Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:A.10.B.H Inhibitors of dipeptidyl peptidase 4 (DPP-4)
A.10.B.H.01 Sitagliptin
Pharmacodynamics:Dipeptidylpeptidase-4 refers to transmembrane proteins and is involved in the metabolism of incretins: a glucagon-like peptide (GLP-1) and a glucose-dependent insulinotropic peptide (HIP). Sitagliptin competitively and reversibly inhibits the enzyme dipeptidyl peptidase-4 and thereby enhances GLP-1 and HIP. This leads to an increase in insulin secretion by β-cells of the pancreas. Lowers glycemia on an empty stomach and postprandial hyperglycemia.
Pharmacokinetics:After oral administration, up to 87% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 3 hours. It binds to plasma proteins in 38%.
The therapeutic effect develops 0.5 hours after the start of the treatment. Metabolism in the liver.
The elimination half-life is 12.4 hours. Elimination by the kidneys in 87% and with feces - 13%.
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, regardless of the time of ingestion, 100 mg 1 time / day.
The highest daily dose: 100 mg.
The highest single dose: 100 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: 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.