Regadenoson
Regadenoson Uses, Dosage, Side Effects, Food Interaction and all others data.
Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
Regadenoson rapidly increases coronary blood flow (CBF) which is sustained for a short duration. Mean average peak velocity increased to greater than twice baseline by 30 seconds and decreased to less than twice the baseline level within 10 minutes. Myocardial uptake of the radiopharmaceutical is proportional to (CBF). Regadenoson increases blood flow in normal coronary arteries but not in stenotic (blocked) arteries. The significance of this finding is that stenotic arteries will take up less of the radiopharmaceutical than normal coronary arteries, resulting in a signal that is less intense in these areas.
| Trade Name | Regadenoson |
| Availability | Prescription only |
| Generic | Regadenoson |
| Regadenoson Other Names | Regadenoson |
| Related Drugs | glucagon, adenosine, mannitol, dipyridamole, Tubersol, arginine, inulin, Lexiscan, Persantine |
| Weight | 0.4mg/5ml, |
| Type | Intravenous Solution, Intravenous |
| Formula | C15H18N8O5 |
| Weight | Average: 390.354 Monoisotopic: 390.140015726 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Regadenoson is a coronary vasodilator used in radionuclide myocardial perfusion imaging (MPI).
Diagnostic agent for radionuclide myocardial perfusion imaging (MPI)
How Regadenoson works
Regadenoson is an selective low-affinity (Ki= 1.3 µM) A2A receptor agonist that mimics the effects of adenosine in causing coronary vasodilatation and increasing myocardial blood flow. It is a very weak agonist of the A1 adenosine receptor (Ki > 16.5 µM). Furthermore, it has negligible affinity to A2B and A3 adenosine receptors. Regadenoson is undergoing trials for use in pharmacological stress tests. Adenosine slows conduction time through the A-V node, can interrupt the reentry pathways through the A-V node, and can restore normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT), including PSVT associated with Wolff-Parkinson-White Syndrome.
Toxicity
The most common (incidence ≥ 5%) adverse reactions to regadenoson are dyspnea, headache, flushing, chest discomfort, dizziness, angina pectoris, chest pain, and nausea. MTD (male, supine position): 20 µg/kg; MTD (male, standing position): 10 µg/kg;
Food Interaction
- Avoid caffeine. Do not consume caffeine for at least 12 hours before the administration of regadenoson as caffeine can reduce the ability to detect ischemic changes.
[Moderate] ADJUST DOSING INTERVAL: Caffeine and other xanthine derivatives are nonspecific, competitive antagonists of adenosine receptors.
As such, they may interfere with the vasodilating effect of regadenoson, an adenosine receptor agonist.
In a placebo-controlled study that assessed the effects of oral caffeine on regadenoson-induced increase in coronary flow reserve (CFR), healthy subjects who took caffeine 200 mg orally two hours prior to regadenoson administration exhibited a median CFR that was 92% that of subjects who took placebo.
The study was done using positron emission tomography with radiolabeled water.
MANAGEMENT: Patients should avoid consumption of caffeine-containing products for at least 12 hours prior to administration of regadenoson for myocardial perfusion imaging.
Regadenoson Disease Interaction
Major: MI, sinus/AV node dysfunctionModerate: arrhythmias, COPD/asthma, hypotension, seizures
Volume of Distribution
Central compartment: 11.5 L; Steady state: 78.7 L
Elimination Route
The pharmacokinetic profile of regadenoson is best described by a 3-compartment model.
T max, injection = 1 to 3 minutes;
Onset of pharmacodynamic response = 1 to 3 minutes;
E max 12.3 ng/mL
Half Life
Initial phase: 2-4 minutes; Intermediate phase: 30 minutes (this phase coincides with a loss of the pharmacodynamic effect); Terminal phase: 2 hours
Clearance
Average plasma renal clearance = 450 mL/min. As this value is larger than the glomerular filtration rate, this suggests occurrence of renal tubular secretion.
Elimination Route
58% of total regadenoson eliminate is via renal excretion
Innovators Monograph
You find simplified version here Regadenoson
