Acetohexamide

A sulfonylurea class antidiabetic drug

Structural formula of Acetohexamide

Acetohexamide is an oral hypoglycemic agent belonging to the sulfonylurea class of drugs. It is used in the management of type 2 diabetes mellitus to help control blood sugar levels. Acetohexamide works by stimulating the release of insulin from the beta cells of the pancreas.

Pharmacology

Acetohexamide is a first-generation sulfonylurea, which means it is one of the earlier drugs developed in this class. It functions by binding to the sulfonylurea receptor on the beta cells, leading to the closure of ATP-sensitive potassium channels. This action results in the depolarization of the cell membrane and the opening of voltage-gated calcium channels, which increases intracellular calcium and stimulates insulin secretion.

Chemical Structure

Ball-and-stick model of Acetohexamide

The chemical structure of acetohexamide is characterized by a sulfonylurea moiety, which is essential for its hypoglycemic activity. The presence of a cyclohexyl group differentiates it from other sulfonylureas and influences its pharmacokinetic properties.

Pharmacokinetics

Acetohexamide is absorbed from the gastrointestinal tract and undergoes hepatic metabolism. It is metabolized to an active metabolite, hydroxyhexamide, which also contributes to its hypoglycemic effect. The drug and its metabolites are excreted primarily in the urine.

Clinical Use

Acetohexamide is indicated for the treatment of type 2 diabetes in patients who cannot achieve adequate glycemic control with diet and exercise alone. It is typically used as part of a comprehensive diabetes management plan that includes lifestyle modifications.

Side Effects

Common side effects of acetohexamide include hypoglycemia, nausea, and dizziness. As with other sulfonylureas, there is a risk of severe hypoglycemia, especially in patients with renal or hepatic impairment, or those who are elderly.

Contraindications

Acetohexamide 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.

Related pages

• Sulfonylurea
• Type 2 diabetes mellitus
• Insulin