Regadenoson

What is Regadenoson?

• Regadenoson (Lexiscan) is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.

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Regadenoson

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Regadenoson2

What are the uses of this medicine?

Regadenoson (Lexiscan) is a stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress.

How does this medicine work?

• An adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity.
• Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation.
• This leads to an increase in coronary blood flow and enhances myocardial perfusion.
• Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor.
• This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Second- or third-degree AV block, or
• sinus node dysfunction
• unless the patients have a functioning artificial pacemaker.

What drug interactions can this medicine cause?

• Methylxanthines, e.g., caffeine, aminophylline and theophylline, interfere with the activity of LEXISCAN. Patients should avoid consumption of any products containing methylxanthines as well as any drugs containing theophylline or aminophylline for at least 12 hours before LEXISCAN administration. Aminophylline may be used to attenuate severe or persistent adverse reactions to LEXISCAN.
• Dipyridamole may increase the activity of LEXISCAN. When possible, withhold dipyridamole for at least two days prior to LEXISCAN administration.

Is this medicine FDA approved?

• Regadenoson was approved by the United States Food and Drug Administration on April 10, 2008, and is marketed by Astellas Pharma under the tradename Lexiscan.

How should this medicine be used?

Recommended dosage:

• The recommended dose of LEXISCAN is 5 mL (0.4 mg regadenoson) administered as an intravenous injection within 10 seconds; followed immediately by saline flush and radiopharmaceutical.

Administration:

• Patients should be instructed to avoid consumption of any products containing methylxanthines, including caffeinated coffee, tea or other caffeinated beverages, caffeine-containing drug products, aminophylline and theophylline for at least 12 hours before a scheduled radionuclide myocardial perfusion imaging (MPI).
• Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Do not administer LEXISCAN if it contains particulate matter or is discolored.
• Administer LEXISCAN as an intravenous injection within 10 seconds into a peripheral vein using a 22 gauge or larger catheter or needle.
• Administer a 5 mL saline flush immediately after the injection of LEXISCAN.
• Administer the radionuclide myocardial perfusion imaging agent 10–20 seconds after the saline flush. The radionuclide may be injected directly into the same catheter as LEXISCAN.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: Single-dose pre-filled syringe: 0.4 mg/5 mL (0.08 mg/mL)

This medicine is available in fallowing brand namesː

• LEXISCAN

What side effects can this medication cause?

The most common side effects of this medicine include:

• dyspnea
• headache
• flushing
• chest discomfort
• dizziness
• angina pectoris
• chest pain
• nausea

What special precautions should I follow?

• Fatal and nonfatal myocardial infarction (MI), ventricular arrhythmias, and cardiac arrest have occurred following LEXISCAN injection. Avoid use in patients with symptoms or signs of acute myocardial ischemia, for example unstable angina or cardiovascular instability, who may be at greater risk. Cardiac resuscitation equipment and trained staff should be available before administration.
• Adenosine receptor agonists, including LEXISCAN, can depress the SA and AV nodes and may cause first-, second- or third-degree AV block, or sinus bradycardia.
• New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter have been reported following LEXISCAN injection.
• Hypersensitivity, including anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria, and rashes have occurred. Have personnel and resuscitative equipment immediately available.
• Adenosine receptor agonists, including LEXISCAN, induce vasodilation and hypotension. The risk of serious hypotension may be higher in patients with autonomic dysfunction, stenotic valvular heart disease, pericarditis or pericardial effusions, stenotic carotid artery disease with cerebrovascular insufficiency, or hypovolemia.
• Adenosine receptor agonists, including LEXISCAN, may induce clinically significant increases in blood pressure particularly in patients with a history of hypertension and when the MPI includes low level exercise.
• Adenosine receptor agonists, including LEXISCAN, may induce dyspnea, bronchoconstriction and respiratory compromise in patients with chronic obstructive pulmonary disease (COPD) or asthma. Resuscitative measures should be available.
• LEXISCAN may lower the seizure threshold. New onset or recurrence of convulsive seizures has occurred. Some seizures are prolonged and require urgent anticonvulsive management. Methylxanthine use is not recommended in patients who experience a seizure in association with LEXISCAN.
• Hemorrhagic and ischemic cerebrovascular accidents have occurred.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Flushing, dizziness and increased heart rate.

Treatment of overdosage:

• Methylxanthines, such as caffeine, aminophylline, and theophylline, are competitive adenosine receptor antagonists and aminophylline has been used to terminate side effects of overdose.
• Aminophylline may be administered in doses ranging from 50 mg to 250 mg by slow intravenous injection (50 mg to 100 mg over 30–60 seconds).
• Methylxanthine use is not recommended in patients who experience a seizure in association with LEXISCAN administration.

Can this medicine be used in pregnancy?

• There are no available data on LEXISCAN use in pregnant women to inform a drug-associated risk.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• regadenoson

Inactive ingredients:

• none

Who manufactures and distributes this medicine?

Marketed by: Astellas Pharma US, Inc. Northbrook, IL 60062

Syringes Manufactured by: Hospira, Inc. Lake Forest, IL 60045 USA

• LEXISCAN® and ADENOSCAN® are registered trademarks of Astellas US LLC.

What should I know about storage and disposal of this medication?

• Store at controlled room temperature, 25°C (77°F); excursions permitted to 15° to 30°C (59°– 86°F).

• Dailymed label info on Regadenoson
• FDA Regadenoson

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