Myocardial perfusion imaging: IV: 0.4 mg as a single dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Mild to severe impairment: No dosage adjustment necessary.
Dialysis: Dialyzable; no dosage adjustment necessary.
No dosage adjustment necessary.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Lexiscan: 0.4 mg/5 mL (5 mL) [contains edetate (edta) disodium dihydrate, propylene glycol]
No
IV: Administer within 10 seconds into a peripheral vein using a ≥22-gauge catheter or needle, followed immediately by a 5 mL saline flush. Wait 10 to 20 seconds, then administer the radionuclide myocardial perfusion imaging agent. The radionuclide may be injected directly into the same catheter as regadenoson.
Radionuclide myocardial perfusion imaging: A pharmacologic stress agent for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Cardiovascular: Cardiac conduction disturbance (20% to 26%), tachycardia (22%), flushing (16%), ventricular premature contractions (14%), chest discomfort (13%), angina (≤12%), depression of ST segment on ECG (≤12%)
Central nervous system: Headache (26%)
Respiratory: Dyspnea (28%; COPD patients 18%; asthma patients 11%)
1% to 10%:
Cardiovascular: Atrial premature contractions (7%), chest pain (7%), systolic hypotension (7%; >35 mm Hg), ventricular conduction abnormalities (6%), systolic hypertension (5%; ≥180 mm Hg and ≥20 mm Hg from baseline), decreased diastolic blood pressure (4%; >25 mm Hg), first degree atrioventricular block (PR prolongation >220 msec; 3%)
Central nervous system: Dizziness (8%), feeling hot (5%)
Gastrointestinal: Nausea (6%), abdominal distress (5%), dysgeusia (5%)
Respiratory: Respiratory distress (13% to 19%; in patients with asthma or COPD), wheezing (3%)
<1%, postmarketing, and/or case reports: Abdominal pain, anaphylaxis, acute coronary syndrome, angioedema, asystole, atrioventricular conduction disturbance (other than AV blocks), bronchoconstriction, cardiac arrest, cerebrovascular accident (hemorrhagic and ischemic), diarrhea, fecal incontinence, heart block (including third-degree AV block), hypersensitivity reaction, hypertension, increased diastolic blood pressure (≥30 mm Hg), musculoskeletal pain, myalgia, myocardial infarction, oxygen desaturation, pharyngeal edema, prolonged QT interval on ECG (transient), respiratory arrest, second degree atrioventricular block, seizure, skin rash, supraventricular tachyrhythmia (includes atrial fibrillation or flutter), symptomatic hypotension, syncope, transient ischemic attacks, tremor, urticaria, ventricular arrhythmia, vomiting
Second- or third-degree atrioventricular (AV) block or sinus node dysfunction in patients without a functioning artificial pacemaker
Concerns related to adverse events:
• Atrial fibrillation/flutter: New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter has occurred.
• Cerebrovascular effects: Hemorrhagic and ischemic cerebrovascular accidents have occurred.
• Conduction disturbances: May depress SA and AV node conduction and may produce first-, second-, or third-degree heart block, or sinus bradycardia. Third-degree heart block and asystole within minutes of administration have been reported.
• Hypersensitivity reactions: Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, and other hypersensitivity reactions (eg, decreased oxygen saturation, hypotension, throat tightness, urticaria, rash) have occurred. Equipment for resuscitation and trained personnel experienced in handling serious hypersensitivity reactions should always be immediately available prior to administration.
• Hypertension: May produce clinically significant hypertension; typically within minutes of administration and usually resolves within 10 to 15 minutes. Effects may persist; in some patients, hypertension continued for 45 minutes after administration. Use with caution in patients with underlying hypertension, especially when low-level exercise is used during MPI.
• Hypotension: May induce arterial vasodilation and hypotension. Use with caution in patients with autonomic dysfunction, hypovolemia, left main coronary artery stenosis, pericarditis, pericardial effusion, stenotic valvular heart disease, or stenotic carotid artery disease with cerebrovascular insufficiency. Syncope and transient ischemic attacks have also been reported.
• Myocardial ischemia: Fatal and nonfatal myocardial infarction, ventricular arrhythmias, and cardiac arrest have occurred. Avoid use in patients with symptoms or signs of acute myocardial ischemia, unstable angina, or cardiovascular instability; these patients may be at increased risk of serious cardiovascular reactions. Equipment for resuscitation and trained personnel experienced in handling cardiac emergencies should always be immediately available prior to administration. Adhere to recommended duration of injection; longer injection times may increase duration and magnitude of coronary blood flow increase. If serious reactions occur, consider the use of aminophylline, an adenosine antagonist.
• Respiratory effects: May cause dyspnea, bronchoconstriction, and respiratory compromise. Equipment for resuscitation and appropriate bronchodilator (eg, albuterol) therapy should always be immediately available prior to administration.
Disease-related concerns:
• Seizure: May lower the seizure threshold; new-onset or recurrence of seizures, some prolonged, has occurred.
Special populations:
• Elderly: Use with caution; may have a higher incidence of regadenoson-induced hypotension.
None known.
Aminophylline: May enhance the neuroexcitatory and/or seizure-potentiating effect of Regadenoson. Aminophylline may diminish the vasodilatory effect of Regadenoson. Management: Avoid using aminophylline or other methylxanthines (eg, caffeine) for at least 12 hours prior to the administration of regadenoson. Aminophylline may be administered after regadenoson to diminish adverse events. Monitor for seizures. Risk D: Consider therapy modification
Caffeine and Caffeine Containing Products: May diminish the vasodilatory effect of Regadenoson. Management: Avoiding using caffeine or other methylxanthine containing products (e.g., theophylline) for at least 12 hours prior to the administration of regadenoson. Risk D: Consider therapy modification
Dipyridamole: May enhance the adverse/toxic effect of Regadenoson. Specifically, adenosine mediated effects may be enhanced. Management: Avoid dipyridamole for 48 hours prior to the administration of regadenoson when possible. Risk D: Consider therapy modification
Theophylline: May enhance the neuroexcitatory and/or seizure-potentiating effect of Regadenoson. Theophylline may diminish the vasodilatory effect of Regadenoson. Management: Avoid using theophylline or other methylxanthines (eg, caffeine) for at least 12 hours prior to the administration of regadenoson. Methylxanthines may be administered after regadenoson to diminish adverse events. Monitor for seizures. Risk D: Consider therapy modification
Adverse events have been observed in animal reproduction studies.
It is not known if regadenoson is excreted in breast milk. Due to the potential for serious adverse effects in the nursing infant, the manufacturer recommends interrupting nursing for 10 hours after administration.
Avoid dietary caffeine for at least 12 hours prior to pharmacologic stress testing.
Heart rate, blood pressure, continuous cardiac monitoring, oxygen saturation
Regadenoson, a low affinity agonist of the A2A adenosine receptor, increases coronary blood flow (CBF) and mimics the increase in CBF caused by exercise. Myocardial uptake of the radiopharmaceutical is proportional to CBF creating the contrast required to identify stenotic coronary arteries.
Distribution: 11.5 L (Gordi, 2006)
Metabolism: Unknown
Half-life elimination: Initial phase: 2 to 4 minutes; Intermediate phase: 30 minutes; Terminal phase: 2 hours
Time to peak, plasma: 1 to 4 minutes
Excretion: Urine (57% as unchanged drug)
Renal function impairment: Regadenoson clearance decreases in parallel with a reduction in creatinine clearance, resulting in increased elimination half-lives and AUC values.
Body weight: Clearance increases with increased body weight.
Solution (Lexiscan Intravenous)
0.4 mg/5 mL (per mL): $60.06
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