Glibenclamide Prevents Hypoglycemia-Induced Fatal Cardiac Arrhythmias in Rats

Endocrinology. 2018 Jul 1;159(7):2614-2620. doi: 10.1210/en.2018-00419.

Abstract

Sulfonylureas increase the incidence of severe hypoglycemia in people with type 2 diabetes and might increase the risk of sudden cardiac death. Sulfonylureas stimulate insulin secretion by closing pancreatic ATP-sensitive potassium ion (KATP) channels. To investigate the role of KATP channel modulators on cardiac arrhythmias and mortality in the setting of severe hypoglycemia, adult Sprague-Dawley rats underwent hyperinsulinemic (0.2 U/kg/min) severe hypoglycemic (10 to 15 mg/dL) clamps with continuous electrocardiography. The rats were randomized for treatment with intravenous vehicle (VEH), the sulfonylurea glibenclamide (GLIB; KATP channel blocker; 5 mg/kg/h), or diazoxide (DIAZ; KATP channel opener; 5 mg/kg/h). The results demonstrated that GLIB completely prevented first-degree heart block compared with VEH (0.18 ± 0.09/min) and DIAZ (0.2 ± 0.05/min). Second-degree heart block was significantly reduced with GLIB (0.12 ± 0.1/min) compared with VEH (0.6 ± 0.2/min) and DIAZ (6.9 ± 3/min). The incidence of third-degree heart block was completely prevented by GLIB compared with VEH (67%) and DIAZ (87.5%). Hypoglycemia-induced mortality was completely prevented by GLIB compared with VEH (60%) and DIAZ (82%). In conclusion, although GLIB increases the risk of hypoglycemia by increasing insulin secretion, these results have demonstrated a paradoxical protective role of GLIB against severe hypoglycemia-induced fatal cardiac arrhythmias.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arrhythmias, Cardiac / etiology*
  • Arrhythmias, Cardiac / prevention & control*
  • Diazoxide / therapeutic use
  • Glyburide / therapeutic use*
  • Heart Rate / drug effects
  • Hypoglycemia / complications*
  • Hypoglycemia / metabolism
  • Insulin / metabolism
  • Male
  • Random Allocation
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Insulin
  • Diazoxide
  • Glyburide