Relugolix – Description
- Regadenoson is an A2A adenosine receptor agonist that acts as a coronary vasodilator and is used as a pharmacologic stress agent in radionuclide myocardial perfusion imaging.
- Regadenoson can be used as an alternative to adenosine for diagnosing coronary artery disease. Although similar in activity to adenosine, there is an increased ease of use with regadenoson as it is given as a rapid intravenous injection vs. the infusion used in adenosine-facilitated perfusion imaging studies. Initial studies have shown adverse events rates to be similar to adenosine; however, regadenoson has an increased selectivity for the A2A adenosine receptor and lower affinity for the A1, A2B, and A3 receptors as compared to adenosine.
- The activation of the non-A2A adenosine receptors are often implicated in high-degree AV block and bronchoconstriction.
- Additionally, studies comparing the images obtained with regadenoson to those obtained with adenosine demonstrate that they are similar in assessing the extent of reversible perfusion abnormalities (62% +/- 2% and 63% +/-3% vs. 61% +/- 3% and 64% +/-4%, respectively). Regadenoson was FDA-approved in April 2008.3390633907
Indications & Dosage
- coronary artery disease diagnosis
For use in radionuclide myocardial perfusion imaging for coronary artery disease diagnosis in patients unable to undergo adequate exercise stress
Intravenous dosage
Adults:
0.4 mg IV once.33906
Maximum Dosage Limits:
•Adults
0.4 mg IV single dose.
•Geriatric
0.4 mg IV single dose.
•Adolescents
Safety and efficacy have not been established.
•Children
Safety and efficacy have not been established.
•Infants
Safety and efficacy have not been established.
•Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
- AV block
- bradycardia
- sick sinus syndrome
Precautions
- angina
- asthma
- autonomic neuropathy
- breast-feeding
- cardiac arrest
- cardiac disease
- chronic obstructive pulmonary disease
- geriatric
- hypotension
- hypovolemia
- myocardial infarction
- pericardial effusion
- pericarditis
- pregnancy
- pulmonary disease
- pulmonary edema
- respiratory arrest
- seizures
- valvular heart disease
- ventricular fibrillation
Pregnancy
- There are no data describing regadenoson use in human pregnancy to inform a drug-associated risk. Adverse developmental outcomes were observed in animal reproductive studies.
- Regadenoson doses at 10- to 20-times the maximum recommended human dose (MRHD) caused reduced fetal body weights, ossification delays in limb phalanges and metatarsals, and maternal toxicity.
- Maternal toxicity occurred in rabbits at doses 4-times the MRHD; maternal toxicity, increased embryo-fetal loss, and fetal malformations were noted with regadenoson doses 12- and 20-times the MRHD.33906
Lactation
- There is no information on the presence of regadenoson in human milk or the effects of regadenoson on the breast-fed infant or milk production.
- Because of the potential risk of serious cardiac reactions in the breast-fed infant, advise the breast-feeding mother to pump and discard breast milk for 10 hours after regadenoson administration.33906
Interactions
- Acetaminophen; Aspirin, ASA; Caffeine
- Acetaminophen; Caffeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Caffeine; Pyrilamine
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Caffeine
- Aspirin, ASA; Caffeine; Orphenadrine
- Aspirin, ASA; Dipyridamole
- Butalbital; Acetaminophen; Caffeine
- Butalbital; Acetaminophen; Caffeine; Codeine
- Butalbital; Aspirin; Caffeine; Codeine
- Caffeine
- Caffeine; Sodium Benzoate
- Digoxin
- Dipyridamole
- Ergotamine; Caffeine
- Green Tea
- Nicotine
- Theophylline, Aminophylline
- Trandolapril; Verapamil
- Verapamil
Adverse Reactions
- abdominal pain
- anaphylactic shock
