Effects of endothelin a receptor blockade on endothelial function in patients with chronic heart failure

Circulation. 2001 Feb 20;103(7):981-6. doi: 10.1161/01.cir.103.7.981.

Abstract

Background: Chronic heart failure (CHF) is associated with impaired endothelium-dependent vasodilation and increased basal vascular tone due, in part, to elevated endothelin-1 plasma levels. In the present study, we investigated whether a reduction of vascular tone using an endothelin A receptor blocker attenuates the impairment of endothelium-dependent, flow-mediated vasodilation (FMD).

Methods and results: Twenty-one patients with CHF randomly received either the endothelin A receptor blocker LU 135252 (30 mg/d, n=7; 300 mg/d, n=7) or a placebo (n=7). Using high-resolution ultrasound, FMD and endothelium-independent, nitroglycerin-induced dilation of the brachial artery were assessed at baseline in the 21 patients with CHF and in 11 controls and after 3 weeks treatment in the 21 patients with CHF. FMD at baseline was impaired in all 21 patients with CHF (3.2+/-2%) when compared with the 11 controls (9.7+/-4.9%; P=0.0005). In comparison with baseline, FMD significantly improved after 3 weeks of treatment with LU 135252 in all 14 patients receiving it (from 3.0+/-2.0% to 4.9+/-2.9%; P=0.04), but FMD remained unchanged with placebo. Subgroup analysis, according to different dosages, revealed a significant increase of FMD compared with baseline (from 2.4+/-1.5% to 5.5+/-2.4%; P=0.03) in the patients treated with the low-dose (30 mg/d), whereas a high dose of 300 mg/d failed to increase FMD significantly. Improvement in the high-dose group, however, may have been masked by reduced vasodilator capacity due to a significant increase in vessel size (from 4.8+/-0.4 to 5.1+/-0.7 mm; P=0.03).

Conclusions: These results suggest that endothelin A receptor blockade improves FMD in CHF patients.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Blood Flow Velocity / drug effects
  • Brachial Artery / drug effects*
  • Brachial Artery / physiopathology
  • Chronic Disease
  • Dose-Response Relationship, Drug
  • Endothelin Receptor Antagonists*
  • Endothelin-1
  • Endothelins / blood
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / physiopathology
  • Female
  • Heart Failure / blood
  • Heart Failure / drug therapy*
  • Heart Failure / physiopathology
  • Heart Function Tests / drug effects
  • Humans
  • Linear Models
  • Male
  • Middle Aged
  • Nitroglycerin / pharmacology
  • Phenylpropionates / therapeutic use*
  • Protein Precursors / blood
  • Pyrimidines / therapeutic use*
  • Receptor, Endothelin A
  • Treatment Outcome
  • Vasodilation / drug effects

Substances

  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Endothelins
  • Phenylpropionates
  • Protein Precursors
  • Pyrimidines
  • Receptor, Endothelin A
  • darusentan
  • Nitroglycerin