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Regadenoson: Drug information

Regadenoson: Drug information
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For additional information see "Regadenoson: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Lexiscan
Pharmacologic Category
  • Diagnostic Agent
Dosing: Adult
Myocardial perfusion imaging

Myocardial perfusion imaging: IV: 0.4 mg as a single dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Mild to severe impairment: No dosage adjustment necessary.

Dialysis: Dialyzable; no dosage adjustment necessary.

Dosing: Liver Impairment: Adult

No dosage adjustment necessary.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.

>10%:

Cardiovascular: Angina pectoris (≤12%), cardiac conduction disturbance (20% to 26%; including atrial fibrillation, atrial flutter, atrioventricular conduction disturbance [other than AV blocks: <1%], first-degree atrioventricular block [PR prolongation >220 msec: 3%], premature atrial contractions [7%], premature ventricular contractions [14%], second-degree atrioventricular block [<1%], supraventricular tachyarrhythmia, ventricular arrhythmia, ventricular conduction abnormalities [6%]), chest discomfort (13%), depression of ST segment on ECG (≤12%), flushing (16%)

Nervous system: Headache (26%)

Respiratory: Dyspnea (28%)

1% to 10%:

Cardiovascular: Chest pain (7%), decreased diastolic blood pressure (4%; >25 mm Hg), systolic hypotension (7%; >35 mm Hg)

Gastrointestinal: Abdominal distress (5%), dysgeusia (5%), nausea (6%)

Nervous system: Dizziness (8%), feeling hot (5%)

<1%: Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema)

Postmarketing:

Cardiovascular: Acute coronary syndrome, acute myocardial infarction (Shah 2013), asystole (Derbas 2019; Park 2023), cardiomyopathy (takotsubo; including decreased left ventricular ejection fraction, heart failure) (Farid 2020; Kalavakunta 2017), chest tightness (Ahmad 2021), complete atrioventricular block (Park 2023), increased ST segment on ECG (Shah 2013), left bundle branch block (Hamilton 2021), Prinzmetal angina (Fogelson 2022), prolonged QT interval on ECG, severe bradycardia (Derbas 2019), syncope, tachycardia (Hamilton 2021)

Gastrointestinal: Abdominal pain, diarrhea, fecal incontinence, vomiting

Nervous system: Cerebrovascular accident (including intracranial hemorrhage, ischemic stroke), seizure (Radwan 2019), shivering (Ahmad 2021), transient ischemic attacks, tremor

Neuromuscular & skeletal: Musculoskeletal pain, myalgia

Respiratory: Wheezing

Contraindications

Second- or third-degree atrioventricular (AV) block or sinus node dysfunction in patients without a functioning artificial pacemaker

Warnings/Precautions

Concerns related to adverse events:

• Atrial fibrillation/flutter: New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter has occurred.

• Cerebrovascular effects: Hemorrhagic and ischemic cerebrovascular accidents have occurred.

• Conduction disturbances: May depress SA and AV node conduction and may produce first-, second-, or third-degree heart block, or sinus bradycardia. Third-degree heart block and asystole within minutes of administration have been reported.

• Hypersensitivity reactions: Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, and other hypersensitivity reactions (eg, decreased oxygen saturation, hypotension, throat tightness, urticaria, rash) have occurred. Equipment for resuscitation and trained personnel experienced in handling serious hypersensitivity reactions should always be immediately available prior to administration.

• Hypertension: May produce clinically significant hypertension; typically within minutes of administration and usually resolves within 10 to 15 minutes. Effects may persist; in some patients, hypertension continued for 45 minutes after administration. Use with caution in patients with underlying hypertension, especially when low-level exercise is used during MPI.

• Hypotension: May induce arterial vasodilation and hypotension. Use with caution in patients with autonomic dysfunction, hypovolemia, left main coronary artery stenosis, pericarditis, pericardial effusion, stenotic valvular heart disease, or stenotic carotid artery disease with cerebrovascular insufficiency. Syncope and transient ischemic attacks have also been reported.