- anaphylactoid reactions
- angina
- angioedema
- asystole
- atrial fibrillation
- atrial flutter
- AV block
- back pain
- bradycardia
- bronchospasm
- cardiac arrest
- chest pain (unspecified)
- diarrhea
- dizziness
- dysgeusia
- dyspnea
- fecal incontinence
- flushing
- headache
- hypertension
- hypotension
- intracranial bleeding
- musculoskeletal pain
- myalgia
- myocardial infarction
- nausea
- premature atrial contractions (PACs)
- premature ventricular contractions (PVCs)
- QT prolongation
- rash
- respiratory arrest
- seizures
- sinus tachycardia
- stroke
- syncope
- tachypnea
- tremor
- urticaria
- vomiting
- wheezing
Monitoring Parameters
- ECG
Classifications
- Diagnostic Agents
- Diagnostic Agents, Other
Global Drug Names
- Austria
- Rapiscan – (GE Healthcare)
- Belgium
- Rapiscan – (GE Healthcare)
- Czech Republic
- Rapiscan – (GE Healthcare)
- Denmark
- Rapiscan – (Dupharma)
- Finland
- Rapiscan – (GE Healthcare)
- France
- Rapiscan – (Mallinckrodt)
- Greece
- Rapiscan – (Rapidscan)
- Ireland
- Rapiscan – (GE Healthcare)
- Netherlands
- Rapiscan – (Rapidscan)
- Norway
- Rapiscan – (GE Healthcare)
- Poland
- Rapiscan – (Gilead)
- Portugal
- Rapiscan – (Rapidscan)
- Spain
- Rapiscan – (Rapidscan)
- Sweden
- Rapiscan – (GE Healthcare)
- Switzerland
- Rapiscan – (GE Healthcare)
- United Kingdom
- Rapiscan – (Rapidscan)
References
10759.Lexiscan (regadenoson) package insert. Northbrook, IL: Astellas Pharma; 2018 May.
10762.Gaemperli O, Schepis T, Koepfli P, et al. Interaction of caffeine with regadenoson-induced hyperemic myocardial blood flow as measured by positron emission tomography: a randomized, double-blind, placebo-controlled crossover trial. J Am Coll Cardiol 2008;51:328-9.
10764.Zhao G, Messina E, Xu X, et al. Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonist. J Cardiovasc Pharmacol 2007;49:369-75
10765.Lapeyre AC, Goraya TY, Johnston DL, et al. The impact of caffeine on vasodilator stress perfusion studies. J Nucl Cardiol 2004;11:506-11.
10766.Namdar M, Koepfli P, Grathwohl R, et al. Caffeine decreases exercise-induced myocardial flow reserve. J Am Coll Cardiol 2006;47:405-10.
28438.Persantine (dipyridamole) package insert. Ridgefield, CT: Boehringer Ingelheim Pharmaceuticals, Inc.; 2003 May.
29325.Adenocard (adenosine) package insert. Northbrook, IL: Astellas Pharma US, Inc.; 2019 Dec.
29326.Sylven C, Beermann B, Kaijser L, et al. Nicotine enhances angina pectoris-like chest pain and atrioventricular blockade provoked by intravenous bolus of adenosine in healthy volunteers. J Cardiovasc Pharmacol 1990;16:962-5.
33906.Lexiscan (regadenoson) package insert. Northbrook, IL: Astellas Pharma; 2018 May.
33907.Iskandrian AE, Bateman TM, Belardinelli L, et al. Adenosine versus regadenoson comparative evaluation in myocardial perfusion imaging: results of the ADVANCE phase 3 multicenter, international trial. J Nucl Cardiol 2007;14:645-58.
33908.Lieu HD, Shryock JC, von Mering GO, et al. Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans. J Nucl Cardiol 2007;14:514-20.
33910.Gordi T, Frohna P, Sun H, et al. A population pharmacokinetic/pharmacodynamic analysis of regadenoson, an adenosine A2A-receptor agonist, in healthy male volunteers. Clin Pharmacokinet 2006;45:1201-12.
56449.Food and Drug Administration (US FDA) Drug Safety Communication. FDA warns of rare but serious risk of heart attack and death with cardiac nuclear stress test drugs Lexiscan (regadenoson) and Adenoscan (adenosine). Retrieved Nov 20, 2013. Available on the World Wide Web at http://www.fda.gov/Drugs/DrugSafety/ucm375654.htm
71483.Institute for Safe Medication Practices (ISMP). Acute Care ISMP Medication Safety Alert. Regadenoson glass syringes may be incompatible with needleless connectors. 2024 Oct; 29(20):1-3.
