Sulphonylurea
A class of oral medications used to treat type 2 diabetes
Sulphonylureas are a class of oral hypoglycemic agents used in the management of type 2 diabetes mellitus. They function primarily by stimulating the release of insulin from the beta cells of the pancreas.
Mechanism of Action[edit | edit source]
Sulphonylureas work by binding to the sulphonylurea receptor (SUR) on the surface of pancreatic beta cells. This binding inhibits the ATP-sensitive potassium channels, leading to cell depolarization. The depolarization opens voltage-gated calcium channels, resulting in an influx of calcium ions. The increase in intracellular calcium concentration triggers the exocytosis of insulin-containing granules, thereby increasing insulin secretion.
Types of Sulphonylureas[edit | edit source]
Sulphonylureas are divided into first-generation and second-generation agents:
First-Generation[edit | edit source]
Second-Generation[edit | edit source]
- Glyburide (also known as glibenclamide)
- Glipizide
- Glimepiride
Second-generation sulphonylureas are more potent and have a longer duration of action compared to first-generation agents.
Clinical Use[edit | edit source]
Sulphonylureas are typically used in patients with type 2 diabetes who have not achieved adequate glycemic control with lifestyle modifications alone. They are often used in combination with other antidiabetic agents such as metformin or thiazolidinediones.
Side Effects[edit | edit source]
Common side effects of sulphonylureas include:
- Hypoglycemia
- Weight gain
- Gastrointestinal disturbances
Rare but serious side effects include:
Contraindications[edit | edit source]
Sulphonylureas are contraindicated in patients with:
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
- Severe liver or kidney impairment
History[edit | edit source]
Sulphonylureas were first discovered in the 1940s. The first sulphonylurea, tolbutamide, was introduced in the 1950s. Since then, several other sulphonylureas have been developed, with improvements in potency and side effect profiles.
Also see[edit | edit source]
- Insulin therapy
- Biguanides
- Thiazolidinediones
- Dipeptidyl peptidase-4 inhibitors
- Sodium-glucose co-transporter 2 inhibitors
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