Regadenoson (2 brand names, 1 dosage form, 1 route)
Available dosage forms: SOLUTION.
Routes of administration: INTRAVENOUS.
Brand Names
- LEXISCAN
- REGADENOSON
Indications and Usage
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 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.
Contraindications
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) ].
Adverse Reactions
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) ]
Drug Interactions
No formal pharmacokinetic drug interaction studies have been conducted with regadenoson injection.
Mechanism of Action
Regadenoson is a low affinity agonist (Ki ≈ 1.3 µM) for the A2A adenosine receptor, with at least 10-fold lower affinity for the A1 adenosine receptor (Ki > 16.5 µM), and weak, if any, affinity for the A2B and A3 adenosine receptors. Activation of the A2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow (CBF).
Overdosage
Regadenoson injection 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 injection 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 injection administration [see Warnings and Precautions (5.8) ].