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Regadenoson

Pronunciation: (re-ga-DEN-oh-son)
Class: Diagnostic aid

Trade Names:
Lexiscan
- Injection, solution 0.4 mg per 5 mL

Pharmacology

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Activates the A _2A adenosine receptor, producing coronary vasodilation and increasing coronary blood flow.

Pharmacokinetics

Absorption

C _max is 1 to 4 min after injection.

Metabolism

Unknown.

Elimination

Terminal t _½ is approximately 2 h.

Onset

1 to 4 min after injection.

Special Populations

Renal Function Impairment

No dose adjustment is needed.

Hepatic Function Impairment

No dose adjustment is needed.

Elderly

No dose adjustment is needed.

Age/Gender/Race

Age, gender, and race have minimal effects on the pharmacokinetics.

Indications and Usage

For radionuclide myocardial perfusion imaging in patients unable to undergo adequate exercise stress.

Contraindications

Second- or third-degree AV block; sinus node dysfunction.

Dosage and Administration

Adults

IV 0.4 mg as a rapid (approximately 10 sec) injection into a peripheral vein.

General Advice

Administer using a 22-gauge or larger catheter or needle.
Administer saline flush 5 mL immediately after the injection.
Administer the radionuclide myocardial perfusion imaging agent 10 to 20 sec after the saline flush. The radionuclide may be injected directly into the same catheter.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Methylxanthines (eg, caffeine, theophylline)

May interfere with the vasodilation activity of regadenoson. Patients should avoid consumption of any product containing methylxanthines for at least 12 h prior to regadenoson administration.

Dipyridamole

The effects of regadenoson may be altered. Withhold dipyridamole for at least 2 days prior to regadenoson administration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Rhythm abnormalities (26%); angina pectoris or scapulothoracic segment depression (12%); ventricular conduction abnormalities (6%); first-degree AV block (3%); AV conduction abnormalities (other than AV blocks), second-degree AV block (0.1%).

CNS

Headache (26%); dizziness (8%).

Dermatologic

Flushing (16%).

GI

Nausea (6%); abdominal discomfort, dysgeusia (5%).

Respiratory

Dyspnea (28%).

Miscellaneous

Chest discomfort (13%); chest pain (7%); feeling hot (5%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Bronchoconstriction

Bronchoconstriction and respiratory compromise may occur.

Hypotension

Arterial vasodilation and hypotension may occur.

Myocardial ischemia

Fatal cardiac arrest, life-threatening ventricular arrhythmias, and MI may occur from ischemia induced by pharmacological stress agents.

Sinuatrial (SA) and AV nodal block

Regadenoson may depress SA and AV nodes and cause first-, second-, or third-degree AV block, or sinus bradycardia.

Overdosage

Symptoms

Dizziness, flushing, increased heart rate.

Patient Information

Instruct patient to avoid consumption of products containing methylxanthines, including coffee, tea, caffeine-containing beverages or drugs, and theophylline, for at least 12 h prior to scheduled radionuclide myocardial perfusion imaging.
Caution patients with COPD or asthma to discuss respiratory history and bronchodilator therapy with health care provider before scheduling a myocardial perfusion imaging study.