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Glibenclamide/Glyburide

格列苯脲

Mechanism of action:

Glibenclamide 是一種第二代磺醯尿素類（sulfonylurea）衍生物。Glibenclamide 能結合並抑制胰島 β 細胞膜上的磺醯脲受體 1（SUR1），此受體為 ATP-敏感鉀離子通道蛋白（ATP-sensitive potassium channel）的調節亞基。被 glibenclamide 抑制後，鉀離子外流減少，細胞膜發生去極化（depolarization）。去極化會造成鈣離子通道（calcium channel）開啟，鈣離子內流增加，促使胰島素釋放。

​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.

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