Regadenoson

Regadenoson

Names
Trade names	Lexiscan, Rapiscan, others
Other names	CVT-3146, 1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]- N-methylpyrazole-4-carboxamide
IUPAC name 2-{4-[(methylamino)carbonyl]- 1H-pyrazol-1-yl}adenosine
Clinical data
Drug class	A2A adenosine receptor agonist
Main uses	Pharmacologic stress testing
Side effects	Dizziness, headache, ST segment changes, flushing, shortness of breath, chest pain
Pregnancy category	US: C (Risk not ruled out)
Routes of use	Intravenous
External links
AHFS/Drugs.com	Monograph
Legal
License data	EU EMA: by INN US DailyMed: Regadenoson US FDA: Regadenoson
Legal status	US: ℞-only In general: ℞ (Prescription only)
Chemical and physical data
Formula	C15H18N8O5
Molar mass	390.360 g·mol−1
3D model (JSmol)	Interactive image
SMILES CNC(=O)C1=CN(N=C1)C2=NC(=C3C(=N2)N(C=N3)[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)N
InChI InChI=1S/C15H18N8O5/c1-17-13(27)6-2-19-23(3-6)15-20-11(16)8-12(21-15)22(5-18-8)14-10(26)9(25)7(4-24)28-14/h2-3,5,7,9-10,14,24-26H,4H2,1H3,(H,17,27)(H2,16,20,21)/t7-,9-,10-,14-/m1/s1 N Key:LZPZPHGJDAGEJZ-AKAIJSEGSA-N N

Regadenoson, sold under the brand name Lexiscan among others, is a medication used for pharmacologic stress testing. It is used as part of radionuclide myocardial perfusion imaging. It is given by injection into a vein.

Common side effects include dizziness, headache, ST segment changes, flushing, shortness of breath, and chest pain. Other side effects may include seizures and anaphylaxis. It should not be used in people with low blood pressure or poorly controlled heart failure. It is an A_2A adenosine receptor agonist which results in vasodilation of blood vessels to the heart.

Regadenoson was approved for medical use in the United States in 2008 and Europe in 2010. In the United States it costs about 270 USD per dose as of 2021.

Medical uses

Dosage

It is given at a dose of 0.4 mg.

Chemistry

Regadenoson has a 2 to 3 minute biological half-life, as compared with adenosine's 10-second half-life. As a result, regadenoson stress protocols use a single bolus, instead of a 4-6 minute continuous infusion, which was needed with adenosine. Another difference is that adenosine infusion is weight based (140mcg/kg/minute), while with regadenoson, a 0.4 mg/5mL preloaded syringe dose is standard for all weights. Regadenoson stress tests are not affected by the presence of beta blockers, as regadenoson vasodilates via the adenosine pathway without stimulating beta adrenergic receptors.

External links

External sites:	US NLM: Regadenoson
Identifiers:	ATC code: C01EB21 (WHO) CAS Number: 313348-27-5 Y 875148-45-1 PubChem CID: 219024 IUPHAR/BPS: 5596 DrugBank: DB06213 N ChemSpider: 189859 N UNII: 7AXV542LZ4 KEGG: D05711 Y ChEMBL: ChEMBL1201750 N

• "FDA warns of rare but serious risk of heart attack and death with cardiac nuclear stress test drugs Lexiscan (regadenoson) and Adenoscan (adenosine)". U.S. Food and Drug Administration (FDA). 12 January 2017. Archived from the original on 19 September 2020. Retrieved 4 August 2020.