Толбутамид

Химические свойства

White or almost white, crystalline powder.

Использование

Tolbutamide, have been used in a cDNA microarray assay to probe changes in gene expression in HepG2 cells upon their administration. It has been utilized to counteract insulin activity in a patch-clamp investigation of ATP sensitive K+ channels in mouse pancreatic β-cells. The activity of various biotransformation enzymes in cultured primary rat proximal tubular cells in the presence of tolbutamide and other compounds has been studied.

Определение

ChEBI: An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.

Общее описание

Tolbutamide is N-[(butylamino)carbonyl]-4-methylbenzenesulfonamide;or 1-butyl-3-(p-tolylsulfonyl)urea (Orinase,generic). Orinase Diagnostic was the sodium salt, which isfreely soluble in water for injection, but this product was discontinuedc. 2000.

Реакции воздуха и воды

Insoluble in water.

Профиль реактивности

TOLBUTAMIDE is an amide. Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx). TOLBUTAMIDE is incompatible with acids. .

Пожароопасность

Flash point data for TOLBUTAMIDE are not available. TOLBUTAMIDE is probably combustible.

Механизм действия

Tolbutamide is one of the most widely used antidiabetic agents. Its action is preferably connected with stimulatory action of β-cells in the pancreas, which results in intensive insulin secretion.

Клиническое использование

Tolbutamide should be used only when the diabetic patientis an adult or shows adult-onset diabetes, and the patientshould adhere to dietary restrictions.

Профиль безопасности

Moderately toxic by ingestion and several other routes. A human teratogen. Human reproductive effects by ingestion and possibly other routes: stillbirth, developmental abnormalities of the cardlovascular (circulatory) system and urogenital system, and unspecified neonatal effects. Human systemic effects by ingestion: nausea or vomiting, hypoglycemia. Other experimental teratogenic and reproductive effects. Mutation data reported. Implicated in aplastic anemia. When heated to decomposition it emits very toxic fumes of NO, and SOx.