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Oral hypoglycemic agent, sulfonylurea derivative of II generation. Stimulates insulin secretion by pancreatic β-cells, increases insulin release. Acts mainly during the second stage of insulin secretion. Increases peripheral tissue sensitivity to insulin and the degree of its binding to target cells. It has hypolipidemic effect and decreases thrombogenic properties of blood.
After oral administration, glibenclamide is rapidly and almost completely absorbed from the gastrointestinal tract. Binding to plasma proteins is more than 95%. It is metabolized in the liver with the formation of inactive metabolites.
It is excreted mainly as metabolites in the urine (95%) and in bile. T1/2 is about 10 hours.
Contraindications to use
Type 1 diabetes mellitus, ketoacidosis, diabetic precoma and coma, severe microcirculatory disorders, infectious diseases, marked renal and/or hepatic dysfunction. Hypersensitivity to sulfonylurea derivatives and sulfonamides. It is not used during major surgical interventions.
Use in pregnancy and lactation
Glibenclamide is not recommended for use in pregnancy and lactation.
Administration in patients with liver dysfunction
Prohibited in patients with significant liver dysfunction. Caution is used in patients with hepatic impairment (including in anamnesis).
Administration in patients with impaired renal function
It is contraindicated in patients with significant renal dysfunction. Caution is used in patients with renal impairment (including in the anamnesis).
Administration in elderly patients
The initial dose for elderly patients is 1 mg/day.
Indications of active ingredients of the drug Glibenclamide
Type 2 diabetes mellitus in adults with ineffective diet therapy.
The dose is set individually, depending on age, severity of diabetes, level of glycemia on an empty stomach and 2 hours after meals.
The average dose is 2.5-15 mg/day, the frequency of administration is 1-3 times/day. It is taken 20-30 minutes before the meal. In doses greater than 15 mg/day is used rarely and does not cause significant enhancement of hypoglycemic effect.
For elderly patients, the initial dose is 1 mg/day.
When switching from biguanides, the starting dose of glibenclamide is 2.5 mg/day. Biguanides should be discontinued, and the dose of glibenclamide may be increased by 2.5 mg every 5-6 days, if necessary, until compensation for carbohydrate metabolism. If there is no compensation within 4-6 weeks, combined therapy with glibenclamide and biguanides should be planned.