Sulfonylurea hypoglycemic drugs

Sulfonylureas are a class of oral antidiabetic medications commonly used to treat type 2 diabetes.

These drugs work by stimulating the pancreas to release more insulin, which helps lower blood sugar levels in individuals with diabetes. Sulfonylureas are particularly effective for people with type 2 diabetes whose bodies still produce some insulin.

One of the main advantages of sulfonylureas is their ability to quickly lower blood sugar levels, making them a popular choice for managing diabetes. However, this rapid action can sometimes lead to hypoglycemia (low blood sugar), especially if the dose is too high or if meals are skipped.

Common sulfonylureas include glyburide, glipizide, and glimepiride. These medications are usually taken once or twice daily with meals. It is important for individuals using sulfonylureas to monitor their blood sugar levels regularly and be aware of the signs of hypoglycemia.

Methylphenidate (D860): The first generation of sulfonylurea hypoglycemic drugs; it is still used in some countries due to its low price; rapid absorption and short action; take half an hour before meals; usual dosage is 0.5g, twice or three times daily, with a limit of 3g; few side effects, but may cause discomfort in the middle and upper abdomen, occasional loss of appetite, and skin rashes and measles in a few people, and very rarely cause jaundice and leukopenia.

Sulfonylurea hypoglycemic drugs
hypoglycemic drugs


The first generation of sulfonylurea hypoglycemic drugs; slow and long-lasting action, and the metabolites also have activity; reaches the highest effective plasma concentration after a week of use; because of the long action time, it may cause nocturnal hypoglycemia; can cause water retention, leading to hyponatremia. Currently, some countries have stopped using the first-generation sulfonylurea hypoglycemic drugs and replaced them with second-generation ones.


The first variety of the second-generation sulfonylurea hypoglycemic drugs; widely used worldwide and affordable; slow absorption, long half-life, belonging to the long-acting sulfonylurea hypoglycemic drugs; has a significant hypoglycemic effect, especially good at reducing fasting blood glucose; start with a small dose, once daily, and slowly adjust as needed; limited to 15mg daily, divided into two doses in the morning and evening; reduce the dose for the elderly and weak individuals to avoid severe hypoglycemia; may have gastrointestinal reactions.


A long-acting sulfonylurea hypoglycemic drug; widely used in Europe; can promote insulin secretion in the first phase; has a mild hypoglycemic effect and less likely to cause severe hypoglycemia; usually taken once before breakfast and once before dinner; among sulfonylurea hypoglycemic drugs, it has a more significant effect on reducing platelet aggregation; there are reports that it can delay the progression of retinopathy.

Sulfonylurea hypoglycemic drugs
Sulfonylurea hypoglycemic drugs


Rapid and complete absorption; a fast-acting and short-acting sulfonylurea hypoglycemic drug; has a significant hypoglycemic effect and less likely to cause severe hypoglycemia; can promote rapid release of insulin after meals; usual dosage is 2.5~3mg daily, taken twice before breakfast and dinner.

Glibenclamide controlled-release tablets:

A controlled-release preparation designed for specific gastrointestinal system; taken once daily, it can maintain a stable drug concentration throughout the day; there is no need to take it half an hour before meals; take one dose in the morning; insulin peaks can occur after each meal; can increase insulin sensitivity; better control of fasting blood glucose than rapid-release glibenclamide. Usual dosage is 5~20mg daily, taken once before breakfast.


Rapidly absorbed and almost completely absorbed; peaks in blood plasma occur 2~3 hours after oral administration; a short-acting sulfonylurea; mainly metabolized in the liver, about 95% excreted through bile, and a small amount (about 5%) through the kidney; applicable to those with poor kidney function; usual dosage is 15~180mg daily, taken 2~3 times.


The third generation of sulfonylurea hypoglycemic drugs; compared to glibenclamide, glyburide has a faster and longer-lasting hypoglycemic effect; plasma half-life of 9 hours, only one dose per day is needed; clinically used for type 2 diabetes, 1~8mg daily. Fasting blood glucose (FBG), 2-hour postprandial blood glucose (PBG), and HbA1C are significantly improved. Only mild hypoglycemic reactions.

Sulfonylurea hypoglycemic drugs can be divided into short-acting, intermediate-acting, and long-acting types. Short-acting sulfonylurea drugs include glipizide, gliclazide, etc. Intermediate-acting sulfonylurea drugs include glimepiride, glibenclamide, etc. Long-acting sulfonylurea drugs include glyburide, glipizide controlled-release tablets.

There are several types of antidiabetic medications available to help manage blood sugar levels in individuals with diabetes. These medications work in different ways to achieve the common goal of controlling blood glucose levels.

Biguanides: Biguanides, such as metformin, are commonly prescribed as a first-line treatment for type 2 diabetes. They work by reducing the amount of glucose produced by the liver and improving the body's sensitivity to insulin.

Sulfonylureas: Sulfonylureas stimulate the pancreas to release more insulin, thereby lowering blood sugar levels. Examples include glyburide, glipizide, and glimepiride.

DPP-4 Inhibitors: Dipeptidyl peptidase-4 (DPP-4) inhibitors work by increasing the levels of incretin hormones, which stimulate insulin release and inhibit the release of glucagon. Sitagliptin and saxagliptin are common DPP-4 inhibitors.

SGLT2 Inhibitors: Sodium-glucose cotransporter 2 (SGLT2) inhibitors help lower blood sugar levels by increasing the excretion of glucose through urine. Canagliflozin and dapagliflozin are examples of SGLT2 inhibitors.

GLP-1 Receptor Agonists: Glucagon-like peptide-1 (GLP-1) receptor agonists stimulate insulin secretion, inhibit glucagon release, and slow down gastric emptying. Exenatide and liraglutide are well-known GLP-1 receptor agonists.

These are just a few examples of the different types of antidiabetic medications available, each with its own mechanism of action and potential side effects. It is important for individuals with diabetes to work closely with their healthcare providers to determine the most suitable medication regimen based on their specific needs and health status.

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