Regadenoson

{{DrugProjectFormSinglePage |authorTag=

Gerald Chi

|genericName=

Regadenoson

|aOrAn=

a

|drugClass=

vasodilator

|indication=

radionuclide myocardial perfusion imaging in patients unable to undergo adequate exercise stress

|hasBlackBoxWarning=

|adverseReactions=

angina, dysrhythmia, chest discomfort, chest pain, tachycardia, ventricular premature complex, nausea, dizziness, headache, dyspnea, and flushing

|blackBoxWarningTitle= Title

|blackBoxWarningBody= ConditionName:

• Content

|fdaLIADAdult=

Radionuclide Myocardial Perfusion Imaging

• Lexiscan® (regadenoson) injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress.

• Dosing Information

• The recommended intravenous dose of Lexiscan is 5 mL (0.4 mg regadenoson)
• Administer Lexiscan as a rapid (approximately 10 seconds) injection 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.
• 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.

|offLabelAdultGuideSupport=

There is limited information regarding Off-Label Guideline-Supported Use of Regadenoson in adult patients.

|offLabelAdultNoGuideSupport=

There is limited information regarding Off-Label Non–Guideline-Supported Use of Regadenoson in adult patients.

|fdaLIADPed=

• Safety and effectiveness in pediatric patients (< 18 years of age) have not been established.

|offLabelPedGuideSupport=

There is limited information regarding Off-Label Guideline-Supported Use of Regadenoson in pediatric patients.

|offLabelPedNoGuideSupport=

There is limited information regarding Off-Label Non–Guideline-Supported Use of Regadenoson in pediatric patients.

|contraindications=

• Do not administer Lexiscan to patients with the following conditions (unless these patients have a functioning artificial pacemaker):

• Second- or third- degree AV block
• Sinus node dysfunction

|warnings=

• Myocardial Ischemia

• Fatal and nonfatal myocardial infarction, 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; these patients may be at greater risk of serious cardiovascular reactions to Lexiscan. Cardiac resuscitation equipment and trained staff should be available before administering Lexiscan. If serious reactions to Lexiscan occur, consider the use of aminophylline, an adenosine antagonist, to shorten the duration of increased coronary blood flow induced by Lexiscan.

• Sinoatrial and Atrioventricular Nodal Block

• 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 requiring intervention. In clinical trials first-degree AV block (PR prolongation > 220 msec) developed in 3% of patients within 2 hours of Lexiscan administration; transient second-degree AV block with one dropped beat was observed in one patient receiving Lexiscan. In postmarketing experience, third degree heart block and asystole within minutes of Lexiscan administration have occurred.

• Hypersensitivity, Including Anaphylaxis

• Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria and rashes have occurred. In clinical trials, hypersensitivity reactions were reported in fewer than 1 percent of patients. Have personnel and resuscitative equipment immediately available.

• Hypotension

• Adenosine receptor agonists, including Lexiscan, induce arterial vasodilation and hypotension. In clinical trials, decreased systolic blood pressure (> 35 mm Hg) was observed in 7% of patients and decreased diastolic blood pressure (> 25 mm Hg) was observed in 4% of patients within 45 min of Lexiscan administration. The risk of serious hypotension may be higher in patients with autonomic dysfunction, hypovolemia, left main coronary artery stenosis, stenotic valvular heart disease, pericarditis or pericardial effusions, or stenotic carotid artery disease with cerebrovascular insufficiency. In postmarketing experience, syncope, transient ischemic attacks and seizures have been observed.

• Hypertension

• Administration of adenosine receptor agonists, including Lexiscan, may result in clinically significant increases in blood pressure in some patients. Among patients who experienced an increase in blood pressure in clinical trials, the increase was observed within minutes of Lexiscan administration. Most increases resolved within 10 to 15 minutes, but in some cases, increases were observed at 45 minutes following administration. In post-marketing experience, cases of potentially clinically significant hypertension have been reported, particularly with underlying hypertension and when low-level exercise was included in the MPI.

• Bronchoconstriction

• Adenosine receptor agonists, including Lexiscan, may cause dyspnea, bronchoconstriction, and respiratory compromise. Appropriate bronchodilator therapy and resuscitative measures should be available prior to Lexiscan administration.

|clinicalTrials=

• Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
• During clinical development, 1,651 subjects were exposed to Lexiscan, with most receiving 0.4 mg as a rapid (≤ 10 seconds) intravenous injection. Most of these subjects received Lexiscan in two clinical studies that enrolled patients who had no history of bronchospastic lung disease as well as no history of a cardiac conduction block of greater than first-degree AV block, except for patients with functioning artificial pacemakers. In these studies (Studies 1 and 2), 2,015 patients underwent myocardial perfusion imaging after administration of Lexiscan (N = 1,337) or Adenoscan® (N = 678). The population was 26–93 years of age (median 66 years), 70% male and primarily Caucasian (76% Caucasian, 7% African American, 9% Hispanic, 5% Asian). Table 1 shows the most frequently reported adverse reactions.
• Overall, any adverse reaction occurred at similar rates between the study groups (80% for the Lexiscan group and 83% for the Adenoscan group). Aminophylline was used to treat the reactions in 3% of patients in the Lexiscan group and 2% of patients in the Adenoscan group. Most adverse reactions began soon after dosing, and generally resolved within approximately 15 minutes, except for headache which resolved in most patients within 30 minutes.

This image is provided by the National Library of Medicine.

• ECG Abnormalities

• The frequency of rhythm or conduction abnormalities following Lexiscan or Adenoscan is shown in Table 2.

This image is provided by the National Library of Medicine.

