Regadenoson

Regadenoson is a low affinity agonist (K i ≈ 1.3 µM) for the A 2A adenosine receptor, with at least 10-fold lower affinity for the A 1 adenosine receptor (K i > 16.5 µM), and weak, if any, affinity for the A 2B and A 3 adenosine receptors. Activation of the A 2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow (CBF).

• Regadenoson injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress. Regadenoson injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress (1) .

• Do not administer regadenoson injection to patients with: Second- or third-degree AV block, or sinus node dysfunction unless these patients have a functioning artificial pacemaker [see Warnings and Precautions ( 5.2) ]. Do not administer regadenoson injection to patients with: · Second- or third-degree AV block, or · sinus node dysfunction unless the patients have a functioning artificial pacemaker (4) .contraindicated

The recommended dose of regadenoson injection is 5 mL (0.4 mg regadenoson) administered as an intravenous injection within 10 seconds. · Patients should be instructed to avoid consumption of any products containing methylxanthines, including caffeinated coffee, tea or other caffeinated beverages, caffeine-containing drug products, aminophylline and theophylline for at least 12 hours before a scheduled radionuclide MPI [see Drug Interactions ( 7.1) and Clinical Pharmacology ( 12.2) ] Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Do not administer regadenoson injection if it contains particulate matter or is discolored. Aminister regadenoson injection as an intravenous injection within 10 seconds into a peripheral vein using a 22 gauge or larger catheter or needle.· Administer a 5 mL saline flush immediately after the injection of regadenoson.· Administer the radionuclide myocardial perfusion imaging agent 10–20 seconds after the saline flush. The radionuclide may be injected directly into the same catheter as regadenoson injection. · The recommended dose of regadenoson injection is 5 mL (0.4 mg regadenoson) administered as an intravenous injection within 10 seconds; followed immediately by saline flush and radiopharmaceutical (2) .

Myocardial Ischemia. Fatal cardiac events have occurred. Avoid use in patients with symptoms or signs of acute myocardial ischemia, for example unstable angina or cardiovascular instability, who may be at greater risk. Cardiac resuscitation equipment and trained staff should be available before administration (5.1) . Sinoatrial (SA) and Atrioventricular (AV) Nodal Block. Adenosine receptor agonists, including regadenoson injection, can depress the SA and AV nodes and may cause first-, second- or third-degree AV block, or sinus bradycardia (5.2) . Atrial Fibrillation/Atrial Flutter. New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter have been reported (5.3) . Hypersensitivity, including anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria, and rashes have occurred. Have personnel and resuscitative equipment immediately available (5.4). Hypotension. Adenosine receptor agonists, including regadenoson injection, induce vasodilation and hypotension. The risk of serious hypotension may be higher in patients with autonomic dysfunction, stenotic valvular heart disease, pericarditis or pericardial effusions, stenotic carotid artery disease with cerebrovascular insufficiency, or hypovolemia (5.5) . Hypertension. Adenosine receptor agonists, including regadenoson injection, may induce clinically significant increases in blood pressure particularly in patients with a history of hypertension and when the MPI includes low level exercise (5.6) .

The following adverse reactions are discussed in more detail in other sections of the labeling. Myocardial Ischemia [see Warnings and Precautions ( 5.1 ) ] Sinoatrial and Atrioventricular Nodal Block [see Warnings and Precautions ( 5.2 ) ] Atrial Fibrillation/Atrial Flutter [see Warnings and Precautions ( 5.3 ) ] Hypersensitivity, Including Anaphylaxis [see Warnings and Precautions ( 5.4 ) ] Hypotension [see Warnings and Precautions ( 5.5 ) ] Hypertension [see Warnings and Precautions ( 5.6 ) ] Bronchoconstriction [see Warnings and Precautions ( 5.7 ) ] Seizure [see Warnings and Precautions ( 5.8 ) ] Cerebrovascular Accident (Stroke) [see Warnings and Precautions ( 5.9 ) ] The most common (incidence ≥ 5%) adverse reactions to regadenoson injection are dyspnea, headache, flushing, chest discomfort, dizziness, angina pectoris, chest pain, and nausea ( 6 ). To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy's Laboratories Inc., at 1-888-375-3784 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. During clinical development, 1,651 patients were exposed to regadenoson, with most receiving 0.4 mg as a rapid (≤ 10 seconds) intravenous injection.

8.1 Pregnancy Risk Summary There are no available data on regadenoson use in pregnant women to inform a drug-associated risk. In animal reproduction studies, adverse developmental outcomes were observed with the administration of regadenoson to pregnant rats and rabbits during organogenesis only at doses that produced maternal toxicity (see Data). In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data Reproductive studies in rats showed that regadenoson doses 10 and 20 times the maximum recommended human dose (MRHD) based on body surface area caused reduced fetal body weights and significant ossification delays in fore- and hind limb phalanges and metatarsals; maternal toxicity also occurred at these doses. Skeletal variations were increased in all treated groups. In rabbits, maternal toxicity occurred at regadenoson doses administered during organogenesis at 4 times the MRHD; however, there were no teratogenic effects in offspring at this dose. At higher doses, 12 and 20 times the MRHD, maternal toxicity occurred along with increased embryo-fetal loss and fetal malformations. 8.2 Lactation Risk Summary There is no information on the presence of regadenoson in human milk, the effects on the breastfed infant, or the effects on milk production.

Metabolism

In healthy subjects, the regadenoson plasma concentration-time profile is multi-exponential in nature and best characterized by 3-compartment model. The maximal plasma concentration of regadenoson is achieved within 1 to 4 minutes after injection of regadenoson and parallels the onset of the pharmacodynamic response.

