Original articleRegadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans
Section snippets
Study Population
Thirty-eight subjects were enrolled at four sites from September 2001 through January 2005 into an open-label, phase 2 study of the dose dependency, duration, and reversibility of regadenoson’s coronary hyperemic effect (Table 1). Thirty-four patients were enrolled in a dose-escalation substudy, wherein each subject received a single injection of drug. Four additional patients were enrolled in a substudy to demonstrate the action of aminophylline to reverse the hyperemic effect of 400 μg of
Coronary Vasodilator Effects of Adenosine and Regadenoson
Intracoronary administration of adenosine (18 μg) resulted in a transient peak increase in coronary blood flow velocity of 3.1 ± 0.44–fold (n = 30; range, 2.4- to 3.9-fold) above baseline. The time to a near-peak (ie, ≥85% of maximum observed peak) flow velocity response to adenosine was approximately 30 seconds. Regadenoson, administered as an intravenous bolus in each patient after the response to adenosine had returned to baseline, increased coronary blood flow velocity in a dose-dependent
Discussion
A rapid intravenous bolus injection of regadenoson (400-500 μg) induced an increase in coronary blood flow by 2.5-fold or greater for a duration of 2 to 3 minutes, with side effects that were brief and well tolerated in subjects undergoing cardiac catheterization for evaluation or treatment of suspected ischemic heart disease. The results indicate that regadenoson can induce coronary hyperemia with a magnitude and duration that are suitable for myocardial perfusion imaging. The maximal coronary
Acknowledgment
We thank Drs Michael Ragosta III, Louis I. Heller, and Kenneth M. Kent for their contributions in enrolling subjects for this trial. Drs Shryock, Olmsted, Blackburn, and Belardinelli are current employees of CV Therapeutics, which provided funding for the study, and therefore have a potential conflict of interest. The other authors have indicated they have no financial conflicts of interest.
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This research was supported by a grant from CV Therapeutics, Palo Alto, Calif.
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Drs Lieu and Shryock contributed equally to the manuscript