Acute effects of glibenclamide on reactive hyperaemia in the lower limbs in humans

Clin Hemorheol Microcirc. 2002;27(2):77-82.

Abstract

Three episodes of 1 min ischemia in the lower limbs in humans reduced the metabolic debt repayment (expressed as AUC of reactive hyperaemia) following more prolonged ischemia (666.6+/-86.6 vs 500.0+/-33.5 ml/100 ml). The administration of the ATP-dependent K(+) channel blocker glibenclamide was associated with a significant reduction in the AUC of reactive hyperaemia (666.6+/-86.6 vs 563.1+/-76.6 ml/100 ml), and with the removal of the protective effect produced by 3 episodes of 1 min ischemia (563.1+/-76.6 vs 551.8+/-71.3 ml/100 ml). Plasma level of glibenclamide reached the peak value of 1.295+/-0.15 micromol/l 2 h after drug administration, ranging around the 1 micromol/l concentration in the following 3 hours. Our findings produce indirect evidence that, similarly to the ischemic preconditioning of the heart, the protective effects towards ischemia of brief repeated episodes of sub-maximal occlusion in the peripheral circulation of the lower limbs in humans are mediated by ATP-dependent K(+) channels.

Publication types

  • Clinical Trial

MeSH terms

  • Adult
  • Area Under Curve
  • Female
  • Glyburide / blood
  • Glyburide / pharmacokinetics*
  • Glyburide / pharmacology
  • Humans
  • Hyperemia / drug therapy*
  • Hyperemia / prevention & control
  • Ischemia
  • Ischemic Preconditioning / methods
  • Lower Extremity / pathology*
  • Male
  • Middle Aged
  • Potassium Channel Blockers / blood
  • Potassium Channel Blockers / pharmacokinetics*
  • Potassium Channel Blockers / pharmacology

Substances

  • Potassium Channel Blockers
  • Glyburide