Regadenoson overdosage may result in serious reactions [see Warnings and Precautions ( 5 )]. In a study of healthy volunteers, symptoms of flushing, dizziness and increased heart rate were assessed as intolerable at regadenoson doses greater than 0.02 mg/kg. Aminophylline to Reverse Effects Methylxanthines, such as caffeine, aminophylline, and theophylline, are competitive adenosine receptor antagonists and aminophylline has been used to terminate persistent pharmacodynamic effects. Aminophylline may be administered in doses ranging from 50 mg to 250 mg by slow intravenous injection (50 mg to 100 mg over 30–60 seconds). Methylxanthine use is not recommended in patients who experience a seizure in association with regadenoson administration [see Warnings and Precautions ( 5.8) ].

• Apr 10, 2008NDANDA022161Astellas
• Apr 11, 2022ANDAANDA207604Apotex
• Apr 11, 2022ANDAANDA212806Meitheal
• Apr 11, 2022ANDAANDA213210Dr Reddys
• May 23, 2022ANDAANDA214252Ims Ltd
• Jul 12, 2022ANDAANDA207320Gland
• Aug 31, 2022ANDAANDA214349Hospira
• Oct 26, 2022ANDAANDA216437Eugia Pharma

1. 1Nausea51011%
2. 2Dyspnoea4098.6%
3. 3Injection Site Extravasation3617.6%
4. 4Vomiting3587.6%
5. 5Headache3186.7%
6. 6Hypotension3156.7%
7. 7Cardiac Arrest2836.0%
8. 8Dizziness2745.8%
9. 9Seizure2565.4%
10. 10Chest Pain2334.9%
11. 11Blood Pressure Decreased2084.4%
12. 12Bradycardia1964.1%
13. 13Tremor1884.0%
14. 14Loss Of Consciousness1833.9%
15. 15Unresponsive To Stimuli1643.5%

The 10 most recently updated of 97 ClinicalTrials.gov registrations naming Regadenoson as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Technical Development of Cardiovascular Magnetic Resonance Imaging (CMR) Using a Low Specific Absorption Rate (SAR) Scanner System
  Recruiting · Interventional · 2,950 enrolled · National Heart, Lung, and Blood Institute (NHLBI)
  NCT03331380updated 2026-06-08
• Impact of Stress CT Myocardial Perfusion on Downstream Resources and Prognosis
  Active not recruiting · Interventional · 2,000 enrolled · Centro Cardiologico Monzino
  NCT03976921updated 2026-06-03
• The Multicenter Stress Cardiac Magnetic Resonance Quantitative Perfusion Imaging in the United States Study
  Recruiting · Interventional · 1,000 enrolled · Brigham and Women's Hospital
  NCT06854458updated 2026-06-03
• Safety and Accuracy of Regadenoson-Atropine Stress Echocardiography in CAD
  Terminated · Interventional · 45 enrolled · Henry Ford Health System
  NCT00894179updated 2026-05-22
• Improvement Assessment of Coronary Flow Dysfunction Using Fundamental Fluid Dynamics
  Active not recruiting · Observational · 68 enrolled · University of Cincinnati
  NCT01719016updated 2026-05-07
• Relationship Between Abnormal Myocardial Perfusion and Diastolic Dysfunction in Sickle Cell Disease Using PET
  Recruiting · Phase 2 · Interventional · 40 enrolled · St. Jude Children's Research Hospital
  NCT05583721updated 2026-05-06
• A Study to Evaluate the Safety and Pharmacokinetics of Regadenoson in Pediatric Patients
  Recruiting · Phase 1 · Phase 2 · Interventional · 54 enrolled · GE Healthcare
  NCT04604782updated 2026-05-06
• Allograft Dysfunction in Heart Transplant
  Recruiting · Phase 4 · Interventional · 376 enrolled · Paul Kim
  NCT03102125updated 2026-05-01
• Quantitative Analysis of Cardiac Muscle Perfusion
  Not yet recruiting · Interventional · 35 enrolled · St. Anne's University Hospital Brno, Czech Republic
  NCT07548879updated 2026-04-23
• Hyperpolarized 13C Pyruvate-MRI and FDG-PET in a Single Exam for the Prognosis of Ischemic Cardiomyopathy
  Recruiting · Observational · 15 enrolled · University of Texas Southwestern Medical Center
  NCT06814587updated 2026-02-27

Frequently asked questions

How does Regadenoson work?

Regadenoson is a low affinity agonist (K i ≈ 1.3 µM) for the A 2A adenosine receptor, with at least 10-fold lower affinity for the A 1 adenosine receptor (K i > 16.5 µM), and weak, if any, affinity for the A 2B and A 3 adenosine receptors. Activation of the A 2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow (CBF).

What is Regadenoson used for?

According to FDA labeling, Regadenoson carries indications including: Regadenoson injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress. Regadenoson injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress (1) .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Regadenoson?

Regadenoson is classified as Other cardiac preparations, Adenosine Receptor Agonist, Adenosine Receptor Agonists, Coronary Arterial Vasodilation, Decreased Blood Pressure, Positive Chronotropy.

What are the contraindications for Regadenoson?

Regadenoson labeling lists contraindications including: Do not administer regadenoson injection to patients with: Second- or third-degree AV block, or sinus node dysfunction unless these patients have a functioning artificial pacemaker [see Warnings and Precautions ( 5.2) ]. Do not administer regadenoson injection to patients with: · Second- or third-degree AV block, or · sinus node dysfunction unless the patients have a functioning artificial pacemaker (4) .. Always consult the full prescribing information and a clinician.