Glibenclamide

5-chloro- N-[2 - [4 - ( cyclohexylcarbamoyl -sulfamoyl )-phenyl] ethyl] -2-methoxy -benzamide

A10BB01

Antidiabetic agents, sulfonylureas

Potassium channel blockers

173-175 ° C

5.3

2.3 ± 0.3 mg.l -1 ( pH 6.5)

  • > 10 g · kg -1 ( LD50, dog, oral)
  • > 15 g · kg -1 ( LD50, guinea pig, oral)
  • 3.25 g · kg -1 ( LD50, mouse, oral)

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Glibenclamide is a chemical compound selected from the group of the sulfonylureas, which is used in medicine as an oral antidiabetic. It causes an increase in insulin release from β cells of the pancreas.

If it is possible to lower the blood sugar effectively, even with glibenclamide the risk of late complications of diabetes mellitus is lowered. However, due to adverse effects of metformin as the active substance is today the first choice.

Action principle

As other sulfonylureas glyburide blocked potassium channels in the β - cells, thus inhibiting the outflow of these ions. This leads to a depolarization and thus the opening of calcium channels, voltage-controlled; Calcium ions flow into the cell increases. Characterized enzymes are activated which cause the release of insulin. Thus glibenclamide can act, which is a body's ability to insulin must be present.

Adverse effects

The hypoglycemic effect of glibenclamide is a quickly and can last up to 24 hours. This should be taken into account in the dose and in the control of blood glucose statement because a relative overdose may ( as in irregular food intake ) lead to hypoglycaemia. Feared is colloquially called " hypoglycemic shock" or " sugar shock." The problem is the Gewichtsnormalisieung overweight diabetics as glibenclamide has an appetite stimulating effect ( insulin release ).

Glibenclamide impairs ischemic preconditioning of the heart muscle, which can lead to more extensive myocardial infarction in case of interruption of the myocardial oxygen supply. On the other hand, cardioprotective effects have been described as an anti-arrhythmic effect.

Swell

Trade names

Daonil (A, CH), Euglucon (D, A), Gliben CT ( D), Glibenorm (CH), Glibesifar (CH), Glucobene (A), Normoglucon (A), Maninil (D), Melix (CH), Semi- Daonil (CH), Semi- Euglucon (D ), numerous generics (D, A, CH)

Glucovance (A)

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