• Myocardial ischemia: Fatal and nonfatal myocardial infarction, ventricular arrhythmias, and cardiac arrest have occurred. Avoid use in patients with symptoms or signs of acute myocardial ischemia, unstable angina, or cardiovascular instability; these patients may be at increased risk of serious cardiovascular reactions. Equipment for resuscitation and trained personnel experienced in handling cardiac emergencies should always be immediately available prior to administration. Adhere to recommended duration of injection; longer injection times may increase duration and magnitude of coronary blood flow increase. If serious reactions occur, consider the use of aminophylline, an adenosine antagonist.

• Respiratory effects: May cause dyspnea, bronchoconstriction, and respiratory compromise. Equipment for resuscitation and appropriate bronchodilator (eg, albuterol) therapy should always be immediately available prior to administration.

Disease-related concerns:

• Seizure: May lower the seizure threshold; new-onset or recurrence of seizures, some prolonged, has occurred.

Special populations:

• Older adult: Use with caution; may have a higher incidence of regadenoson-induced hypotension.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intravenous:

Lexiscan: 0.4 mg/5 mL (5 mL) [contains edetate (edta) disodium dihydrate, propylene glycol]

Generic: 0.4 mg/5 mL (5 mL)

Solution, Intravenous [preservative free]:

Generic: 0.4 mg/5 mL (5 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Lexiscan Intravenous)

0.4 mg/5 mL (per mL): $61.86

Solution (Regadenoson Intravenous)

0.4 mg/5 mL (per mL): $4.80 - $60.06

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

IV: Administer within 10 seconds into a peripheral vein using a ≥22-gauge catheter or needle, followed immediately by a 5 mL saline flush. Wait 10 to 20 seconds, then administer the radionuclide myocardial perfusion imaging agent. The radionuclide may be injected directly into the same catheter as regadenoson.

Use: Labeled Indications

Radionuclide myocardial perfusion imaging: A pharmacologic stress agent for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Aminophylline: May decrease vasodilatory effects of Regadenoson. Aminophylline may increase neuroexcitatory and/or seizure-potentiating effects of Regadenoson. Management: Avoid using aminophylline or other methylxanthines (eg, caffeine) for at least 12 hours prior to the administration of regadenoson. Aminophylline may be administered after regadenoson to diminish adverse events. Monitor for seizures. Risk D: Consider Therapy Modification

Caffeine and Caffeine Containing Products: May decrease vasodilatory effects of Regadenoson. Management: Avoid use of caffeine and caffeine-containing products for at least 12 hours prior to regadenoson administration. Risk D: Consider Therapy Modification

Dipyridamole: May increase adverse/toxic effects of Regadenoson. Specifically, adenosine mediated effects may be enhanced. Management: Avoid dipyridamole for 48 hours prior to the administration of regadenoson when possible. Risk D: Consider Therapy Modification

Theophylline: May decrease vasodilatory effects of Regadenoson. Theophylline may increase neuroexcitatory and/or seizure-potentiating effects of Regadenoson. Management: Avoid using theophylline or other methylxanthines (eg, caffeine) for at least 12 hours prior to the administration of regadenoson. Methylxanthines may be administered after regadenoson to diminish adverse events. Monitor for seizures. Risk D: Consider Therapy Modification

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if regadenoson is excreted in breast milk. Due to the potential for serious adverse effects in the nursing infant, the manufacturer recommends interrupting nursing for 10 hours after administration.

Dietary Considerations

Avoid dietary caffeine for at least 12 hours prior to pharmacologic stress testing.

Monitoring Parameters

Heart rate, blood pressure, continuous cardiac monitoring, oxygen saturation

Mechanism of Action

Regadenoson, a low affinity agonist of the A2A adenosine receptor, increases coronary blood flow (CBF) and mimics the increase in CBF caused by exercise. Myocardial uptake of the radiopharmaceutical is proportional to CBF creating the contrast required to identify stenotic coronary arteries.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: 11.5 L (Gordi, 2006)

Metabolism: Unknown

Half-life elimination: Initial phase: 2 to 4 minutes; Intermediate phase: 30 minutes; Terminal phase: 2 hours

Time to peak, plasma: 1 to 4 minutes

Excretion: Urine (57% as unchanged drug)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function: Regadenoson clearance decreases in parallel with a reduction in creatinine clearance, resulting in increased elimination half-lives and AUC values.

