Dosing and uses of Lexiscan (regadenoson)
Adult dosage forms and strengths
intravenous solution
- 0.4mg/5mL
Pharmacologic Stress Agent
Indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress
5 mL (0.4 mg) IVp
Administration
Administer as rapid (~10 sec) injection into a peripheral vein using 22 gauge or larger catheter or needle
Inspect visually, prior to admin, DO NOT administer if discolored or particulate matter present
Administer 5 mL saline flush, immediately after
Administer radionuclide myocardial perfusion imaging agent 10-20 sec after saline flush
- Radionuclide may be injected directly into same catheter as regadenoson
Pediatric dosage forms and strengths
Safety and efficacy not established
Lexiscan (regadenoson) adverse (side) effects
>10%
Dyspnea (28%)
Headache (26%)
Rhythm conduction abnormalities (26%)
Flushing (16%)
PVCs (14%)
Chest Discomfort (13%)
Angina or ST segment depression (12%)
1-10%
Dizziness (8%)
Chest pain (7%)
PACs (7%)
Nausea (6%)
Ventricular conduction abnormalities (6%)
Abdominal discomfort (5%)
Dysgeusia (5%)
Feeling hot (5%)
First-degree AV block (3%)
<1%
Anaphylaxis, angioedema, cardiac arrest, respiratory arrest/distress, throat tightness, and urticaria/rashes, atrial fibrillation, seizures, cardiovascular accidents (stroke)
Postmarketing reports
Cardiovascular: Myocardial infarction, cardiac arrest, ventricular arrhythmias, supraventricular tachyarrhythmias including atrial fibrillation with rapid ventricular response (new-onset or recurrent), atrial flutter, heart block (including third-degree block), asystole, marked hypertension, symptomatic hypotension in association with transient ischemic attack, seizures and syncope
Central nervous system: Tremor, seizure, transient ischemic attack, and cerebrovascular accident including intracranial hemorrhage
Warnings
Contraindications
2/3° AV block or sinus node dysfunction (unless patient has a functioning pacemaker installed)
Cautions
Myocardial infarction
1° AV block
SA block
QT prolongation has occurred shortly after administration in postmarketing surveillence
Hypotension in association with transient ischemic attack, tremors, syncope, and seizures
Hypertension (transient) may occur following administration
Conduction disturbances; depresses SA and AV node conduction and may produce first, second, and third-degree heart block
Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria and rashes have occurred
Adenosine receptor agonists may cause dyspnea, bronchoconstriction, and respiratory compromise; caution with asthma or bronchoconstrictive disease
Nucleoside transport inhibitors (eg, dipyridamole) and potentiate the vasoactive effects of regadenoson; withhold for 5 half-lives before regadenoson administration
Methylxanthines (eg, caffeine, theophylline) are adenosine receptor antagonists and inhibit regadenoson’s vasoactive effects; withhold methylxanthines for 5 half-lives before regadenoson administration
Aminophylline may increase risk of seizures associated with regadenoson injection
May lower seizure threshold; new-onset or recurrence of convulsive seizures has occurred following regadenoson injection; some seizures are prolonged and require emergent anticonvulsive management
Hemorrhagic and ischemic cerebrovascular accidents have occurred
New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter reported
Risk for myocardial infarction and death
- Avoid use for cardiac nuclear stress tests in patients with signs or symptoms of acute myocardial ischemia (eg, unstable angina, cardiovascular instability); use may increase risk of fatal MI
- Screen all nuclear stress test candidates for risks
Pregnancy and lactation
Pregnancy category: C
Lactation: Not known whether excreted in breast milk, not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Lexiscan (regadenoson)
Mechanism of action
Low affinity agonist for the A2A adenosine receptor
Activation of the A2A adenosine receptor produces coronary vasodilation and increases coronary blood flow