Trade Names:Lexiscan- Injection, solution 0.4 mg per 5 mL
Activates the A 2A adenosine receptor, producing coronary vasodilation and increasing coronary blood flow.
T max is 1 to 4 min after injection.
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).
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.Hepatic Function Impairment
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.Elderly
No dose adjustment is needed.Gender
Gender has minimal effects on the pharmacokinetics of regadenoson.Race
Race has minimal effects on the pharmacokinetics of regadenoson.Body weight
Cl increases with increased body weight.
For radionuclide myocardial perfusion imaging in patients unable to undergo adequate exercise stress.
Second- or third-degree AV block or sinus node dysfunction (unless patient has a functioning pacemaker).
IV 0.4 mg as a rapid (approximately 10 sec) injection into a peripheral vein.
Store at 59° to 86°F.
The effects of regadenoson may be altered. Withhold dipyridamole for at least 2 days prior to regadenoson administration.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.
None well documented.
Rhythm or conduction abnormalities (26%); angina pectoris or scapulothoracic segment depression (12%); ventricular conduction abnormalities (6%); first-degree AV block (3%).
Headache (26%); dizziness (8%).
Nausea (6%); abdominal discomfort, dysgeusia (5%); abdominal pain, diarrhea, fecal incontinence, vomiting (postmarketing).
Musculoskeletal pain, myalgia (postmarketing).
Dyspnea (28%); wheezing (postmarketing).
Chest discomfort (13%); chest pain (7%); feeling hot (5%).
Category C .
Safety and efficacy not established.
May have a higher incidence of hypotension.
Bronchoconstriction and respiratory compromise may occur.
Arterial vasodilation and hypotension may occur.
Fatal cardiac arrest, life-threatening ventricular arrhythmias, and MI may occur from ischemia induced by pharmacological stress agents.
Regadenoson may depress S-A and AV nodes and cause first-, second-, or third-degree AV block, or sinus bradycardia.
Dizziness, flushing, increased heart rate.
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