Tolbutamide

1-butyl- 3-( p- tosylsulfonyl ) urea

A10BB03, V04CA01

Sulfonylurea antidiabetic

128.5 ° C

5.16

Very poor in water ( 109 mg · l-1 at 37 ° C)

2490 mg · kg -1 ( LD50, rat, oral)

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Tolbutamide is a drug for the treatment of type 2 diabetes, the so-called adult-onset diabetes, which, for example, glibenclamide is one from the series of the sulfonylureas.

Operation

It effects by binding to the SUR1 receptor, which is a subunit of the ATP-dependent potassium channel of the β - cells in the islets of Langerhans of the endocrine pancreas, inhibition precisely this. This results in a depolarisation of the membrane, which in turn leads to an influx of calcium ions into the β - cells. Calcium is an important effector in the fusion of vesicles with the membrane dar. in the vesicles of the pancreas are insulin and C- peptide, which are increasingly distributed in the sequence. Insulin leads to the desired drop in blood sugar levels.

Disadvantage

This therapy leads sooner or later to a fatigue of insulin secretion from the β - cells. The patient is only a certain amount of time spared the injection of insulin. It should be advised primarily to maintain a strict diet in combination with physical activity, since insulin resistance, which yes is present in type 2, in part, by the appropriate lifestyle is reversible.