Glibenclamid tablets 5 mg. №50

Description

Glibenclamid №50 Composition
active substance: glibenclamide;

1 tablet contains 5 mg glibenclamide in terms of 100% dry matter;

excipients: lactose, potato starch, povidone, ponso 4R (E 124), magnesium stearate.

Glibenclamid №50 Dosage form
Pills.

Basic physical and chemical properties: tablets of a flat-cylindrical shape with a line and a chamfer, pale pink color. Slight marbling and blotches are allowed on the surface.

Glibenclamid №50 pharmacotherapeutic group
Oral hypoglycemic drugs. Sulfonamides, sulfonylurea derivatives.

ATX code А10В В01.

Pharmacodynamics
Glibenclamide has a hypoglycemic effect in both type II diabetes patients and healthy people, as it increases insulin secretion by pancreatic b-cells by stimulating them. This action depends on the concentration of glucose in the environment of the b-cells.

Pharmacokinetics
After oral administration, glibenclamide is rapidly and almost completely absorbed. Simultaneous food intake does not significantly affect this. The binding of glibenclamide to blood plasma proteins is more than 98%. The maximum concentration in the blood serum is reached after 2.5 hours and is 100 ng / ml. After 8-10 hours, the concentration in the blood serum decreases, depending on the administered dose, by 10-20 ng / ml. The half-life after intravenous administration is about 2 hours, and after administration – 7 hours. However, some studies indicate that this time can be extended to 8-10 hours in diabetic patients. Glibenclamide is completely metabolized in the liver to several metabolites that are not significantly involved in the glucose-lowering effect of glibenclamide. Metabolites are excreted in urine and bile in approximately equal amounts, and their complete excretion ends in 45-72 hours. In patients with impaired liver function, the excretion of glibenclamide from plasma is slowed down. In patients with renal failure, depending on the degree of renal dysfunction, excretion of metabolites increases compensatory. In moderate renal failure (creatinine clearance ≥ 30 ml / min), the total elimination remains unchanged, and in severe renal failure, cumulation is possible.

Indications
Non-insulin dependent diabetes mellitus in adults (type II diabetes mellitus), if other measures, such as strict adherence to diet, weight loss, sufficient physical activity, did not lead to a satisfactory correction of blood glucose levels.

Contraindications
Hypersensitivity to the active substance, to Ponceau 4R or to any component of the drug.
hypersensitivity to other sulfonylureas, sulfonamides, sulfonamide diuretics and probenecid.
in cases of diabetes mellitus, and when insulin treatment is required: insulin-dependent diabetes mellitus (type I diabetes mellitus), complete secondary ineffectiveness of glibenclamide therapy in type II diabetes mellitus, metabolism with a bias towards acidosis, coma or diabetic coma, condition after resection of the pancreas.
severe liver dysfunction.
severe renal dysfunction.
During pregnancy and breastfeeding.
use with bosentan.