Description

Simple

A medication used in imaging to help healthcare providers view blood flow through the heart.

Clinical

A coronary vasodilator used in radionuclide myocardial perfusion imaging (MPI).

Overview

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.

Pharmacology

Indication

Diagnostic agent for radionuclide myocardial perfusion imaging (MPI)

Pharmacodynamic

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 pr... Read more

Mechanism of action

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 A... Read more

Absorption

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

Protein binding

Information currently not available.

Volume of distribution

Central compartment: 11.5 L;Steady state: 78.7 L

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.

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

Route of elimination

58% of total regadenoson eliminate is via renal excretion

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;

Adverse Effects

Contraindications

  • Hypersensitivity:
    • false
  • Regions: US
  • Patient Conditions:
      • Name: Second- or third-degree AV block
      • Drugbank Id: DBCOND0108429
  • Hypersensitivity:
    • false
  • Regions: US
  • Patient Conditions:
      • Name: Sinus Node Dysfunction
      • Drugbank Id: DBCOND0037740

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Regadenoson
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
3-isobutyl-1-methyl-7H-xanthine
3-isobutyl-1-methyl-7H-xanthine may decrease effectiveness of Regadenoson as a diagnostic agent.
6-O-benzylguanine
6-O-benzylguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
7-Deazaguanine
7-Deazaguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
7,9-Dimethylguanine
7,9-Dimethylguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
8-azaguanine
8-azaguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
8-chlorotheophylline
8-chlorotheophylline may decrease effectiveness of Regadenoson as a diagnostic agent.
9-Deazaguanine
9-Deazaguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
9-Methylguanine
9-Methylguanine may decrease effectiveness of Regadenoson as a diagnostic agent.
Acefylline
Acefylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Aminophylline
Aminophylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Bamifylline
Bamifylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Bromotheophylline
Bromotheophylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Bufylline
Bufylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Cafedrine
Cafedrine may decrease effectiveness of Regadenoson as a diagnostic agent.
Caffeine
Caffeine may decrease effectiveness of Regadenoson as a diagnostic agent.
Dipyridamole
The risk or severity of adverse effects can be increased when Dipyridamole is combined with Regadenoson.
Doxofylline
Doxofylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Dyphylline
Dyphylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Etamiphylline
Etamiphylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Fenethylline
Fenethylline may decrease effectiveness of Regadenoson as a diagnostic agent.
3 References
  1. 1 . Mitka M: New stress test agents reduce adverse effects. JAMA. 2008 May 14;299(18):2140. doi: 10.1001/jama.299.18.2140.PubMed: 18477777
  2. 2 . Lieu HD, Shryock JC, von Mering GO, Gordi T, Blackburn B, Olmsted AW, Belardinelli L, Kerensky RA: Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans. J Nucl Cardiol. 2007 Jul;14(4):514-20.PubMed: 17679059
  3. 3 . Zoghbi GJ, Iskandrian AE: Selective adenosine agonists and myocardial perfusion imaging. J Nucl Cardiol. 2012 Feb;19(1):126-41. doi: 10.1007/s12350-011-9474-9.PubMed: 22130964