Metformin Canon, 850 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. It reduces the level of 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.

It is practically not bound to plasma proteins.

It accumulates in salivary glands, muscles, liver and kidneys. It is excreted unchanged by the kidneys. T1/2 is 9-12 hours. Cumulation of the drug is possible in impaired renal function.

Indications

Type 2 diabetes mellitus in adults (especially in patients with obesity) when diet therapy and physical activity are ineffective, 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:

Active ingredients:

metformin 850 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, the other hypoglycemic drug should be discontinued and Metformin Canon should be started at the above doses.
Combination therapy with insulin

The recommended initial 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

Metformin Canon is used in monotherapy and in combination therapy with insulin.
The recommended initial dose of the drug Metformin is 500 mg 1 time per day 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 in elderly patients
Because of possible decrease of renal function the dose of Metformin should be chosen under the regular control of renal function parameters (control of 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 drug without the guidance of the attending physician.

Interaction

Contraindicated combinations

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

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

Combinations requiring special caution
Simultaneous use of metformin with danazol may result in hyperglycemic effects. If treatment with danazolol is necessary and after discontinuation, 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 concentration, in some cases causing ketosis. If it is necessary to use such a combination and after discontinuation of GCS, metformin dose adjustment is required under control of blood glucose concentration.

In concomitant use of loop diuretics and metformin there is a risk of lactoacidosis due to possible functional renal failure.

The use of beta2-adrenomimetics in the form of injections decreases 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 the 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 reduced 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 heavy physical work, 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 lactocidosis are nausea, vomiting, diarrhea, decreased body temperature, abdominal pain, muscle pain; further on, rapid breathing, dizziness, impaired consciousness and development of coma may be noted.

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

Similarities