Important: This page is general information, not medical advice. It does not recommend or prescribe any treatment. Always consult your doctor or pharmacist before starting, stopping or changing any medicine.
Quick facts
- Drug class
- Pharmacologic Cardiac Stress Test Agent [EPC], Adenosine Receptor Agonists [MoA]
- How it is given
- intravenous
- Type
- human prescription drug
We do not publish dosing. How much of this medicine to take, how often, and for how long depends on your age, weight, kidney and liver function, other conditions and other medicines. That is a decision for the person who prescribes or dispenses it. Follow the directions on your own pack and ask your pharmacist if anything is unclear.
What it is used to treat
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) .
About this medicine
Regadenoson is an A 2A adenosine receptor agonist that is a coronary vasodilator [see Clinical Pharmacology ( 12.1 ) ]. Regadenoson is chemically described as adenosine, 2-[4-[(methylamino)carbonyl]-1 H -pyrazol-1-yl].Its structural formula is: The molecular formula for regadenoson is C 15 H 18 N 8 O 5 and its molecular weight is 390.35. Regadenoson is a sterile, nonpyrogenic solution for intravenous injection. The solution is clear and colorless. Each 1 mL in the 5 mL pre-filled syringe contains 0.08 mg regadenoson on an anhydrous basis, 10.9 mg dibasic sodium phosphate dihydrate, 5.4 mg monobasic sodium phosphate monohydrate, 150 mg propylene glycol, 1 mg edetate disodium dihydrate, and Water for Injection, with pH between 6.3 and 7.7.
How it works
12.1 Mechanism of Action 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).
Who should not take it
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) .
Warnings and cautions
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) . Bronchoconstriction. Adenosine receptor agonists, including regadenoson injection, may induce dyspnea, bronchoconstriction and respiratory compromise in patients with chronic obstructive pulmonary disease (COPD) or asthma. Resuscitative measures should be available ( 5.7 ). Seizure. regadenoson injection may lower the seizure threshold. New onset or recurrence of convulsive seizures has occurred. Some seizures are prolonged and require urgent anticonvulsive management. Methylxanthine use is not recommended in patients who experience a seizure in association with regadenoson injection (5.8). […]
Reported side effects
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. Most of these patients received regadenoson in two clinical studies that enrolled patients who had no history of bronchospastic lung disease as well as no history of a cardiac conduction block of greater than first-degree AV block, except for patients with functioning artificial pacemakers. In these studies (Studies 1 and 2), 2,015 patients underwent myocardial perfusion imaging after administration of regadenoson (N = 1,337) or ADENOSCAN (N = 678). The population was 26–93 years of age (median 66 years), 70% male and primarily Caucasian (76% Caucasian, 7% African American, 9% Hispanic, 5% Asian). Table 1 shows the most frequently reported adverse reactions. […]
Interactions with other medicines
No formal pharmacokinetic drug interacion studies have been conducted with regadenoson. Methylxanthines, e.g., caffeine, aminophylline and theophylline, interfere with the activity of regadenoson injection (7.1, 12.2 ). Aminophylline may be used to attenuate severe and/or persistent adverse reactions to regadenoson injection (7.1, 10) . Dipyridamole may increase the activity of regadenoson injection. When possible, withhold dipyridamole for at least two days prior to regadenoson injection administration (7.1) . 7.1 Effects of Other Drugs on Regadenoson • Methylxanthines (e.g., caffeine, aminophylline and theophylline) are non-specific adenosine receptor antagonists that interfere with the vasodilation activity of regadenoson [see Clinical Pharmacology ( 12.2) and Patient Counseling Information ( 17) ]. Patients should avoid consumption of any products containing methylxanthines as well as any drugs containing theophylline or aminophylline for at least 12 hours before regadenoson administration. Aminophylline may be used to attenuate severe or persistent adverse reactions to regadenoson [see Overdosage ( 10 ) ]. • In clinical studies, regadenoson was administered to patients taking other cardioactive drugs (i.e., β- blockers, calcium channel blockers, ACE inhibitors, nitrates, cardiac glycosides, and angiotensin receptor blockers) without reported adverse reactions or apparent effects on efficacy. • Dipyridamole may change the effects of regadenoson. When possible, withhold dipyridamole for at least two days prior to regadenoson administration. 7.2 Effect of Regadenoson on Other Drugs Regadenoson does not inhibit the metabolism of substrates for CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 in human liver microsomes, indicating that it is unlikely to alter the pharmacokinetics of drugs metabolized by these cytochrome P450 enzymes. 7.1 Effects of Other Drugs on Regadenoson • Methylxanthines (e.g., caffeine, aminophylline and theophylline) are non-specific adenosine receptor antagonists that interfere with the vasodilation activity of regadenoson [see Clinical Pharmacology ( 12.2) and Patient Counseling Information ( 17) ]. […]
Use in specific groups
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. Because of the potential risk of serious cardiac reactions in the breastfed infant, advise the nursing mother to pump and discard breast milk for 10 hours after administration of regadenoson. 8.4 Pediatric Use Safety and effectiveness in pediatric patients have not been established. 8.5 Geriatric Use Of the 1,337 patients receiving regadenoson in Studies 1 and 2, 56% were 65 years of age and over and 24% were 75 years of age and over. Older patients (≥ 75 years of age) had a similar adverse event profile compared to younger patients (< 65 years of age), but had a higher incidence of hypotension (2% vs. ≤ 1%). […]
If too much is taken
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) ].
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This page is built from the openFDA record of the U.S. Food and Drug Administration's approved labelling for this product, effective 1 November 2022. Label text has been shortened and reformatted for readability; safety wording has not been altered in meaning. FDA labelling describes products approved in the United States — brand names, strengths, formulations and approved uses may differ in your country. Always read the leaflet that comes with your own pack. PocketsInfo is not affiliated with, and is not endorsed by, the FDA. Retrieved 2026-07-30.