Effects of adenosine and a selective A2A adenosine receptor agonist on hemodynamic and thallium-201 and technetium-99m-sestaMIBI biodistribution and kinetics

JACC Cardiovasc Imaging. 2009 Oct;2(10):1198-208. doi: 10.1016/j.jcmg.2009.06.013.

Abstract

Objectives: The purpose of this study was to compare a selective A(2A) adenosine receptor agonist (regadenoson) with adenosine in clinically relevant canine models with regard to effects on hemodynamics and thallium-201 ((201)Tl) and technetium-99m ((99m)Tc)-sestaMIBI biodistribution and kinetics.

Background: The clinical application of vasodilator stress for perfusion imaging requires consideration of the effects of these vasodilating agents on systemic hemodynamics, coronary flow, and radiotracer uptake and clearance kinetics.

Methods: Sequential imaging and arterial blood sampling was performed on control, anesthetized closed-chest canines (n = 7) to evaluate radiotracer biodistribution and kinetics after either a bolus administration of regadenoson (2.5 microg/kg) or 4.5-min infusion of adenosine (280 microg/kg). The effects of regadenoson on coronary flow and myocardial radiotracer uptake were then evaluated in an open-chest canine model of a critical stenosis (n = 7). Results from ex vivo single-photon emission computed tomography were compared with tissue well-counting.

Results: The use of regadenoson compared favorably with adenosine in regard to the duration and magnitude of the hemodynamic effects and the effect on (201)Tl and (99m)Tc-sestaMIBI biodistribution and kinetics. The arterial blood clearance half-time was significantly faster for (99m)Tc-sestaMIBI (regadenoson: 1.4 +/- 0.03 min; adenosine: 1.5 +/- 0.08 min) than for (201)Tl (regadenoson: 2.5 +/- 0.16 min, p < 0.01; adenosine: 2.7 +/- 0.04 min, p < 0.01) for both vasodilator stressors. The relative microsphere flow deficit (0.34 +/- 0.02%) during regadenoson stress was significantly greater than the relative perfusion defect with (99m)Tc-sestaMIBI (0.69 +/- 0.03%, p < 0.001) or (201)Tl (0.53 +/- 0.02%, p < 0.001), although (201)Tl tracked the flow deficit within the ischemic region better than (99m)Tc-sestaMIBI. The perfusion defect score was larger with (201)Tl (22 +/- 2.8% left ventricular) than with (99m)Tc-sestaMIBI (17 +/- 1.7% left ventricular, p < 0.05) on ex vivo single-photon emission computed tomography images.

Conclusions: The bolus administration of regadenoson produced a hyperemic response comparable to a standard infusion of adenosine. The biodistribution and clearance of both (201)Tl and (99m)Tc-sestaMIBI during regadenoson were similar to adenosine vasodilation. Ex vivo perfusion images under the most ideal conditions permitted detection of a critical stenosis, although (201)Tl offered significant advantages over (99m)Tc-sestaMIBI for perfusion imaging during regadenoson vasodilator stress.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Adenosine / administration & dosage
  • Adenosine / pharmacology*
  • Adenosine A2 Receptor Agonists*
  • Animals
  • Blood Flow Velocity / drug effects
  • Chronic Disease
  • Coronary Circulation / drug effects*
  • Coronary Stenosis / diagnostic imaging*
  • Coronary Stenosis / metabolism
  • Coronary Stenosis / physiopathology
  • Disease Models, Animal
  • Dogs
  • Hyperemia / diagnostic imaging
  • Hyperemia / physiopathology
  • Infusions, Intravenous
  • Injections, Intravenous
  • Metabolic Clearance Rate
  • Myocardial Perfusion Imaging / methods*
  • Myocardium / metabolism
  • Myocardium / pathology
  • Predictive Value of Tests
  • Purines / administration & dosage
  • Purines / pharmacology*
  • Pyrazoles / administration & dosage
  • Pyrazoles / pharmacology*
  • Radiopharmaceuticals / blood
  • Radiopharmaceuticals / pharmacokinetics*
  • Receptor, Adenosine A2A / metabolism
  • Technetium Tc 99m Sestamibi / blood
  • Technetium Tc 99m Sestamibi / pharmacokinetics*
  • Thallium Radioisotopes / blood
  • Thallium Radioisotopes / pharmacokinetics*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon*
  • Vasodilator Agents / administration & dosage
  • Vasodilator Agents / pharmacology*

Substances

  • Adenosine A2 Receptor Agonists
  • Purines
  • Pyrazoles
  • Radiopharmaceuticals
  • Receptor, Adenosine A2A
  • Thallium Radioisotopes
  • Vasodilator Agents
  • regadenoson
  • Technetium Tc 99m Sestamibi
  • Adenosine