Regadenoson

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

Pharmacology

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

Pharmacokinetics

Absorption

T _max is 1 to 4 min after injection.

Elimination

Terminal half-life is approximately 2 h. 57% of the dose is excreted unchanged in the urine (range, 19% to 77%), with an average plasma renal clearance around 450 mL/min (ie, in excess of the glomerular filtration rate).

Special Populations

Regadenoson Cl decreases in parallel with a reduction in creatinine Cl, resulting in increased elimination half-lives and AUC values. No dose adjustment is needed.

Pharmacokinetics have not been evaluated. Because more than 55% of the dose is excreted in the urine as unchanged drug and factors that decrease Cl do not affect the plasma concentration in the early stages after dosing when clinically meaningful pharmacologic effects are observed, no dose adjustment is needed.

No dose adjustment is needed.

Gender has minimal effects on the pharmacokinetics of regadenoson.

Race has minimal effects on the pharmacokinetics of regadenoson.

Cl increases with increased body weight.

Indications and Usage

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

Contraindications

Second- or third-degree AV block or sinus node dysfunction (unless patient has a functioning pacemaker).

Dosage and Administration

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 5 mL of saline flush 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.
• Visually inspect for particulate matter and discoloration; do not administer if the solution is discolored or contains particulate matter.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

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

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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

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

CNS

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

Dermatologic

Flushing (16%).

GI

Nausea (6%); abdominal discomfort, dysgeusia (5%); abdominal pain, diarrhea, fecal incontinence, vomiting (postmarketing).

Musculoskeletal

Musculoskeletal pain, myalgia (postmarketing).

Respiratory

Dyspnea (28%); wheezing (postmarketing).

Miscellaneous

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

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

May have a higher incidence of hypotension.

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 (S-A) and AV nodal block

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

Overdosage

Symptoms

Dizziness, flushing, increased heart rate.

Patient Information

• Advise patient that medication will be prepared and administered by a health care provider.
• 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.

Copyright © 2009 Wolters Kluwer Health.