Regadenoson

What is regadenoson used for?

Regadenoson is a prescription medicine that is used during a stress test of the heart.

Description

Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator [see Clinical Pharmacology. Regadenoson is chemically described as adenosine, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]-, monohydrate. Its structural formula is:

The molecular formula for regadenoson is C15H18N8O5 • H2O and its molecular weight is 408.37. Regadenoson Injection is a sterile, nonpyrogenic solution for intravenous injection. The solution is clear and colorless. Each 1 mL in the 5 mL pre-filled syringe contains 0.084 mg of regadenoson monohydrate, corresponding to 0.08 mg regadenoson on an anhydrous basis, 8.7 mg dibasic sodium phosphate anhydrous, 5.4 mg monobasic sodium phosphate monohydrate, 150 mg propylene glycol, 1 mg edetate disodium dihydrate, and water for injection, with pH between 6.3 and 7.7.

Mechanism of Action

Regadenoson is a low affinity agonist (Ki ≈ 1.3 μM) for the A2A adenosine receptor, with at least 10-fold lower affinity for the A1 adenosine receptor (Ki > 16.5 μM), and weak, if any, affinity for the A2B and A3 adenosine receptors. Activation of the A2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow (CBF).

Before taking regadenoson, tell your doctor:

• If you are allergic to regadenoson; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have signs of a heart attack.
• If you have heart block or a slow heartbeat without a working pacemaker.
• If you are breast-feeding. Do not breast-feed for at least 10 hours after getting regadenoson.

This is not a list of all drugs or health problems that interact with regadenoson.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take regadenoson with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take regadenoson?

• Tell all of your health care providers that you take regadenoson. This includes your doctors, nurses, pharmacists, and dentists.
• Heart attacks and heartbeats that are not normal have happened with regadenoson. Sometimes this has been deadly. Talk with the doctor.
• If you are taking aminophylline, dipyridamole, theophylline, or any drug containing caffeine, talk with doctor. These drugs can affect how well regadenoson works.
• Do not eat or drink anything that has caffeine (for example, tea, coffee, cola, and chocolate) for 12 hours before using regadenoson.
• This medicine may raise the chance of seizures in some people, including people who have had seizures in the past. Talk to your doctor to see if you have a greater chance of seizures while taking regadenoson.
• If you are 75 or older, use regadenoson with care. You could have more side effects.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using regadenoson while you are pregnant.

How is regadenoson best taken?

Use regadenoson as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into a vein.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

What are the side effects of regadenoson that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high or low blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.
• Chest pain or pressure.
• Fast or slow heartbeat.
• A heartbeat that does not feel normal.
• Shortness of breath.
• Seizures.

What are some other side effects of regadenoson?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache.
• Flushing.
• Dizziness.
• Upset stomach.
• Stomach pain.
• Change in taste.
• Feeling of warmth.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out regadenoson?

• If you need to store regadenoson at home, talk with your doctor, nurse, or pharmacist about how to store it.

Label

PRINCIPAL DISPLAY PANEL – REGADENOSON INJECTION 5 ML CARTON