Comparison of the Safety of Adenosine and Regadenoson in Patients Undergoing Outpatient Cardiac Stress Testing

Abstract

Among patients undergoing an outpatient pharmacologic stress test, the use of adenosine was associated with a lower occurrence of adverse effects and lower rate of a rescue agent use and may provide a potential medication cost savings opportunity compared with regadenoson.

Acute adverse events in cardiac MR imaging with gadolinium-based contrast agents: results from the European Society of Cardiovascular Radiology (ESCR) MRCT Registry in 72,839 patients

“…Across different pharmacological stressors, regadenoson and dobutamine showed an increased likelihood when compared to adenosine. In line with the recent literature, adverse event rates were higher among regadenoson and limited to mild and moderate events, mainly dyspnea [ 24 , 25 ]. This difference could be attributed to the pharmacokinetic properties of regadenoson with a comparably long, tri-phasic half-life time [ 23 ].…”

Intravenous regadenoson with aminophylline reversal is safe and equivalent to intravenous adenosine infusion for fractional flow reserve measurements

“…Though studies have shown that regadenoson is equivalent to adenosine with regards to FFR testing, there are significant cost differences between these pharmacological agents. Regadenoson with aminophylline is likely to be more expensive when compared to adenosine based on average wholesale pricing; however, the utility of regadenoson extends beyond cost alone. Although aminophylline is a safe and effective reversal agent for regadenoson, most patients would not require reversal given regadenoson's limited side effect profile.…”

Safety issues of compounds acting on adenosinergic signalling

“…Safety profile with no significant difference compared to adenosine [47] Capadenoson (partial A 1 AdR agonist) Reduced bradycardic adverse effects in preclinical models and no effect on heart rate in clinical studies [91] 2-CI-IB-MECA (selective A 3 AdR agonist) Impairment of oligodendrocytes through generation of ROS and mitochondrial membrane depolarization [51] Caffeine (non-selective AdR antagonist) Symptoms and signs of acute intoxications vary from weakness, vomiting, fever and seizure to life-threatening cerebral oedemas, arrhythmias, electrolyte disturbances and death [64] Chronic exposure leads to caffeine tolerance and after termination of consumption typical withdrawal symptoms occur [60] Developmental toxicity and influences on lactation performance were reported in studies on experimental animals. Genotoxicity was demonstrated on lower organisms such as bacteria, fungi etc [30,[71][72][73][74] Rolofylline (selective A 1 AdR antagonist) Increased frequency of seizures and strokes in treated patients [22] 2-Amino-4-phenyl-8-pyrrolidin-1-ylmethyl-indeno [1,2-d]pyrimidin-5-one (dual acting A 2A AdR and A 1 AdR antagonist)…”

“…A 2A AdR selective agonists, like regadenoson and apadenoson, were developed to overcome adverse effects of adenosine in patients undergoing cardiac stress testing due to its non‐selective activity. Many clinical trials have been conducted to compare the safety profile of regadenoson and adenosine; however, there were no significant improvements in reducing frequencies of adverse effects . Recently, it has been shown that A 2A AdR activation increases blood–brain barrier permeability, which could be suitable for drug delivery into brain or could on the other side pose a risk for different chemicals to reach CNS …”

“…[7,33,35] improvements in reducing frequencies of adverse effects. [47] Recently, it has been shown that A 2A AdR activation increases blood-brain barrier permeability, which could be suitable for drug delivery into brain or could on the other side pose a risk for different chemicals to reach CNS. [48] A 2B AdR subtype is a special case of low-affinity receptor requiring lM concentrations of adenosine to be activated.…”