Regadenoson.
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.
Department of Pharmacology, Sri Devaraj Urs Medical College, Tamaka, Kolar, Karnataka, India.
G M
GM
Bengalorkar
K
K
Bhuvana
N
N
Sarala
T N
TN
Kumar
D058917:Adenosine A2 Receptor Antagonists / Q000009:adverse effects / Q000494:pharmacology*; D001783:Blood Flow Velocity / Q000187:drug effects; D003324:Coronary Artery Disease / Q000175:diagnosis*; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006940:Hyperemia / Q000139:chemically induced; D055414:Myocardial Perfusion Imaging / Q000379:methods; D011687:Purines / Q000009:adverse effects / Q000494:pharmacology*; D011720:Pyrazoles / Q000009:adverse effects / Q000494:pharmacology*; D013312:Stress, Physiological / Q000187:drug effects*; D014665:Vasodilator Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*
D058917:Adenosine A2 Receptor Antagonists; D011687:Purines; D011720:Pyrazoles; D014665:Vasodilator Agents; C430916:regadenoson