LEXISCAN

In healthy subjects, the regadenoson plasma concentration-time profile is multi-exponential in nature and best characterized by 3-compartment model. The maximal plasma concentration of regadenoson is achieved within 1 to 4 minutes after injection of LEXISCAN and parallels the onset of the pharmacodynamic response. The half-life of this initial phase is approximately 2 to 4 minutes. An intermediate phase follows, with a half-life on average of 30 minutes coinciding with loss of the pharmacodynami...

Agreement between LEXISCAN and ADENOSCAN The efficacy and safety of LEXISCAN were determined relative to ADENOSCAN in two randomized, double-blind studies (Studies 1 and 2) in 2,015 patients with known or suspected coronary artery disease who were indicated for pharmacologic stress MPI. A total of 1,871 of these patients had images considered valid for the primary efficacy evaluation, including 1,294 (69%) men and 577 (31%) women with a median age of 66 years (range 26–93 years of age). Each patient received an initial stress scan using ADENOSCAN (6-minute infusion using a dose of 0.14 mg/kg/m...

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

• Myocardial Ischemia [see Warnings and Precautions ( 5.1 ) ]
• Sinoatrial and Atrioventricular Nodal Block [see Warnings and Precautions ( 5.2 ) ]
• Atrial Fibrillation/Atrial Flutter [see Warnings and Precautions ( 5.3 ) ]
• Hypersensitivity, Including Anaphylaxis [see Warnings and Precautions ( 5.4 ) ]
• Hypotension [see Warnings and Precautions ( 5.5 ) ]
• Hypertension [ see Warnings and Prec...

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 ( 5.2 ) ]. Do not administer LEXISCAN to patients with:
• Second- or third-degree AV block, or
• sinus node dysfunction unless the patients have a functioning artificial pacemaker ( 4 ).

• Myocardial Ischemia. Fatal cardiac events have occurred. 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 ( 5.1 ).
• Sinoatrial (SA) and Atrioventricular (AV) Nodal Block. Adenosine receptor agonists, including LEXISCAN, can depress the SA and AV nodes and may cause first-, second- or third-d...

7 DRUG INTERACTIONS No formal pharmacokinetic drug interaction studies have been conducted with LEXISCAN.

• Methylxanthines, e.g., caffeine, aminophylline and theophylline, interfere with the activity of LEXISCAN ( 7.1 , 12.2 ).
• Aminophylline may be used to attenuate severe and/or persistent adverse reactions to LEXISCAN ( 7.1 , 10 ).
• Dipyridamole may increase the activity of LEXISCAN. When po...