The Sound of Evolution
Glibenclamide/Glyburide
Mechanism of action:
Glibenclamide is a second-generation sulfonylurea derivative. Glibenclamide binds to and inhibits sulfonylurea receptor 1 (SUR1) on the membrane of pancreatic β cells. This receptor is the regulatory subunit of the ATP-sensitive potassium channel. Once inhibited by glibenclamide, potassium efflux decreases and the cell membrane undergoes depolarization. This depolarization opens calcium channels, increases calcium influx, and stimulates insulin release.
Reference(s):
1. Jaber LA et al. (1996). Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus. Ann Pharmacother.
2. Ravindran S et al. (2006). Identification of glyburide metabolites formed by hepatic and placental microsomes of humans and baboons. Biochem Pharmacol.
3. Shuster DL et al. (2014). Identification of CYP3A7 for glyburide metabolism in human fetal livers. Biochem Pharmacol.