Regadenoson

(BAN, USAN, rINN)
Regadenoson Chemical formula
Synonyms: CVT-3146; Régadénoson; Regadenosón; Regadenosonum. 1-(6Amino-9zole-4-carboxamide monohydrate.
Cyrillic synonym: Регаденозон.

💊 Chemical information

Chemical formula: C15H18N8O5, H2O = 408.4.
CAS — 313348-27-5 (regadenoson); 875148-45-1 (regadenoson monohydrate).

💊 Adverse Effects, Treatment, and Precautions

As for Adenosine. Regadenoson may be used with caution in patients with asthma or chronic obstructive pulmonary disease.

💊 Interactions

As for Adenosine.

💊 Pharmacokinetics

After intravenous injection of regadenoson, peak plasma concentrations are reached within 1 to 4 minutes and decline in a multi-exponential fashion. The initial half-life is about 2 to 4 minutes, followed by an intermediate stage with a half-life of about 30 minutes, during which the pharmacodynamic effect is lost; the half-life during the terminal phase is about 2 hours. Regadenoson does not appear to be metabolised; about 57% of a dose is excreted unchanged in the urine.
1. Gordi T, et al. A population pharmacokinetic/pharmacodynamic analysis of regadenoson, an adenosine A -receptor agonist, in healthy male volunteers. Clin Pharmacokinet 2006; 45: 1201–12
2. Gordi T, et al. Regadenoson pharmacokinetics and tolerability in subjects with impaired renal function. J Clin Pharmacol 2007; 47: 825–33.

💊 Uses and Administration

Regadenoson has similar properties to adenosine but has a greater selectivity for the adenosine A2A-receptor. It is a coronary vasodilator and increases coronary blood flow and is used to provide a pharmacological stress as an adjunct to radionuclide myocardial perfusion imaging. It is given intravenously in a single dose of 400 micrograms by rapid injection over about 10 seconds, followed by 5 mL of sodium chloride 0.9%; the radionuclide should be given 10 to 20 seconds after the sodium chloride.
1. Hendel RC, et al. Initial clinical experience with regadenoson, a novel selective A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging. J Am Coll Cardiol 2005; 46: 2069–75
2. Iskandrian AE, 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.

💊 Preparations

Proprietary Preparations

USA: Lexiscan.
Published May 08, 2019.