Sulfonylureas are one of the common hypoglycemic drugs. What is the mechanism of action? How should be taken? What are the adverse effects? These are the things that diabetic patients should know. What are the types of sulfonylureas and how should they be taken? Mechanism of action of sulfonylureas – Promote insulin secretion from pancreatic beta cells – Some sulfonylureas have peripheral effects Enhance the sensitivity of peripheral tissues (liver, muscle) to insulin Indications for sulfonylureas – Patients with type 2 diabetes whose pancreatic beta cells are still functioning and whose blood glucose is not well controlled by diet and exercise therapy. Diabetic patients, especially non-obese type 2 diabetic patients, can be preferred. The first generation of sulfonylureas: D860, chlorosulfonylurea The second generation: glibenclamide Glipizide and controlled-release tablets Gliclazide and extended-release tablets Gliquidone The third generation: Glimepiride Glibenclamide – Slow absorption, long half-life, long duration of action, is a long-acting sulfonylurea drugs. – The hypoglycemic effect is obvious, especially the effect of lowering fasting blood sugar is better. – Start with a small dose, once a day, and adjust slowly as needed. – Prone to severe hypoglycemia. Gliclazide – Medium-acting sulfonylurea hypoglycemic drug. – Duration of action can be 10-15 hours, and it can be taken twice a day. – Among the sulfonylureas, the lowering effect of platelet aggregation is more obvious. Glipizide and controlled-release tablets Glipizide – Rapidly and completely absorbed, it is a fast-acting, short-acting preparation. – The hypoglycemic effect is more obvious, and hypoglycemia is less likely to occur. – Generally 2.5-30 mg/day, starting with a small dose, taken 30 minutes before meals. Glipizide Controlled Release Tablets – A controlled release tablet designed with an advanced gastrointestinal controlled release system. – It can be taken once a day to maintain the blood concentration at a more stable level throughout the day. – Taken at the same time as breakfast, it is not necessary to take the drug half an hour before a meal. – Glucose-lowering effect is similar to that of fast-acting glipizide. Glipizidone – Rapidly absorbed, short-acting sulfonylurea. – Peak blood level occurs 2 to 3 hours after oral administration. – It is mainly metabolized in the liver and about 95% is excreted by the bile. – Only 5% is excreted by the kidney. – It can be considered for patients who have impaired renal function but good hepatic function and do not want to inject insulin. Glimepiride – has a dual action, stimulating insulin secretion and improving insulin resistance. – The hypoglycemic effect is fast and long-lasting. – The plasma half-life is 9 hours, and it can be used once a day. – It can be taken immediately before or during meals, regardless of meal times. – Low hypoglycemic reactions. Adverse effects of sulfonylureas – The main adverse effect is hypoglycemia: mostly seen in patients using long-acting formulations. – Weight gain. – Allergic reactions: urticaria, skin erythema, exfoliative dermatitis, etc.