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Regadenoson

Generic name: regadenoson systemic

Brand names: Lexiscan

Dosage Forms

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 disodium dihydrate, propylene glycol]

Pharmacology

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/Pharmacodynamics

Distribution

11.5 L (Gordi, 2006)

Metabolism

Unknown

Excretion

Urine (57% as unchanged drug)

Time to Peak

Plasma: 1 to 4 minutes

Half-Life Elimination

Initial phase: 2 to 4 minutes; Intermediate phase: 30 minutes; Terminal phase: 2 hours

Use in Specific Populations

Special Populations: Renal Function Impairment

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

Special Populations Note

Body weight: Clearance increases with increased body weight.

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.

Contraindications

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

Dosage and Administration

Dosing: Adult

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

Dosing: Geriatric

Refer to adult dosing.

Administration

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.

Dietary Considerations

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

Storage

Store at 25°C (77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

Drug Interactions

Aminophylline: May diminish the vasodilatory effect of Regadenoson. Consider therapy modification

Caffeine and Caffeine Containing Products: May diminish the vasodilatory effect of Regadenoson. Management: Avoiding using caffeine or other methylxanthine containing products (e.g., theophylline) for at least 12 hours prior to the administration of regadenoson. Consider therapy modification

Dipyridamole: May enhance the adverse/toxic effect of Regadenoson. Specifically, adenosine mediated effects may be enhanced. Management: Avoid dipyridamole for 48 hours prior to the administration of regadenoson when possible. Consider therapy modification

Theophylline: May diminish the vasodilatory effect of Regadenoson. Consider therapy modification

Adverse Reactions

>10%:

Cardiovascular: Cardiac conduction disturbance (20% to 26%), tachycardia (22%), flushing (16%), ventricular premature contractions (14%), chest discomfort (13%), angina (≤12%), depression of ST segment on ECG (≤12%)

Central nervous system: Headache (26%)

Respiratory: Dyspnea (28%; COPD patients 18%; asthma patients 11%)

1% to 10%:

Cardiovascular: Atrial premature contractions (7%), chest pain (7%), systolic hypotension (7%; >35 mm Hg), ventricular conduction abnormalities (6%), systolic hypertension (5%; ≥180 mm Hg and ≥20 mm Hg from baseline), decreased diastolic blood pressure (4%; >25 mm Hg), first degree atrioventricular block (PR prolongation >220 msec; 3%)

Central nervous system: Dizziness (8%), feeling hot (5%)

Gastrointestinal: Nausea (6%), abdominal distress (5%), dysgeusia (5%)

Respiratory: Respiratory distress (13% to 19%; in patients with asthma or COPD), wheezing (3%)

<1%, postmarketing, and/or case reports: Abdominal pain, anaphylaxis, acute coronary syndrome, angioedema, asystole, atrioventricular conduction disturbance (other than AV blocks), bronchoconstriction, cardiac arrest, cerebrovascular accident (hemorrhagic and ischemic), diarrhea, fecal incontinence, heart block (including third-degree AV block), hypersensitivity reaction, hypertension, increased diastolic blood pressure (≥30 mm Hg), musculoskeletal pain, myalgia, myocardial infarction, oxygen desaturation, pharyngeal edema, prolonged Q-T interval on ECG (transient), respiratory arrest, second degree atrioventricular block, seizure, skin rash, supraventricular tachyrhythmia (includes atrial fibrillation or flutter), symptomatic hypotension, syncope, transient ischemic attacks, tremor, urticaria, ventricular arrhythmia, vomiting

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.

Concurrent drug therapy issues:

  • Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

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

Monitoring Parameters

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

Pregnancy

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

What is this drug used for?

  • It is used during a stress test of the heart.

Frequently reported side effects of this drug

  • Nausea
  • Abdominal pain
  • Sensation of warmth
  • Change in taste
  • Flushing

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

  • Severe cerebrovascular disease like change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or vision changes.
  • Chest pain
  • Severe dizziness
  • Passing out
  • Vision changes
  • Slow heartbeat
  • Fast heartbeat
  • Abnormal heartbeat
  • Severe headache
  • Seizures
  • Shortness of breath
  • Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Source: Wolters Kluwer Health. Last updated January 29, 2020.