Acetohexamide Explained

Acetohexamide should not be confused with acetazolamide.

Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, particularly in people whose diabetes cannot be controlled by diet alone.[1]

Mechanism of action

Acetohexamide binds to an ATP-sensitive K+ (KATP) channel on the cell membrane of pancreatic beta cells. This inhibits the outflux of potassium, which causes the membrane potential to become more positive. This depolarization in turn opens voltage-gated calcium channels. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of insulin.[2]

Risks

Sulfonylureas, especially first-generation sulfonylureas such as Acetohexamide, can cause severe hypoglycemia and increase the risk of adverse cardiovascular events. [3] [4]

Notes and References

  1. Montgomery DA . Current Therapeutics. CCII. Acetohexamide . The Practitioner . 193 . 555–60 . October 1964 . 14216839 .
  2. Web site: Acetohexamide . DrugBank .
  3. Web site: www.accessdata.fda.gov.
  4. Web site: Acetohexamide . Medline Plus . https://web.archive.org/web/20050911024428/http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a682478.html . 11 September 2005 .