KATP blocker
ATP-sensitive potassium channel blocker
- Pancreatic beta-cell depolarization → insulin release
- Insulin secretion is independent of glucose → hypoglycemia risk while fasting
- Effect wanes as beta-cell mass declines
- ↑ insulin → weight gain
- ATP-gated; Not voltage-gated
- Blocks the ATP-sensitive potassium (KATP) channel = inwardly rectifying potassium channel (Kir6) + sulfonylurea receptor (SUR)
- Closes pancreatic β-cell KATP channels → membrane depolarization → insulin release even at low glucose → hypoglycemia risk
- Sulfonylureas
- Meglitinides
Drugs with this mechanism (7)
- Glimepiride — Once-daily second-generation sulfonylurea; hypoglycemia and weight gain.
- Glipizide — Second-generation sulfonylurea; shorter-acting, safer in renal impairment.
- Glipizide ER — Extended-release sulfonylurea; hypoglycemia and weight gain remain limiting.
- Glyburide — Long-acting sulfonylurea; higher hypoglycemia risk in the elderly.
- Nateglinide — Rapid mealtime insulin secretagogue; skip it when the meal is skipped.
- Repaglinide — Rapid, short-acting meal-time insulin secretagogue (glinide).
- Tolbutamide — First-generation short-acting sulfonylurea.
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