acetohexamide

Acetohexamide is an oral antidiabetic medication in the sulfonylurea class, used to improve glycemic control in adults with type 2 diabetes. It belongs to the first generation of sulfonylureas and is typically prescribed in combination with diet and exercise to lower elevated blood glucose. It is not indicated for type 1 diabetes or for diabetic ketoacidosis.

Mechanism of action: It lowers blood glucose primarily by stimulating insulin release from pancreatic beta cells. It binds to receptors on beta cells, closing ATP-sensitive potassium channels, leading to cell depolarization and insulin secretion. The effect depends on residual beta-cell function.

Pharmacokinetics: Administered orally. Onset of action occurs within hours, with a duration longer than short-acting agents but shorter than the longest-acting first-generation agents; dosing is usually once or twice daily, adjusted for hepatic or renal impairment. It is metabolized in the liver and excreted in urine.

Safety: The principal adverse effect is hypoglycemia, particularly in the elderly, with irregular meals, liver or kidney impairment, or when used with other hypoglycemic agents. Weight gain and gastrointestinal upset can occur. Contraindications include type 1 diabetes, diabetic ketoacidosis, and known hypersensitivity to sulfonylureas; use in pregnancy and lactation is generally avoided.

Clinical status: Following the development of newer sulfonylureas with more favorable pharmacokinetics and safety profiles, acetohexamide usage has declined, though it may still be used in some regions or specific patient situations.