Glycyclamide

Glycyclamide is a sulfonylurea class antidiabetic drug used in the management of type 2 diabetes mellitus. It functions by stimulating the release of insulin from the beta cells of the pancreas.

Mechanism of Action

Glycyclamide, like other sulfonylureas, works by binding to the sulfonylurea receptor (SUR1) on the pancreatic beta cells. This binding leads to the closure of ATP-sensitive potassium channels, resulting in depolarization of the cell membrane. The depolarization opens voltage-gated calcium channels, allowing calcium influx, which triggers the exocytosis of insulin-containing granules.

Pharmacokinetics

Glycyclamide is administered orally and is absorbed from the gastrointestinal tract. It undergoes hepatic metabolism and is primarily excreted via the kidneys. The drug's half-life and duration of action can vary based on individual patient factors such as renal function.

Clinical Use

Glycyclamide is indicated for the treatment of type 2 diabetes mellitus in patients who cannot achieve adequate glycemic control with diet and exercise alone. It is often used in combination with other antidiabetic agents such as metformin or thiazolidinediones.

Side Effects

Common side effects of glycyclamide include hypoglycemia, weight gain, and gastrointestinal disturbances. Hypoglycemia is a significant risk, especially in elderly patients or those with renal impairment. Other potential side effects include allergic reactions and hematological changes.

Contraindications

Glycyclamide is contraindicated in patients with type 1 diabetes, diabetic ketoacidosis, and in those with known hypersensitivity to sulfonylureas. Caution is advised in patients with renal or hepatic impairment.

History

Glycyclamide was developed as part of the second generation of sulfonylureas, which are characterized by their increased potency and shorter half-lives compared to first-generation agents.

See Also

• Sulfonylurea
• Type 2 diabetes mellitus
• Insulin
• Metformin
• Thiazolidinediones