Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite

Br J Pharmacol. 2013 Jun;169(3):659-70. doi: 10.1111/bph.12152.

Abstract

Background and purpose: Nitrite (NO₂⁻) has recently been shown to represent a potential source of NO, in particular under hypoxic conditions. The aim of the current study was to compare the haemodynamic effects of NO₂⁻ in healthy volunteers and patients with stable congestive heart failure (CHF).

Experimental approach: The acute haemodynamic effects of brachial artery infusion of NO₂⁻ (0.31 to 7.8 μmol·min⁻¹) was assessed in normal subjects (n = 20) and CHF patients (n = 21).

Key results: NO₂⁻ infusion was well tolerated in all subjects. Forearm blood flow (FBF) increased markedly in CHF patients at NO₂⁻ infusion rates which induced no changes in normal subjects (ANOVA: F = 5.5; P = 0.02). Unstressed venous volume (UVV) increased even with the lowest NO₂⁻ infusion rate in all subjects (indicating venodilation), with CHF patients being relatively hyporesponsive compared with normal subjects (ANOVA: F = 6.2; P = 0.01). There were no differences in venous blood pH or oxygen concentration between groups or during NO₂⁻ infusion. Venous plasma NO₂⁻ concentrations were lower in CHF patients at baseline, and rose substantially less with NO₂⁻ infusion, without incremental oxidative generation of nitrate, consistent with accelerated clearance in these patients. Plasma protein-bound NO concentrations were lower in CHF patients than normal subjects at baseline. This difference was attenuated during NO₂⁻ infusion. Prolonged NO₂⁻ exposure in vivo did not induce oxidative stress, nor did it induce tolerance in vitro.

Conclusions and implications: The findings of arterial hyper-responsiveness to infused NO₂⁻ in CHF patients, with evidence of accelerated transvascular NO₂⁻ clearance (presumably with concomitant NO release) suggests that NO₂⁻ effects may be accentuated in such patients. These findings provide a stimulus for the clinical exploration of NO₂⁻ as a therapeutic modality in CHF.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Aged
  • Brachial Artery
  • Cohort Studies
  • Drug Tolerance
  • Female
  • Forearm
  • Heart Failure / drug therapy
  • Heart Failure / metabolism
  • Heart Failure / physiopathology*
  • Hemodynamics / drug effects
  • Humans
  • In Vitro Techniques
  • Infusions, Intra-Arterial
  • Male
  • Metabolic Clearance Rate
  • Middle Aged
  • Nitric Oxide / administration & dosage
  • Nitric Oxide / analogs & derivatives
  • Nitric Oxide / metabolism
  • Nitric Oxide / pharmacokinetics
  • Nitroglycerin / administration & dosage
  • Nitroglycerin / metabolism
  • Nitroglycerin / pharmacokinetics
  • Nitroglycerin / pharmacology
  • Oxidative Stress / drug effects
  • Regional Blood Flow / drug effects
  • Saphenous Vein / drug effects
  • Saphenous Vein / physiopathology
  • Sodium Nitrite / administration & dosage
  • Sodium Nitrite / metabolism
  • Sodium Nitrite / pharmacokinetics*
  • Sodium Nitrite / pharmacology
  • Vasodilation / drug effects
  • Vasodilator Agents / administration & dosage
  • Vasodilator Agents / metabolism
  • Vasodilator Agents / pharmacokinetics*
  • Vasodilator Agents / pharmacology
  • Vasomotor System / drug effects*
  • Vasomotor System / physiopathology

Substances

  • Vasodilator Agents
  • Nitric Oxide
  • Nitroglycerin
  • Sodium Nitrite