regadenoson
Injection, Solution · Intravenous
Uses
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.
Dosage and administration
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. Administer 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 injection. 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.
Dosage forms and strengths
Single-dose pre-filled syringe: clear, colorless solution containing regadenoson 0.4 mg/5 mL (0.08 mg/mL). Injection: Single-dose pre-filled syringe: 0.4 mg/5 mL (0.08 mg/mL) ( 3 ).
Contraindications
Do not administer regadenoson 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 to patients with: Second- or third-degree AV block, or sinus node dysfunction unless the patients have a functioning artificial pacemaker
Warnings and precautions
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, 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, 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, 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, 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 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 ( 5.8 ). Cerebrovascular Accident (Stroke). Hemorrhagic and ischemic cerebrovascular accidents have occurred ( 5.9 ). 5.1 Myocardial Ischemia Fatal and nonfatal myocardial infarction (MI), ventricular arrhythmias, and cardiac arrest have occurred following regadenoson. Avoid use in patients with symptoms or signs of acute myocardial ischemia, for example unstable angina or cardiovascular instability; these patients may be at greater risk of serious cardiovascular reactions to regadenoson. Cardiac resuscitation equipment and trained staff should be available before administering regadenoson. Adhere to the recommended duration of injection [ see Dosage and Administration ( 2 ) ]. As noted in an animal study, longer injection times may increase the duration and magnitude of increase in coronary blood flow [ see Clinical Pharmacology ( 12.2 ) ]. If serious reactions to regadenoson occur, consider the use of aminophylline, an adenosine antagonist, to shorten the duration of increased coronary blood flow induced by regadenoson [ see Overdosage ( 10 ) ]. 5.2 Sinoatrial and Atrioventricular Nodal Block Adenosine receptor agonists, including regadenoson, can depress the SA and AV nodes and may cause first-, second- or third-degree AV block, or sinus bradycardia requiring intervention. In clinical trials first-degree AV block (PR prolongation > 220 msec) developed in 3% of patients within 2 hours of regadenoson administration; transient second-degree AV block with one dropped beat was observed in one patient receiving regadenoson. In post-marketing experience, third-degree heart block and asystole within minutes of regadenoson administration have occurred [ see Adverse Reactions ( 6.2 ) ]. 5.3 Atrial Fibrillation/Atrial Flutter New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter have been reported following regadenoson [ see Adverse Reactions ( 6.2 ) ]. 5.4 Hypersensitivity, Including Anaphylaxis Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria and rashes have occurred. In clinical trials, hypersensitivity reactions were reported in fewer than 1 percent of patients [s ee Adverse Reactions ( 6.1 ) ]. Have personnel and resuscitative equipment immediately available. 5.5 Hypotension Adenosine receptor agonists, including regadenoson, induce arterial vasodilation and hypotension. In clinical trials, decreased systolic blood pressure (> 35 mm Hg) was observed in 7% of patients and decreased diastolic blood pressure (> 25 mm Hg) was observed in 4% of patients within 45 minutes of regadenoson administration. The risk of serious hypotension may be higher in patients with autonomic dysfunction, hypovolemia, left main coronary artery stenosis, stenotic valvular heart disease, pericarditis or pericardial effusions, or stenotic carotid artery disease with cerebrovascular insufficiency. In post-marketing experience, syncope, transient ischemic attacks and seizures have been observed [ see Adverse Reactions ( 6.2 ) ]. 5.6 Hypertension Administration of adenosine receptor agonists, including regadenoson, may result in clinically significant increases in blood pressure in some patients. Among patients who experienced an increase in blood pressure in clinical trials, the increase was observed within minutes of regadenoson administration. Most increases resolved within 10 to 15 minutes, but in some cases, increases were observed at 45 minutes following administration [ see Clinical Pharmacology ( 12.2 ) ]. In post-marketing experience, cases of potentially clinically significant hypertension have been reported, particularly with underlying hypertension and when low-level exercise was included in the MPI [ see Adverse Reactions ( 6.2 ) ].
