Gliklazid-AKOS

General characteristics. Structure:

Active agent: Gliclazide - 0,08 g. Excipients: starch corn, calcium stearate, talc.

Pharmacological properties:

Gliklazid-AKOS is the peroral hypoglycemic drug derivative of generation sulphonylurea II. Stimulates insulin secretion with pancreas b-cells, strengthens insulinosekretorny effect of glucose, increases sensitivity of peripheral fabrics to insulin. Stimulates activity of desmoenzymes - a muscular glikogensintetaza. Reduces a span from the meal moment prior to insulin secretion. Recovers early peak of secretion of insulin (unlike other derivatives of sulphonylurea which make impact, mainly, during the second stage of secretion). Reduces postprandialny peak of a hyperglycemia. In addition to influence on carbohydrate metabolism, improves microcirculation: reduces adhesion and aggregation of thrombocytes, normalizes permeability of vessels, interferes with development of microthrombosis and atherosclerosis, recovers process of a physiological pristenochny fibrinolysis. Reduces sensitivity of receptors of vessels to adrenaline. Slows down development of a diabetic retinopathy at not proliferative stage. At a diabetic nephropathy against the background of prolonged use causes reliable decrease in a proteinuria. Does not lead to increase in body weight as makes preferential impact on early peak of secretion of insulin and does not cause a giperinsulinemiya; promotes decrease in body weight at patients with obesity at observance of the corresponding diet.

Pharmacokinetics. After intake it is quickly soaked up in digestive tract. Absorption - high. After oral administration of 80 mg the maximum concentration in blood is reached approximately in 4 hours, the size of the maximum concentration - 2,2-8 mkg/ml; after reception of 40 mg - 2-3 h and 2-3 mkg/ml respectively. Communication with proteins of plasma - 85-97%, distribution volume - 0,35 l/kg. Equilibrium concentration in blood is reached in 2 days. It is metabolized in a liver, at the same time 8 metabolites are formed. The quantity of the main metabolite which is found in blood makes 2-3% of all amount of the accepted drug, it has no hypoglycemic effect, however improves microcirculation. It is removed by kidneys - 70% in the form of metabolites, less than 1% in not changed look; with a fecal masses - 12% in the form of metabolites. The elimination half-life makes 8-20 hours.

Indications to use:

Diabetes mellitus of type 2 (non-insulin-dependent) in combination with a dietotherapy and a moderate exercise stress at inefficiency of the last.

Route of administration and doses:

The dose of drug is established individually, depending on age of the patient, clinical displays of a disease and level of a glycemia on an empty stomach and in 2 hours after food. An initial daily dose - 80 mg, an average daily dose - 160 mg, the maximum daily dose - 320 mg. Gliklazid-AKOS accept inside 2 times a day (in the morning and in the evening) in 30-60 minutes prior to food.

Features of use:

Gliclazide is applied to treatment of a non-insulin-dependent diabetes mellitus in combination with a low-calorie diet with the small content of carbohydrates.

During treatment it is regularly necessary to control glucose level in blood on an empty stomach and after meal, daily fluctuations of level of glucose.

In case of surgical interventions or a decompensation of a diabetes mellitus it is necessary to consider a possibility of use of drugs of insulin.

At development of a hypoglycemia if the patient is in consciousness, glucose (or sugar solution) is appointed inside. At a loss of consciousness enter glucose in/in or a glucagon п / to, in oil or in / century. After recovery of consciousness it is necessary to give to the patient food, carbohydrate-rich, in order to avoid repeated development of a hypoglycemia.

At simultaneous use of gliclazide with verapamil regular control of level of glucose in blood is necessary; with acarbose - careful monitoring and correction of the mode of dosing of hypoglycemic means is required.

Simultaneous use of gliclazide and Cimetidinum is not recommended.

Side effects:

From the alimentary system: seldom - anorexia, nausea, vomiting, diarrhea, pains in epigastriums.

From system of a hemopoiesis: in some cases - thrombocytopenia, an agranulocytosis or a leukopenia, anemia (as a rule, reversible character).

From endocrine system: at overdose - a hypoglycemia.

Allergic reactions: skin rash, itch.

Interaction with other medicines:

Hypoglycemic effect of gliclazide is exponentiated at simultaneous use with pyrazyl ketone derivatives, salicylates, phenylbutazone, antibacterial sulfanamide drugs, theophylline, caffeine, MAO inhibitors.

Simultaneous use with non-selective beta adrenoblockers increases probability of development of a hypoglycemia, and also can mask the tachycardia and a tremor of hands characteristic of a hypoglycemia, perspiration at the same time can amplify.

At simultaneous use of gliclazide and acarbose the additive hypoglycemic effect is observed.

Cimetidinum increases concentration of gliclazide in plasma that can cause a heavy hypoglycemia (oppression of TsNS, consciousness disturbance).

At simultaneous use with GKS (including dosage forms for external use), the diuretics, barbiturates, estrogen, progestins combined it is oestrogenic-gestagennymi drugs, dipheninum, rifampicin hypoglycemic effect of gliclazide decreases.

Contraindications:

Hypersensitivity to drug. - Diabetes mellitus of type 1 (insulin-dependent).-Diabetic ketoacidosis, diabetic prekoma and coma. - Giperosmolyarny coma. - Heavy liver and/or renal failure. - Big surgical interventions, extensive burns. - Intestinal impassability, stomach paresis. - The states which are followed by disturbance of absorption of food, development of a hypoglycemia (infectious diseases).-Leukopenia. - Pregnancy, breastfeeding period. With care appoint Gliklazid-AKOS at a feverish syndrome, alcoholism, diseases of a thyroid gland (with disturbance of its function). 
Use at pregnancy is not specified.

Storage conditions:

List B. In dry, protected from light and the place, unavailable to children, at a temperature from 8 to 15 °C. 
Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 80 mg: 20, 40, 60 or 100 pieces.