regadenoson (Rx)

>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

Contraindications

2/3° AV block or sinus node dysfunction (unless patient has a functioning pacemaker installed)

Cautions

Appropriate bronchodilator therapy and resuscitative measures should be available prior to and following therapy; adhere to recommended duration of injection; longer injection times may increase duration and magnitude of increase in coronary blood flow

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: No available data on therapy use in pregnant women to inform drug-associated risk; in animal reproduction studies, adverse developmental outcomes were observed with therapy administration to pregnant rats and rabbits during organogenesis only at doses that produced maternal toxicity

Lactation: There is no information on presence of regadenoson in human milk, effects on breastfed infant, or effects on milk production; because of potential risk of serious cardiac reactions in breastfed infant, advise nursing mother to pump and discard breast milk for 10 hr after therapy

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.

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