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 are dyspnea, headache, flushing, chest discomfort, dizziness, angina pectoris, chest pain, and nausea. To report SUSPECTED ADVERSE REACTIONS, contact Indies Pharma Jamaica Limited at 1-855-463-4377 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. Overall, any adverse reaction occurred at similar rates between the study groups (80% for the regadenoson group and 83% for the Adenoscan group). Aminophylline was used to treat the reactions in 3% of patients in the regadenoson group and 2% of patients in the Adenoscan group. Most adverse reactions began soon after dosing, and generally resolved within approximately 15 minutes, except for headache which resolved in most patients within 30 minutes. Table 1 Adverse Reactions in Studies 1 and 2 Pooled (Frequency ≥ 5%) Regadenoson N = 1,337 Adenoscan N = 678 Dyspnea 28% 26% Headache 26% 17% Flushing 16% 25% Chest Discomfort 13% 18% Angina Pectoris or ST Segment Depression 12% 18% Dizziness 8% 7% Chest Pain 7% 10% Nausea 6% 6% Abdominal Discomfort 5% 2% Dysgeusia 5% 7% Feeling Hot 5% 8% ECG Abnormalities The frequency of rhythm or conduction abnormalities following regadenoson or Adenoscan is shown in Table 2 [ see Warnings and Precautions ( 5.2 ) ]. Table 2 Rhythm or Conduction Abnormalities* in Studies 1 and 2 Regadenoson N / N evaluable (%) Adenoscan N / N evaluable (%) Rhythm or conduction abnormalities † 332/1275 (26%) 192/645 (30%) Rhythm abnormalities 260/1275 (20%) 131/645 (20%) PACs 86/1274 (7%) 57/645 (9%) PVCs 179/1274 (14%) 79/645 (12%) First-degree AV block (PR prolongation > 220 msec) 34/1209 (3%) 43/618 (7%) Second-degree AV block 1/1209 (0.1%) 9/618 (1%) AV conduction abnormalities (other than AV blocks) 1/1209 (0.1%) 0/618 (0%) Ventricular conduction abnormalities 64/1152 (6%) 31/581 (5%) *12-lead ECGs were recorded before and for up to 2 hours after dosing. †includes rhythm abnormalities (PACs, PVCs, atrial fibrillation/flutter, wandering atrial pacemaker, supraventricular or ventricular arrhythmia) or conduction abnormalities, including AV block. Respiratory Abnormalities In a randomized, placebo-controlled trial of 999 patients with asthma (n = 532) or stable chronic obstructive pulmonary disease (n = 467), the overall incidence of pre-specified respiratory adverse reactions was greater in the regadenoson group compared to the placebo group (p < 0.001). Most respiratory adverse reactions resolved without therapy; a few patients received aminophylline or a short-acting bronchodilator. No differences were observed between treatment arms in the reduction of >15% from baseline at two-hours in FEV 1 (Table 3). Table 3 Respiratory Adverse Effects* Asthma Cohort Chronic Obstructive Pulmonary Disease (COPD) Cohort Regadenoson (N=356) Placebo (N=176) Regadenoson (N=316) Placebo (N=151) Overall Pre-specified Respiratory Adverse Reaction † 12.9% 2.3% 19.0% 4.0% Dyspnea 10.7% 1.1% 18.0% 2.6% Wheezing 3.1% 1.1% 0.9% 0.7% FEV 1 reduction >15% ‡ 1.1% 2.9% 4.2% 5.4% *All patients continued the use of their respiratory medications as prescribed prior to administration of regadenoson. †Patients may have reported more than one type of adverse reaction. Adverse reactions were collected up to 24 hours following drug administration. Pre-specified respiratory adverse reactions included dyspnea, wheezing, obstructive airway disorder, dyspnea exertional, and tachypnea. ‡Change from baseline at 2 hours. Renal Impairment In a randomized, placebo-controlled trial of 504 patients (regadenoson n=334 and placebo n=170) with a diagnosis or risk factors for coronary artery disease and NKFK/DOQI Stage III or IV renal impairment (defined as GFR 15-59 mL/min/1.73 m 2 ), no serious adverse events were reported through the 24-hour follow-up period. Inadequate Exercise Stress In an open-label, multi-center trial evaluating regadenoson administration following inadequate exercise stress, 1,147 patients were randomized into one of two groups. Each group underwent two regadenoson stress myocardial perfusion imaging (MPI) procedures.
Drug interactions
No formal pharmacokinetic drug interaction studies have been conducted with regadenoson. Methylxanthines, e.g., caffeine, aminophylline and theophylline, interfere with the activity of regadenoson ( 7.1 , 12.2 ). Aminophylline may be used to attenuate severe and/or persistent adverse reactions to regadenoson ( 7.1 , 10 ). Dipyridamole may increase the activity of regadenoson. When possible, withhold dipyridamole for at least two days prior to regadenoson 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.
Use in specific populations
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%). 8.6 Renal Impairment No dose adjustment is needed in patients with renal impairment including patients with end stage renal disease and/or dependent on dialysis [ see Pharmacokinetics ( 12.3 ) ] .
Overdosage
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 ) ].
