METFORMIN

Active material: Metformin
When ATH: A10BA02
CCF: Oral hypoglycemic agents
When CSF: 15.02.02
Manufacturer: HEMOFARM A.D. (Serbia)

Pharmaceutical form, composition and packaging

Pills, enteric coated white, round, lenticular.

[Ring] povidone K90, corn starch, krospovydon, magnesium stearate, talc.

The composition of the shell: methacrylic acid and methyl methacrylate copolymer (jeudragit L 100-55), macrogol 6000, Titanium dioxide, talc.

10 PC. – blisters (3) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Oral gipoglikemicescoe means of a group of biguanide (dimetilbiguanid). The mechanism of action of metformin is linked to its ability to inhibit gluconeogenesis, as well as the formation of free fatty acids and fat oxidation. Metformin does not affect the amount of insulin in the blood, but changes its expense ratio decrease pharmacodynamic associated insulin to insulin ratios and increase to proinsulinu. An important link in the mechanism of action of metformin is the stimulation of glucose uptake into cells.

Metformin increases blood circulation in the liver and accelerates the process of transformation of glucose into glycogen. Lowers triglycerides, LDL, VLDL. Metformin improves fibrinoliticaskie properties of blood due to suppression of tissue-type plasminogen activator inhibitor.

Pharmacokinetics

Metformin absorbed from the digestive tract. C_max plasma is approximately 2 hours after ingestion. Through 6 h ends with the induction of the digestive tract and the concentration of metformin plasma is gradually decreasing.

Almost does not bind to plasma proteins. It accumulates in the salivary glands, liver and kidneys.

T_1/2 – 1.5-4.5 no. Report the news.

In the human kidney possible accumulation of metformin.

Testimony

Diabetes mellitus type 1 (insulin ) – (c) to reduce the need for insulin and prevent an increase in body mass index (as a supplement to insulinoterapii).

Diabetes mellitus type 2 (non-insulin ) in the case of a poor diet (especially with obesity).

Dosage regimen

Patients, not receiving insulin, first 3 day – by 500 mg 3 times / day, or 1 g 2 times per day during or after a meal. With the 4-th day 14 day – by 1 g 3 times / day. After 15-day dose govern according to the level of glucose in the blood and in urinary. The maintenance dose is 100-200 mg / day.

While applying insulin dose of less than 40 U/day dosing regimen of metformin is the same, When you do this, you can gradually reduce the dose of insulin (on 4-8 U/day through the day). If the patient receives more 40 U/d, the use of metformin and insulin dose reduction requires great care and is performed in a hospital.

Side effect

From the digestive system: possible (usually at the beginning of treatment) nausea, vomiting, diarrhea.

On the part of the endocrine system: gipoglikemiâ (mainly when used in inadequate doses).

Metabolism: in some cases – molernkisly acidosis (It requires discontinuation of treatment).

From the hematopoietic system: in some cases – megaloblastnaya anemia.

Contraindications

Expressed human liver and kidneys, cardiac and respiratory failure, acute phase of myocardial infarction, Saint Martin's evil, diabeticheskaya coma, Ketoacidosis, Lactic acidosis (incl. history), diabetic foot syndrome, pregnancy, lactation, hypersensitivity to metforminu.

Pregnancy and lactation

Is contraindicated in pregnancy and lactation.

Cautions

Not recommended for use in acute infections, exacerbation of chronic infectious and inflammatory diseases, injuries, acute surgical diseases, the danger of dehydration.

Do not use before surgery and during 2 days after the.

It is not recommended to use metformin in patients over 60 years and persons, performing heavy physical work, that is associated with an increased risk of molernkislogo azidoza.

During the period of treatment is necessary to monitor renal function; determination of lactate in plasma should be not less than 2 once a year, as well as on myalgia.

It is possible to use metformin in combination with derivative sulfonylureas. In this case a particularly careful monitoring of blood glucose levels.

Use metformin in combination therapy with insulin is recommended in the hospital.

Drug Interactions

While the use of sulfonylureas, akarʙozoj, insulinom, salicylates, MAO inhibitors, oxytetracycline, ACE inhibitors, with klofibratom, cyclophosphamide may increase the hypoglycemic action of metformin.

At simultaneous application with Valium, hormonal contraceptives for oral administration, adrenaline, glucagon, thyroid hormone, phenothiazine derivatives, thiazide diuretics, derived from Nicotinic Acid may reduce hypoglycemic action of metformin.

Simultaneous reception of cimetidine may increase the risk of developing lactic acidosis.