Included in the formulation
АТХ:A.10.B.D Combination of biguanides and sulfonylurea derivatives
A.10.B.D.10 Metformin and saxagliptin
Pharmacodynamics: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.
Saxaglyptine
Competitively and reversibly inhibits the enzyme dipeptidyl peptidase-4, which leads to an increase in plasma concentrations of insulin and C-peptide, which reduces the production of glucagon by pancreatic α-cells and increases insulin secretion by β-cells of the pancreas. Lowers glycemia on an empty stomach and postprandial hyperglycemia.
Pharmacokinetics: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.
The half-life is 6 hours. Elimination by the kidneys is unchanged.
Saxaglyptine
After oral administration, fasted to 75% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 3 hours. Almost does not bind to plasma proteins.
The therapeutic effect develops 0.5 hours after the start of the treatment. Metabolism in the liver.
The elimination half-life is 3 hours. Elimination by the kidneys is 75% and with feces - 25%.
Indications:It is used for the treatment of non-insulin dependent diabetes mellitus II type.
IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus
Contraindications:Diabetes I type - insulin-dependent, coma, ketoacidosis, individual intolerance.
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 during pregnancy and lactation.
Dosing and Administration:Inside, during dinner - once a day.
The initial dose: metformin / saxagliptin is 1000 / 2.5 mg, increases gradually, to a maximum of 2000/5 mg.
The highest daily dose: metformin / saxagliptin: 2000/5 mg.
The highest single dose: metformin / saxagliptin: 2000/5 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 P 450: ketonazole, 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.