Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea

medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and re ...

used to treat

diabetes mellitus type 2 Type 2 diabetes, formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent urination, ...

, particularly in people whose diabetes cannot be controlled by diet alone.

Mechanism of action

Acetohexamide bind to an ATP-sensitive K⁺ (K_ATP) channel on the cell membrane of

pancreatic beta cell Beta cells (β-cells) are a type of cell found in pancreatic islets that synthesize and secrete insulin and amylin. Beta cells make up 50–70% of the cells in human islets. In patients with Type 1 diabetes, beta-cell mass and function are dimini ...

s. This inhibits the out flux of

potassium Potassium is the chemical element with the symbol K (from Neo-Latin ''kalium'') and atomic number19. Potassium is a silvery-white metal that is soft enough to be cut with a knife with little force. Potassium metal reacts rapidly with atmosphe ...

, which causes the

membrane potential Membrane potential (also transmembrane potential or membrane voltage) is the difference in electric potential between the interior and the exterior of a biological cell. That is, there is a difference in the energy required for electric charges ...

to become more positive. This depolarization in turn opens

voltage-gated calcium channel Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'', muscle, glial cells, neurons, etc.) with a permeabi ...

s. The rise in intracellular

calcium Calcium is a chemical element with the symbol Ca and atomic number 20. As an alkaline earth metal, calcium is a reactive metal that forms a dark oxide-nitride layer when exposed to air. Its physical and chemical properties are most similar to ...

leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of insulin.

Risks

Oral hypoglycemic drugs, including acetohexamide, have been associated with increased cardiovascular mortality. Talk to your doctor about the possible risks, benefits, and alternatives of using this drug for your condition.

References

Potassium channel blockers 1-(Benzenesulfonyl)-3-cyclohexylureas Aromatic ketones {{Gastrointestinal-drug-stub