regadenoson

Action and Spectrum

Actions and Spectrum: 

The main action of regadenoson is to cause coronary artery dilation (widening), which increases blood flow to the heart. 

Drug Interaction

Adverse Reaction

>10%: 

Dyspnea (28%) 

Flushing (16%) 

Chest Discomfort (13%) 

PVCs (14%) 

ST segment depression (12%) 

Rhythm conduction abnormalities (26%) 

Headache (26%) 

1-10%: 

Chest pain (7%) 

Abdominal discomfort (5%) 

Ventricular conduction abnormalities (6%) 

Feeling hot (5%) 

Dysgeusia (5%) 

First-degree AV block (3%) 

Dizziness (8%) 

<1%: 

Angioedema 

Throat tightness 

Anaphylaxis 

Seizures 

Cardiac arrest 

Black Box Warning

Black Box Warning: 

It is essential to follow the dosage and administration instructions for the medication carefully.

Contraindication / Caution

Contraindication/Caution: 

regadenoson should not be used in people hypersensitive to the drug itself. 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the usage of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the presence of the drug in breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology 

regadenoson is a selective adenosine receptor agonist. it binds and activates the A2A adenosine receptors in the heart and blood vessels. Adenosine is a naturally occurring compound that plays a role in regulating blood flow and heart rate. 

Pharmacodynamics: 

The pharmacodynamics of regadenoson involve binding to the A2A receptors, leading to the increase in blood flow to the heart and slowing heart rate, which provide a useful diagnostic tool to evaluate coronary artery disease. 

Pharmacokinetics:  

The pharmacokinetics of regadenoson involves absorption, distribution, metabolism, and elimination of the drug.  

Absorption 

regadenoson is administered as a single bolus injection and rapidly absorbed into the bloodstream. This rapid absorption is because regadenoson is a small molecule and can easily cross cell membranes. 

Distribution 

The peak plasma concentration (Cmax) is reached within 1-2 minutes after the injection. It is highly bound to plasma proteins and has a high volume of distribution. 

Metabolism 

regadenoson is metabolized by the liver’s enzyme adenosine deaminase (ADA). ADA converts regadenoson to inosine, which does not have any pharmacological effect. Inosine is then further metabolized to hypoxanthine and then to xanthine. 

regadenoson has high lipophilicity and high binding to plasma. It makes it less likely to be metabolized by liver enzymes. 

Elimination and excretion 

regadenoson is eliminated rapidly from the body, with a half-life of about 2-3 minutes. Most of the drug is eliminated through the kidneys, with a small fraction eliminated through the lungs. 

Adminstartion

Administration: 

regadenoson is taken intravenously as an injection. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: regadenoson 

Pronounced: reg-ah-den-o-sun 

Why do we use regadenoson? 

regadenoson is used as a myocardial infarction imaging agent.