Description
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] - 1h-pyrazol-1-yl} adenosine propane-1,2-diol. Its structural formula is: The molecular formula for regadenoson is C 15 H 18 N 8 O 5
• C 3 H 8 O 2 and its molecular weight is 466.45. Regadenoson injection 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 the equivalent of 0.08 mg regadenoson as regadenoson propylene glycol solvate, 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. regadenoson-structure
How supplied
Regadenoson injection is supplied as a sterile, preservative-free, clear and colorless solution containing 0.08 mg/mL regadenoson in the following package: Single-dose 5 mL pre-filled glass syringe (NDC 83032-001-02). Store at 20º to 25ºC (68º to 77ºF); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature].
Patient information
Drug Interaction 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 Warnings and Precautions ( 5.8 ) and Clinical Pharmacology ( 12.2 ) ]. Cardiovascular Advise patients that they may be at increased risk of fatal and nonfatal heart attacks, abnormal heart rhythms, cardiac arrest, significant increase or decrease in blood pressure, or cerebrovascular accidents (stroke) with the use of regadenoson [ see Warnings and Precautions ( 5.1 ), ( 5.3 ), ( 5.5 ), ( 5.6 ) and ( 5.9 ) ]. Hypersensitivity Inform patients that allergic reactions have been reported with regadenoson. Advise patients how to recognize such a reaction and when to seek medical attention [ see Warnings and Precautions ( 5.4 ) ]. Respiratory Advise patients with COPD or asthma about the need for administration of pre- and post-study bronchodilator therapy and to call their clinician if they experience any shortness of breath or difficulty breathing following an MPI study with regadenoson [ see Warnings and Precautions ( 5.7 ) ]. Seizures Advise patients that they may be at increased risk of seizures. Question patients about a history of seizures [ see Warnings and Precautions ( 5.8 ) ]. Lactation Advise a woman to pump and discard breast milk for 10 hours after regadenoson administration [ see Use in Specific Populations ( 8.2 ) ]. Brands listed are the trademarks of their respective owners. Manufactured by: Abryl Laboratories Private Limited, Village Bhagwanpur, Tehsil Dera Bassi, District Sahibzada Ajit Singh Nagar, Punjab – 140507, India Manufactured for: Indies Pharma Jamaica Limited Unit-5 Montego Bay Trade Center, Howard Cooke Boulevard Montego Bay Jamaica - West Indies Issued: 08/2024
Label text from the FDA structured product label by Indies Pharma Jamaica Limited (revised Dec 26, 2025). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Regadenoson in 10 products
- Regadenoson Anhydrous in 4 products
regadenoson NDC products (14)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 16729-477 | Regadenoson .08 mg/mL Injection, Solution | Accord Healthcare Inc. | ANDA |
| 60505-6116 | Regadenoson .08 mg/mL Injection, Solution | Apotex Corp. | ANDA |
| 60505-6288 | Regadenoson .08 mg/mL Injection, Solution | Apotex Corp. | ANDA |
| 36000-364 | Regadenoson .08 mg/mL Injection, Solution | Baxter Healthcare Corporation | ANDA |
| 43598-616 | Regadenoson Anhydrous .08 mg/mL Injection | Dr. Reddy's Laboratories Inc. | ANDA |
| 55150-443 | Regadenoson .08 mg/mL Injection | Eugia US LLC | ANDA |
| 68083-175 | Regadenoson .08 mg/mL Injection, Solution | Gland Pharma Limited | ANDA |
| 0641-6253 | Regadenoson Anhydrous .08 mg/mL Injection, Solution | Hikma Pharmaceuticals USA Inc. | ANDA |
| 0409-1401 | Regadenoson Anhydrous .08 mg/mL Injection, Solution | Hospira, Inc. | ANDA |
| 83032-001 | Regadenoson .08 mg/mL Injection, Solution | Indies Pharma Jamaica Limited | ANDA |
| 76329-3321 | Regadenoson Anhydrous .08 mg/mL Injection, Solution | International Medication Systems, Limited | ANDA |
| 85742-012 | Regadenoson .08 mg/mL Injection, Solution | Kanchan Healthcare Inc | ANDA |
| 10135-803 | Regadenoson .08 mg/mL Injection, Solution | Marlex Pharmaceuticals, Inc. | ANDA |
| 71288-201 | Regadenoson .08 mg/mL Injection, Solution | Meitheal Pharmaceuticals Inc. | ANDA |
regadenoson recalls
- D-0039-2025 Nov 13, 2024 · Class II · Ongoing
Labeling: Missing Label
Frequently asked questions
What is regadenoson used for?
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.
What are the side effects of regadenoson?
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 ) ]… See the full label for the complete list.
Who makes regadenoson?
regadenoson is listed by 13 labelers in the FDA NDC directory, including Accord Healthcare Inc., Apotex Corp., Baxter Healthcare Corporation, Dr. Reddy's Laboratories Inc..
Has regadenoson been recalled?
The FDA enforcement database lists 1 recall for regadenoson, most recently D-0039-2025 (class ii): Labeling: Missing Label