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What are Sulfonylureas?

Sulfonylureas are a group of medications used to treat Diabetes (type 2 diabetes). Sulfonylureas help to increase the release of insulin from the pancreas. The first Sulfonylureas were used in the 1950s.

Some of the popular sulfonylureas often prescribed are -

  •    Glucotrol(glipizide)- Glipizide (Glucotrol) is an easily available drug used to treat type 2 diabetes. It is a more popular and widely used drug compared to other drugs. It is available in generic as well as brand versions. Most Medicare and insurance plans cover generic glipizide.
  •    Amaryl(glimepiride)- Glimepiride(Amaryl), is an anti-diabetic medicine generally used to treat type 2 diabetes. It is less preferred than other diabetes medications. It is recommended to use together with diet and exercise. It is taken by mouth or oral medicine. Glimepiride takes up to two hours for maximum effect and lasts for about twenty-four hours.
  •    Glyburide- Glyburide(Glibenclamide), is an antidiabetic medication used for type 2 diabetes. It is also recommended to take it together with diet and exercise. It can be used with other antidiabetic medications.
  •    Glynase- Glynase is somehow the same as glyburide. It is also used with proper diet and exercise to treat type 2 diabetes.
  •    Tolbutamide- It is basically used to improve blood sugar control when taken with proper diet and exercise.

History of Sulfonylureas

Sulfonylureas were firstly discovered, in 1942, by the chemist Marcel Janbon and his co-workers. They were studying sulfonamide antibiotics and discovered the compound sulfonylureas for treating hypoglycemia in animals. Later on, in the 1950s sulfonylureas were developed for treating diabetes.


Sulfonylureas mechanism of action

Sulfonylureas(organic compounds) bind to and close ATP-sensitive K+ channels on the cell membrane of pancreatic beta cells, which depolarizes the cell by preventing the exiting of potassium. This depolarization opens voltage-gated channels. The rise in intracellular calcium accelerates the fusion of insulin granules with the cell membrane and therefore increased the flow of mature insulin.

There is some evidence that sulfonylureas also sensitize β-cells to glucose, that they limit the production of glucose in the liver, that they decrease the breakdown and release of fatty acids by adipose, and decrease the clearance of insulin by the liver.

Furthermore, it has been shown that sulfonylureas interact with the nucleotide exchange factor which has a decreased glucose-lowering effect upon sulfonylurea treatment.

What are the uses of Sulfonylureas?

  •    Sulfonylureas are used to Lower blood sugar levels by stimulating the production of insulin in the beta cells of the pancreas.
  •    Sulfonylureas increase the efficiency of the body to use insulin effectively.
  •    It is also used to increase the utilization of peripheral glucose.
  •    It is used to decrease the generation of glucose in the liver and also increase the number of the insulin receptor.
  •    Sulfonylureas are used to increase insulin release by inhibiting ATP-sensitive potassium channels that depolarize the beta cells.


What are the side effects of Sulfonylureas?

  •    Sulfonylureas are opposed to metformin and the patient can suffer from hypoglycemia due to excess release and production of insulin.
  •    Sulfonylureas also cause problems of increased weight.
  •    Dermatological issues and other kinds of skin problems occur due to the use of Sulfonylureas.
  •    Dark-colored urine and upset stomach (having problems in digestion) are also some of the side effects of Sulfonylureas.
  •    Other common side effects include vomiting, dizziness, headache, nausea, diarrhea, muscle pain, and weakness.

Key Takeaways

Sulfonylureas are oral(taken from the mouth directly) medications that help lower blood glucose levels in people living with Type 2 diabetes. All sulfonylureas are available in generic versions, making the sulfonylureas relatively affordable. The main side effect of sulfonylureas is hypoglycemia(low blood sugar level). The chances of hypoglycemia increase when sulfonylureas are combined with other diabetes medications, like metformin or insulin.

We Specialty Care Clinics help you to understand the mechanism of sulfonylureas and provide you with the best medications for diabetes and the best outcome from the medications. If anyone of you has diabetes or need consultation on the uses of sulfonylureas, connect with us at 469-545-9983