Regadenoson, sold under the brand name Lexiscan among others, is an A_2A

adenosine receptor The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a di ...

agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. It produces

hyperemia Hyperaemia (also hyperemia) is the increase of blood flow to different tissues in the body. It can have medical implications but is also a regulatory response, allowing change in blood supply to different tissues through vasodilation. Clinically, ...

quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging. The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects. Regadenoson was approved by the United States

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

on April 10, 2008, and is marketed by

Astellas Pharma is a Japanese multinational pharmaceutical company, formed on 1 April 2005 from the merger of and . On February 5, 2020, the company announced management changes effective from April 1, 2020. Astellas is a member of the Mitsubishi UFJ Fina ...

under the tradename Lexiscan. It is approved for use in the

European Union The European Union (EU) is a supranational political and economic union of member states that are located primarily in Europe. The union has a total area of and an estimated total population of about 447million. The EU has often been de ...

and under the name of Rapiscan. It is marketed by GE Healthcare and is sold in both the United Kingdom and Germany. Regadenoson was approved for use in the European Union in September 2010. Regadenoson has a two- to three-minute

biological half-life Biological half-life (also known as elimination half-life, pharmacologic half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the bl ...

, as compared with adenosine's ten-second half-life. As a result, regadenoson stress protocols use a single bolus, instead of the four- to six-minute continuous infusion that was needed with adenosine. Whereas the adenosine infusion is weight based (140 mcg/kg/minute), regadenoson is administered as a 0.4 mg/5mL preloaded syringe dose that is standard for all weights. Regadenoson stress tests are not affected by the presence of

beta blockers Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms, and to protect the heart from a second heart attack after a first heart attack ( secondary prevention). They are ...

, as regadenoson vasodilates via the adenosine pathway without stimulating beta adrenergic receptors. Regadenoson can temporarily disrupt the integrity of the blood–brain barrier by inhibiting P-glycoprotein function.

References

External links

* * Vasodilators Purines Pyrazoles Carboxamides Nucleosides Ribosides Adenosine receptor agonists {{cardiovascular-drug-stub