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Regadenoson
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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 A2Aadenosine receptor agonist used when MPI with exercise is contraindicated. It binds to the A2Areceptor 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 (Cmax) 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.
Ovid Technologies (Wolters Kluwer Health)
Title: Regadenoson
Description:
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 A2Aadenosine receptor agonist used when MPI with exercise is contraindicated.
It binds to the A2Areceptor 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 (Cmax) 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.
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