Included in the formulation
АТХ:A.10.B.D.02 Metformin and sulfonamides
Pharmacodynamics:Combined anti-glycemic agent.
Gliclazide
The sulfonylurea compound II generation, by reducing the threshold of stimulation of pancreatic β-cells by glucose stimulates the secretion of insulin, increases its release and the degree of binding to target cells. The hypoglycemic effect depends on the number of functioning β-cells.
Suppresses platelet aggregation, has fibrinolytic, hypolipidemic and weak diuretic action.
Metformin
Reduces the absorption of glucose from the intestine and enhances its peripheral utilization, increasing the sensitivity of tissues to insulin, inhibits gluconeogenesis in the liver. Reduces the level of low density lipoproteins and triglycerides in blood plasma. Does not cause hypoglycemic reactions, does not affect the secretion of insulin β-cells of the pancreas. By suppressing the inhibitor of the tissue plasminogen activator, it has a fibrinolytic effect. Stabilizes or reduces body weight.
Pharmacokinetics:Gliclazide
After oral intake absorbed in the gastrointestinal tract by 90%.The maximum concentration in the blood plasma is achieved after 3 hours. The connection with plasma proteins is 98-99%.
The therapeutic effect develops 10-30 minutes after the beginning of the admission. Metabolism in the liver.
The half-life is 8-12 hours. Elimination by the kidneys: 90% in the form of metabolites, 10% in unchanged form.
Metformin
After oral administration, up to 50-60% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 2.5 hours. Does not bind to plasma proteins.
It accumulates in muscle tissue, salivary glands, kidneys and liver.
Half-life is 6 hours. Elimination of the kidneys unchanged.
Indications:It is used for the treatment of diabetes mellitus II type in the absence of the effect of diet therapy.
IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus
Contraindications:Diabetes I type (insulin-dependent), coma, ketoacidosis, individual intolerance, children under 18 years of age.
Carefully:Concomitant diseases of the endocrine system affecting carbohydrate metabolism: adenohypophysis and adrenocortical insufficiency, dysfunction of the thyroid gland.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside with eating 1-2 tablets 3 times a day.
The highest daily dose: 4 tablets 5/500 mg or 6 tablets 2.5 / 500 mg.
The highest single dose: 5/500 mg.
Side effects:Central and peripheral nervous system: insomnia, paresthesia, emotional lability.
The cardiovascular system: tachycardia.
Digestive system: loss of appetite, constipation, sometimes - exacerbation of hemorrhoids.
Muscular system: symptoms of lactic acidosis - cramps of the calf muscles.
Allergic reactions.
Overdose:Development of hypoglycemia.
Treatment: sugar inside, with loss of consciousness - intravenous injection of 40% dextrose solution.
Interaction:Increase the concentration of the drug in the blood plasma inhibitors of the isoenzyme 3A4 cytochrome P450: ketoconazole, ciclosporin, erythromycin.
Reduced glycemic control while applying the drug to the thiazide diuretics, calcium channel blockers slow, lithium preparations, glucocorticoids, isoniazid, sympathomimetics, nicotinic acid, phenytoin, phenothiazines, thyroid hormones.
With simultaneous application with furosemide, a dose reduction is necessary.
The use of alcohol (especially on an empty stomach) during treatment increases the concentration of lactic acid in the blood plasma and increases the risk of hypoglycemia.
Special instructions:During pregnancy and lactation, the drug is canceled, the treatment of diabetes continues with injections of insulin.