Regadenoson

Abstract

Single-photon emission computerized tomography for myocardial perfusion imaging (MPI) is a non-invasive technique. MPI is performed by subjecting the patient to exercise or by using a pharmacological stress agent. Regadenoson is a selective A 2A adenosine receptor agonist used when MPI with exercise is contraindicated. It binds to the A 2A receptor and stimulates adenylate cyclase, resulting in increased cAMP, which phosphorylates protein kinase A thereby opening the ATP-dependant potassium channels leading to hyperpolarization in the coronary vascular smooth muscle. After a single bolus dose of regadenoson 400 μg, a peak plasma concentration (C max) of 13.6 ng/mL is attained in 1-4 min, with a terminal half-life of 2 h. It has a quick onset, short duration sufficient enough for hyperemic response, with comparable efficacy to adenosine, but with fewer side-effects. The adverse effects of this drug are dyspnea, headache, flushing, chest pain and atrioventricular block. Regadenoson is used for MPI in patients with co-morbid conditions like mild-to-moderate reactive airway disease, obstructive lung disease and renal impairment.