Second-Generation Sulfonylureas

The first-generation sulfonylureas are not frequently used in the modem management of diabetes mellitus because of their relatively low specificity of action, delay in time of onset, occasional long duration of action, and a variety of side effects. They also tend to have more adverse drug interactions than the second-generation sulfonylureas. They are occasionally used in patients who have achieved previous adequate control with these agents. 

Glucotrol (Glipizide) 10.7 (0.5) 14.1 (0.5) 13.1 (0.6) A second generation sulfonylurea that blocks ATP-sensitive K-channels in the membrane of beta cells, stimulating the release of insulin. 

Mechanism of Action A second-generation sulfonylurea that promotes release of insulin from beta cells of the pancreas and increases insulin sensitivity at peripheral sites. Therapeutic Effect Lowers blood glucose concentration. 

No demonstrated advantage over existing second-generation sulfonylureas... 

Glibenclamide is a second generation sulfonylurea. There are two mechanisms of action for the lowering of the blood glucose ... 

Glimepiride [gly MEH pih ride] is a new, second generation sulfonylurea. It was the first sulfonylurea to be approved for concurrent use with insulin, but has no additional advantage over the other sulfonylureas. Elimination is through the urine and feces. Like all sulfonylureas, it can cause hypoglycemia, hyperinsulinemia, and weight gain. 

Second-generation sulfonylureas increase tissue response to insulin and decrease glucose production by the liver resulting in greater hypoglycemic potency at smaller doses. They have a longer duration and cause few side effects, but should not be used if the patient has liver or kidney dysfunction. Sulfonylureas are ... 

Table 1. Overview of first- and second-generation sulfonylureas as well as non-SU secretagogues.

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