Body weight: Clearance increases with increased body weight.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (BE) Belgium: Rapiscan;
  • (CH) Switzerland: Rapiscan;
  • (CZ) Czech Republic: Rapiscan;
  • (DE) Germany: Rapiscan;
  • (EE) Estonia: Rapiscan;
  • (ES) Spain: Rapiscan;
  • (FI) Finland: Rapiscan;
  • (FR) France: Rapiscan;
  • (GB) United Kingdom: Rapiscan;
  • (GR) Greece: Rapiscan;
  • (HU) Hungary: Rapiscan;
  • (IT) Italy: Rapiscan;
  • (NL) Netherlands: Rapiscan;
  • (NO) Norway: Rapiscan;
  • (PL) Poland: Rapiscan;
  • (SA) Saudi Arabia: Rapiscan;
  • (SE) Sweden: Rapiscan;
  • (SI) Slovenia: Rapiscan;
  • (SK) Slovakia: Rapiscan;
  • (TN) Tunisia: Rapiscan
  1. Ahmad T, Linares J, Valencia DN, Agarwal A. Severe shivering as an adverse effect of regadenoson myocardial perfusion imaging. Cureus. 2021;13(3):e14091. doi:10.7759/cureus.14091 [PubMed 33927915]
  2. American Society of Nuclear Cardiology, “Imaging Guidelines for Nuclear Cardiology Procedures: A Report of The American Society of Nuclear Cardiology Quality Assurance Committee,” J Nucl Cardiol, 2006, 13(6):e21-171.
  3. Derbas LA, Thomas GS, Medina CA, Abdel-Karim AA, Saeed IM, Bateman TM. Severe bradycardia and asystole following regadenoson in pharmacological myocardial perfusion imaging: cases and treatment recommendations. JACC Cardiovasc Imaging. 2019;12(7 Pt 1):1288-1290. doi:10.1016/j.jcmg.2019.01.017 [PubMed 30878433]
  4. Farid S, Ahsan M, Garcia-Garcia HM. Regadenoson cardiac stress test-induced takotsubo cardiomyopathy: a case report. Cureus. 2020;12(5):e8004. doi:10.7759/cureus.8004 [PubMed 32528746]
  5. Fogelson B, Livesay J, Johnson JH. Inferior myocardial infarction secondary to coronary artery vasospasm following regadenoson stress imaging. J Med Cases. 2022;13(1):11-14. doi:10.14740/jmc3850 [PubMed 35211229]
  6. Gordi T, Frohna P, Sun HL, et al. A population pharmacokinetic/pharmacodynamic analysis of regadenoson, an adenosine A2A-receptor agonist, in healthy male volunteers. Clin Pharmacokinet. 2006;45(12):1201-1212. [PubMed 17112296]
  7. Hamilton MD, Ezeh E, Suliman M, Saylor J, Thompson E. Stress test-induced left bundle branch block. Cureus. 2021;13(8):e17384. doi:10.7759/cureus.17384 [PubMed 34584794]
  8. Kalavakunta JK, Zoltowska DM, Agrawal Y, Gupta V. Regadenoson cardiac stress test-induced stress cardiomyopathy. BMJ Case Rep. 2017;2017:bcr2017221217. doi:10.1136/bcr-2017-221217 [PubMed 28798245]
  9. Lexiscan (regadenoson) [prescribing information]. Northbrook, IL: Astellas Pharma US Inc; May 2018.
  10. Park CS, Nadeem A. Advanced heart block and asystole after regadenoson infusion: when cautionary tales become reality. Cureus. 2023;15(12):e50787. doi:10.7759/cureus.50787 [PubMed 38239541]
  11. Radwan SS, Schwartz OG. Seizure: an adverse effect of regadenoson in myocardial perfusion imaging. Case Rep Cardiol. 2019;2019:6240605. doi:10.1155/2019/6240605 [PubMed 31089430]
  12. Shah S, Parra D, Rosenstein RS. Acute myocardial infarction during regadenoson myocardial perfusion imaging. Pharmacotherapy. 2013;33(6):e90-e95. doi:10.1002/phar.1238 [PubMed 23471769]
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