Regadenoson

Regadenoson
Names
Trade namesLexiscan, Rapiscan, others
Other namesCVT-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 classA2A adenosine receptor agonist[1]
Main usesPharmacologic stress testing[2]
Side effectsDizziness, headache, ST segment changes, flushing, shortness of breath, chest pain[1]
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Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    use    		Intravenous
    External links
    AHFS/Drugs.comMonograph
    Legal
    License data
    Legal status
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Chemical and physical data
    FormulaC15H18N8O5
    Molar mass390.360 g·mol−1
    3D model (JSmol)
    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.[2] It is used as part of radionuclide myocardial perfusion imaging.[2] It is given by injection into a vein.[2]

    Common side effects include dizziness, headache, ST segment changes, flushing, shortness of breath, and chest pain.[1] Other side effects may include seizures and anaphylaxis.[2] It should not be used in people with low blood pressure or poorly controlled heart failure.[1] It is an A2A adenosine receptor agonist which results in vasodilation of blood vessels to the heart. [1]

    Regadenoson was approved for medical use in the United States in 2008 and Europe in 2010.[3][1] In the United States it costs about 270 USD per dose as of 2021.[4]

    Medical uses

    Dosage

    It is given at a dose of 0.4 mg.[1]

    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.

    References

    1. 1 2 3 4 5 6 7 "Rapiscan EPAR". European Medicines Agency. Archived from the original on 11 August 2020. Retrieved 3 May 2020.
    2. 1 2 3 4 5 "Regadenoson Monograph for Professionals". Drugs.com. Archived from the original on 4 March 2021. Retrieved 16 October 2021.
    3. ↑ "DailyMed - LEXISCAN- regadenoson injection, solution". dailymed.nlm.nih.gov. Archived from the original on 17 October 2021. Retrieved 16 October 2021.
    4. ↑ "Lexiscan Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 16 October 2021.
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