and topical application reduce glucose tolerance and increase the concentration of glucose in the blood, in some cases, causing ketosis. If it is necessary to use this combination, and after stopping the GCS, correction of the dose of metformin is required under the control of the glucose concentration in the blood.
With the simultaneous use of "loop" diuretics and metformin, there is a risk of lactic acidosis because of the possible emergence of functional renal failure.
The use of beta2-adrenomimetics as injections reduces the hypoglycemic effect of metformin due to stimulation of beta2-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 drugs can reduce the concentration of glucose in the blood. If necessary, the dose of metformin should be adjusted.
With the simultaneous use of metformin with derivatives of sulfonylurea, insulin, acarbose and salicylates, an increase in hypoglycemic effect is possible. Nifedipine increases the absorption and C max of metformin, which must be taken into account when they are used simultaneously.
"Loopback" diuretics and non-steroidal anti-inflammatory drugs (NSAIDs) increase the risk of decreased kidney function. In this case, care must be taken when applying metformin.

Special instructions:During the treatment with metformin it is necessary to regularly monitor the concentration of glucose in the blood on an empty stomach and after eating.
The patient should be warned about the need to stop taking the drug and see a doctor if there is vomiting, abdominal pain, muscle pain, general weakness and severe malaise. These symptoms can be a sign of beginning lactic acidosis.
Metformin should be discontinued 48 hours before and 48 hours after the X-ray examination (including urography, intravenous angiography) using radiopaque preparations.
Because the metformin is excreted by the kidneys, before the start of treatment and regularly in the subsequent it is necessary to determine the concentration of creatinine:patients with preserved kidney function 1 time per year; in patients with reduced QC and in elderly patients -2-4 times a year.
Particular caution should be exercised in cases of impaired renal function, for example, during the initial period of therapy with antihypertensive agents, diuretics, NSAIDs. It is necessary to inform the patient about the need to consult a doctor if symptoms of bronchopulmonary infection or infectious disease of the genito-urinary organs appear.
Against the background of metformin should refrain from taking alcohol because of the increased risk of hypoglycemia and disulfiramoid-like effect. Hypovitaminosis B12 with metformin is caused by a violation of absorption and has a reversible character. With the withdrawal of the drug signs of hypovitaminosis B12 quickly disappear.

Effect on the ability to drive transp. cf. and fur:Monotherapy with metformin does not cause hypoglycemia and therefore does not affect the ability to drive vehicles and work with mechanisms.
When metformin is used with other hypoglycemic agents (derivatives of sulfonylureas, - insulin, etc.), hypoglycemic conditions may develop,at which the ability to drive vehicles and engage in other potentially hazardous activities that require increased attention and rapid psychomotor reactions deteriorates.

Form release / dosage:Tablets, film-coated 500 mg, 850 mg, 1000 mg.

Packaging:For tablets with a dosage of 500 mg:
For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
By 3, 5, 6, 10, 12 contour cell packs of 10 tablets or 2, 4, 8 contour cell packs of 15 tablets together with the instruction for use are placed in a pack of cardboard for consumer containers.
For tablets with a dosage of 850 mg and 1000 mg:
For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
By 3, 5, 6, 10, 12 contour mesh packages together with the instruction for use are placed in a pack of cardboard for consumer containers.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001724

Date of registration:02.07.2012 / 27.05.2015

Expiration Date:02.07.2017

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

NGO Farmvilar, OOO Russia

Information update date: & nbsp2016-09-24

Illustrated instructions

Instructions

Metformin-Canon (Metformin-Canon)