Sulfonylureas and their use in clinical practice

Abstract

Many anti-diabetic drugs with different mechanisms of action are now available for treatment of type 2 diabetes mellitus. Sulfonylureas have been extensively used for treatment of type 2 diabetes for nearly 50 years and, even in our times, are widely used for treatment of this devastating chronic illness. Here, we review some of the available data on sulfonylureas, evaluating their mechanism of action and their effects on glycemic control. We can conclude that sulfonylureas are still the most used anti-diabetic agents: maybe this is due to their lower cost, to the possibility of mono-dosing and to the presence of an association with metformin in the same tablet. However, sulfonylureas, especially the older ones, are linked to a greater prevalence of hypoglycemia, and cardiovascular risk; newer prolonged-release preparations of sulfonylureas are undoubtedly safer, mainly due to reducing hypoglycemia, and for this reason should be preferred.

Keywords: glycemic control; hypoglycemia; sulfonylureas.

Figure 1

Mechanism of action of sulfonylureas On the top right corner is represented the SUR, while octagon is sulfonylurea (SU). When the SU binds SUR, the flow of K (arrows) stopped, so the cell membrane is depolarized. An increased flow of calcium cause the contraction of the filaments of actomyosin responsible for the exocytosis of insulin.