REGADENOSON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REGADENOSON (REGADENOSON).
Regadenoson is a selective A2A adenosine receptor agonist, causing coronary vasodilation and increasing coronary blood flow in patients with normal coronary arteries. It is used as a pharmacologic stress agent for myocardial perfusion imaging.
| Metabolism | Primarily metabolized by deamination via adenosine deaminase to a less active metabolite; not significantly metabolized by CYP450 enzymes. |
| Excretion | Renal excretion is the primary route of elimination, accounting for approximately 57% of the dose as unchanged drug in urine. Fecal excretion accounts for approximately 19% as unchanged drug and metabolites. Biliary excretion is minimal. |
| Half-life | Terminal elimination half-life is approximately 20 minutes (range 10-30 minutes) following intravenous administration. Clinically, this short half-life allows for rapid resolution of pharmacodynamic effects (e.g., coronary hyperemia) after cessation of infusion. |
| Protein binding | Approximately 91% bound to plasma proteins, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 1.1 L/kg (range 0.8-1.4 L/kg), indicating extensive distribution into total body water and tissues, consistent with its hydrophilicity. |
| Bioavailability | Not applicable; regadenoson is administered only intravenously, resulting in 100% bioavailability by this route. No oral formulation exists. |
| Onset of Action | Intravenous bolus: Onset of coronary hyperemia occurs within 1-2 minutes. Continuous intravenous infusion: Onset within 2-3 minutes. |
| Duration of Action | Coronary hyperemia persists for approximately 4-10 minutes after discontinuation of intravenous infusion. The duration is sufficient for performing myocardial perfusion imaging (MPI) with radiotracer injection typically during peak hyperemia. |
0.4 mg intravenously as a single bolus over 10 seconds, followed by a 5 mL saline flush; for myocardial perfusion imaging, administer 0.4 mg IV bolus, wait 10-20 seconds, then inject radiotracer. Maximum single dose: 0.4 mg.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. Clinical studies included patients with eGFR <30 mL/min/1.73 m², no dose modification necessary. |
| Liver impairment | No dose adjustment required for hepatic impairment; however, use caution in patients with severe hepatic impairment (Child-Pugh class C) due to potential increased systemic exposure. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dosing. |
| Geriatric use | No specific dose adjustment; clinical studies included patients aged ≥65 years with no observed differences in safety or efficacy. Monitor for hypotension and arrhythmias due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REGADENOSON (REGADENOSON).
| Breastfeeding | It is not known whether regadenoson is excreted in human breast milk. No M/P ratio is available. Due to its short half-life (<5 minutes) and low systemic exposure, significant infant exposure is unlikely. However, caution is advised; nursing should be avoided for 4-6 hours after administration to minimize any potential effects. |
| Teratogenic Risk | Regadenoson is a pregnancy category C drug. There are no adequate and well-controlled studies in pregnant women. In animal studies, regadenoson did not cause fetal harm at doses up to 20 times the maximum recommended human dose. However, because adenosine receptor agonists can cause hemodynamic effects (hypotension, tachycardia) that may reduce uterine blood flow, use during pregnancy is not recommended unless clearly needed. First trimester risks are unknown; second and third trimester use may be associated with transient fetal bradycardia due to adenosine-mediated AV blockade. |
■ FDA Black Box Warning
Fatal cardiac events: Risk of myocardial infarction, cardiac arrest, and death. Do not use in patients with signs or symptoms of acute myocardial ischemia or unstable angina. Resuscitation equipment and trained staff should be available.
| Serious Effects |
["Known hypersensitivity to regadenoson","Second- or third-degree AV block (unless functioning artificial pacemaker)","Sinus node dysfunction (unless functioning artificial pacemaker)","Unstable angina or acute coronary syndrome","Severe hypotension (systolic BP <90 mmHg)","Decompensated heart failure","Uncorrected electrolyte imbalances (e.g., hypokalemia, hypomagnesemia)","QT prolongation (congenital or acquired)","Concomitant use with dipyridamole (may increase risk of severe hypotension)"]
| Precautions | ["Risk of myocardial ischemia and cardiac arrest","Adenosine receptor antagonist (e.g., aminophylline) may be needed to reverse adverse effects","Increased risk in patients with unstable angina, recent MI, or unexplained syncope","Risk of seizures, especially in patients with epilepsy","Hypotension and bradycardia","AV block","Risk of bronchoconstriction in patients with asthma or COPD","Familial QT syndrome (may prolong QT interval)","Extra caution in patients with hepatic impairment","Contraindicated in patients with second- or third-degree AV block or sinus node dysfunction unless paced"] |
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| Fetal Monitoring | Continuous ECG and blood pressure monitoring is required during regadenoson administration. Fetal heart rate monitoring should be considered if used during pregnancy due to risk of transient fetal bradycardia. Monitor for signs of myocardial ischemia, hypotension, and bronchospasm. |
| Fertility Effects | No human studies on fertility are available. Animal studies with regadenoson did not show impaired fertility at doses up to 20 times the MRHD. |