• Respiratory Abnormalities

• In a randomized, placebo-controlled trial (Study 3) of 999 subjects with asthma (n=532) or stable chronic obstructive pulmonary disease (n=467), the overall incidence of pre-specified respiratory adverse reactions was greater in the Lexiscan group compared to the placebo group (p < 0.001). Most respiratory adverse reactions resolved without therapy; a few subjects received aminophylline or a short acting bronchodilator. No differences were observed between treatment arms in the reduction of >15% from baseline at two-hours in FEV1 (Table 3).

This image is provided by the National Library of Medicine.

• Renal Impairment

• In a randomized, placebo-controlled trial of 504 subjects (Lexiscan n=334 and placebo n=170) with a diagnosis or risk factors for coronary artery disease and NKFK/DOQI Stage III or IV renal impairment (defined as GFR 15-59 mL/min/1.73 m2), no serious adverse events were reported through the 24-hour follow-up period.

|postmarketing=

• Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to Lexiscan exposure.

Cardiovascular

Myocardial infarction, cardiac arrest, ventricular arrhythmias, supraventricular tachyarrhythmias including atrial fibrillation or flutter, heart block (including third degree block), asystole, marked hypertension, symptomatic hypotension in association with transient ischemic attack, seizures and syncope have been reported. Some events required intervention with fluids and/or aminophylline. QTc prolongation shortly after Lexiscan administration has been reported.

Digestive

Abdominal pain, occasionally severe, has been reported a few minutes after Lexiscan administration, in association with nausea, vomiting, or myalgias; administration of aminophylline, an adenosine antagonist, appeared to lessen the pain. Diarrhea and fecal incontinence have also been reported following Lexiscan administration.

Musculoskeletal

Musculoskeletal pain has occurred, typically 10-20 minutes after Lexiscan administration; the pain was occasionally severe, localized in the arms and lower back and extended to the buttocks and lower legs bilaterally. Administration of aminophylline appeared to lessen the pain.

Neurologic

Tremor, seizure (particularly with a history of seizure)

Respiratory

Respiratory arrest, dyspnea and wheezing have been reported following Lexiscan administration.

Skin and Hypersensitivy Reactions

Anaphylaxis, angioedema, cardiac or respiratory arrest, respiratory distress, decreased oxygen saturation, hypotension, throat tightness, urticaria, rashes have occurred and have required treatment including resuscitation.

|drugInteractions=

• Drug

• Description

|useInPregnancyFDA=

• Pregnancy Category

|useInPregnancyAUS=

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Regadenoson in women who are pregnant.

|useInLaborDelivery= There is no FDA guidance on use of Regadenoson during labor and delivery.

|useInNursing= There is no FDA guidance on the use of Regadenoson with respect to nursing mothers.

|useInPed= There is no FDA guidance on the use of Regadenoson with respect to pediatric patients.

|useInGeri= There is no FDA guidance on the use of Regadenoson with respect to geriatric patients.

|useInGender= There is no FDA guidance on the use of Regadenoson with respect to specific gender populations.

|useInRace= There is no FDA guidance on the use of Regadenoson with respect to specific racial populations.

|useInRenalImpair= There is no FDA guidance on the use of Regadenoson in patients with renal impairment.

|useInHepaticImpair= There is no FDA guidance on the use of Regadenoson in patients with hepatic impairment.

|useInReproPotential= There is no FDA guidance on the use of Regadenoson in women of reproductive potentials and males.

|useInImmunocomp= There is no FDA guidance one the use of Regadenoson in patients who are immunocompromised.

|administration=

• Oral

• Intravenous

|monitoring=

There is limited information regarding Monitoring of Regadenoson in the drug label.

• Description

|IVCompat=

There is limited information regarding IV Compatibility of Regadenoson in the drug label.

|overdose=

Acute Overdose

Signs and Symptoms

• Description

Management

• Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Regadenoson in the drug label.

|drugBox=

{{Drugbox2 | Verifiedfields = changed | verifiedrevid = 413312613 | IUPAC_name = 2-{4-[(methylamino)carbonyl]- 1H-pyrazol-1-yl}adenosine | image = Regadenoson2.png | width = 300

| tradename = | Drugs.com = Multum Consumer Information | licence_US = Regadenoson | pregnancy_AU = | pregnancy_US = C | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Rx-only | legal_status = | routes_of_administration = Intravenous

| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =

| CAS_number_Ref =  ^Y | CAS_number = 313348-27-5 | CAS_supplemental = 875148-45-1 | ATC_prefix = C01 | ATC_suffix = EB21 | ATC_supplemental = | PubChem = 219024 | DrugBank_Ref =  ^Y | DrugBank = | UNII_Ref =  ^N | UNII = 7AXV542LZ4 | KEGG_Ref =  ^Y | KEGG = D05711 | ChEMBL_Ref =  ^N | ChEMBL = 1201750

| chemical_formula = | C=15 | H=18 | N=8 | O=5 | molecular_weight = 390.354 g/mol | synonyms = 1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]- N-methylpyrazole-4-carboxamide }}

|mechAction=

|structure=

This image is provided by the National Library of Medicine.

|PD=

There is limited information regarding Pharmacodynamics of Regadenoson in the drug label.

|PK=

There is limited information regarding Pharmacokinetics of Regadenoson in the drug label.

|nonClinToxic=

There is limited information regarding Nonclinical Toxicology of Regadenoson in the drug label.

|clinicalStudies=

There is limited information regarding Clinical Studies of Regadenoson in the drug label.

|howSupplied=

|fdaPatientInfo=

There is limited information regarding Patient Counseling Information of Regadenoson in the drug label.

|alcohol=

• Alcohol-Regadenoson interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

|brandNames=

• Lexiscan®

|lookAlike=

• N/A

|drugShortage= }}

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