Sulfonylurea

Sulfonylureas are oral hypoglycemic agents, drugs that are used in type 2 diabetes mellitus ( sugar diabetes ). They allow the increased release of insulin by blocking potassium channels in the β - cells of the pancreas. They are structurally related to the sulfonamides. Some sulfonylureas are also effective as a herbicide.

Use as an antidiabetic

Pharmacology

Sulfonylureas stimulate the insulin release of the β - cells of the pancreas irrespective of the blood glucose concentration ( insulinotropic action ). They block ATP-sensitive potassium channels of the β - cells by binding to specific SUR -1 binding sites. As a result of membrane depolarization to open voltage-gated calcium channels. The influx of calcium resulting in a discharge of insulin from the Speichervesikeln and thus to an increased release of insulin into the blood. They are effective for risk reduction of microvascular events ( glibenclamide ). Gliquidone is mined as the sole representative of the sulfonylureas only by the liver and can therefore be given in renal failure.

Side effects

Sulphonylureas can cause hypoglycaemia, possibly also to gastrointestinal complaints. They promote weight gain by the antilipolytic effect of insulin. Rare side effects include blood disorders or hepatic cholestasis (such as the sulfonamides ).

Sufonylharnstoffe force an insulin secretion from the β cells of the pancreas, so that they can lead to hypoglycemia. Furthermore, studies suggest that sulfonylureas may lead to a failure of β - cells.

According to recent studies, may lead to cardiac risks by sulfonylureas.

Contraindications

Contraindicated are sulfonylureas and their derivatives in type 1 diabetes mellitus, severe hepatic or renal insufficiency ( this does not apply gliquidone and repaglinide ) and pancreatectomy. If you are pregnant, diabetic women should be switched to insulin. Other contraindications for major surgery or severe infections.

Representative

The best known representative is glibenclamide. Glimepiride has a longer duration of action as glibenclamide. Older, much weaker effective sulfonylureas tolbutamide and are carbutamide.

Sulfonylureas of the first generation:

• Carbutamide
• Tolbutamide

Second-generation sulfonylureas:

• Glibenclamide ( Euglucon, Normoglucon, Glucobene, slide Eptal )
• Glibornuride ( Gluborid, Glutril )
• Gliclazide ( Diamicron )
• Glipizide ( Glibenese, Minidiab )
• Gliquidone ( Glurenorm )
• Glisoxepid (Pro - Diaban )
• Glycodiazin ( Redul )

Sulfonylureas of the third generation:

• Glimepiride ( Amaryl )

Use as a herbicide

The sulfonylureas are one of the major drug classes of herbicides. They work by inhibiting acetolactate synthase. They include, for example:

• Amidosulfuron
• Azimsulfuron
• Chlorsulfuron
• Cinosulfuron
• Metsulfuron methyl
• Sulfosulfuron
• Tritosulfuron