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Lexiscan(R) (Regadenoson)

FDA Drug Information • Also known as: Lexiscan(R) (Regadenoson)

Brand Names
Lexiscan(R) (Regadenoson)
Drug Class
Adenosine Receptor Agonist [EPC]
Route
INTRAVENOUS
Dosage Form
INJECTION, SOLUTION
Product Type
HUMAN PRESCRIPTION DRUG

Description

11 DESCRIPTION Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator [see Clinical Pharmacology ( 12- 12.1)]. 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. LEXISCAN 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, 10.9 mg dibasic sodium phosphate dihydrate or 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. STRUCTURE

    • What Is Lexiscan(R) (Regadenoson) Used For?

    1 INDICATIONS & USAGE LEXISCAN® (regadenoson) injection is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress.

    Dosage and Administration

    2 DOSAGE AND ADMINISTRATION The recommended dose of LEXISCAN is 5 mL (0.4 mg regadenoson) administered as an intravenous injection within 10 seconds.

  • 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 MPI [see Drug Interactions ( 7- 7.1) and Clinical Pharmacology ( 12- 12.2)].
  • 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.

    • Side Effects (Adverse Reactions)

    6 ADVERSE REACTIONS The following adverse reactions are discussed in more detail in other sections of the labeling.

  • Myocardial Ischemia [see Warnings and Precautions ( 5- 5.1)]
  • Sinoatrial and Atrioventricular Nodal Block [see Warnings and Precautions ( 5- 5.2)]
  • Atrial Fibrillation/Atrial Flutter [see Warnings and Precautions ( 5- 5.3)]
  • Hypersensitivity, Including Anaphylaxis [see Warnings and Precautions ( 5- 5.4)]
  • Hypotension [see Warnings and Precautions ( 5- 5.5)]
  • Hypertension [see Warnings and Precautions ( 5- 5.6)]
  • Bronchoconstriction [see Warnings and Precautions ( 5- 5.7)]
  • Seizure [see Warnings and Precautions ( 5- 5.8)]
  • Cerebrovascular Accident (Stroke) [see Warnings and Precautions ( 5- 5.9)] 6.1 Clinical Trials Experience 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 patients were exposed to LEXISCAN, with most receiving 0.4 mg as a rapid (≤ 10 seconds) intravenous injection. Most of these patients 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. Table 1 Adverse Reactions in Studies 1 and 2 Pooled (Frequency ≥ 5%) ECG Abnormalities The frequency of rhythm or conduction abnormalities following LEXISCAN or ADENOSCAN is shown in Table 2 [see Warnings and Precautions ( 5- 5.2)]. Table 2 Rhythm or Conduction Abnormalities* in Studies 1 and 2 * 12-lead ECGs were recorded before and for up to 2 hours after dosing. † includes rhythm abnormalities (PACs, PVCs, atrial fibrillation/flutter, wandering atrial pacemaker, supraventricular or ventricular arrhythmia) or conduction abnormalities, including AV block. Respiratory Abnormalities In a randomized, placebo-controlled trial of 999 patients 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 patients 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). Table 3 Respiratory Adverse Effects* * All patients continued the use of their respiratory medications as prescribed prior to administration of LEXISCAN. † Patients may have reported more than one type of adverse reaction. Adverse reactions were collected up to 24 hours following drug administration. Pre-specified respiratory adverse reactions included dyspnea, wheezing, obstructive airway disorder, dyspnea exertional, and tachypnea. ‡ Change from baseline at 2 hours. Renal Impairment In a randomized, placebo-controlled trial of 504 patients (LEXISCAN n=334 and placebo n=170) with a...

    • Drug Interactions

    7 DRUG INTERACTIONS No formal pharmacokinetic drug interaction studies have been conducted with LEXISCAN. 7.1 Effects of Other Drugs on LEXISCAN

  • Methylxanthines (e.g., caffeine, aminophylline and theophylline) are non-specific adenosine receptor antagonists that interfere with the vasodilation activity of LEXISCAN [see Clinical Pharmacology ( 12- 12.2) and Patient Counseling Information ( 17 )]. 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 [see Overdosage ( 10 )].
  • In clinical studies, LEXISCAN was administered to patients taking other cardioactive drugs (i.e., β-blockers, calcium channel blockers, ACE inhibitors, nitrates, cardiac glycosides, and angiotensin receptor blockers) without reported adverse reactions or apparent effects on efficacy.
  • Dipyridamole may change the effects of LEXISCAN. When possible, withhold dipyridamole for at least two days prior to LEXISCAN administration. 7.2 Effect of LEXISCAN on Other Drugs Regadenoson does not inhibit the metabolism of substrates for CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 in human liver microsomes, indicating that it is unlikely to alter the pharmacokinetics of drugs metabolized by these cytochrome P450 enzymes.

    • Contraindications

    4 CONTRAINDICATIONS Do not administer LEXISCAN to patients with:

  • Second- or third-degree AV block, or
  • sinus node dysfunction unless these patients have a functioning artificial pacemaker [see Warnings and Precautions ( 5- 5.2)].

    • Overdosage

    10 OVERDOSAGE LEXISCAN overdosage may result in serious reactions [see Warnings and Precautions ( 5 )]. In a study of healthy volunteers, symptoms of flushing, dizziness and increased heart rate were assessed as intolerable at LEXISCAN doses greater than 0.02 mg/kg. Aminophylline to Reverse Effects Methylxanthines, such as caffeine, aminophylline, and theophylline, are competitive adenosine receptor antagonists and aminophylline has been used to terminate persistent pharmacodynamic effects. 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 [see Warnings and Precautions ( 5- 5.8)].

    How Supplied

    16 HOW SUPPLIED/STORAGE AND HANDLING LEXISCAN(R) (REGADENOSON) INJECTION is supplied in the following dosage forms. NDC 51662-1448-1 LEXISCAN(R) (REGADENOSON) INJECTION 0.4mg/5mL (0.08 mg/mL) 5mL SYR HF Acquisition Co LLC, DBA HealthFirst Mukilteo, WA 98275 Also supplied in the following manufacture supplied dosage forms LEXISCAN is supplied as a sterile, preservative-free solution containing 0.08 mg/mL regadenoson in the following package:

  • Single-dose 5 mL pre-filled plastic Ansyr® syringes with luer-lock fitting (NDC 0469-6501-89). Store at controlled room temperature, 25°C (77°F); excursions permitted to 15° to 30°C (59°– 86°F).

    • About This Information

    This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.

    What are side effects?

    Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.

    What are drug interactions?

    Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.