Lexiscan

Warnings
Precautions

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

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 [see OVERDOSAGE].

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 post-marketing experience, third-degree heart block and asystole within minutes of Lexiscan administration have occurred [see ADVERSE REACTIONS].

Atrial Fibrillation/Atrial Flutter

New-onset or recurrent atrial fibrillation with rapid ventricular response and atrial flutter have been reported following Lexiscan injection [see ADVERSE REACTIONS].

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 [see ADVERSE REACTIONS]. 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 post-marketing experience, syncope, transient ischemic attacks and seizures have been observed [see ADVERSE REACTIONS].

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 [see CLINICAL PHARMACOLOGY]. 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 [see ADVERSE REACTIONS].

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 [see ADVERSE REACTIONS, CLINICAL PHARMACOLOGY, OVERDOSAGE and PATIENT INFORMATION].

Seizure

Lexiscan may lower the seizure threshold. New-onset or recurrence of convulsive seizures has occurred following Lexiscan injection. Some seizures are prolonged and require emergent anticonvulsive management. Aminophylline may increase the risk of seizures associated with Lexiscan injection. Methylxanthine use is not recommended in patients who experience a seizure in association with Lexiscan administration.

Cerebrovascular Accident (Stroke)

Hemorrhagic and ischemic cerebrovascular accidents have occurred. Hemodynamic effects of Lexiscan including hypotension or hypertension may be associated with these adverse reactions [see Hypotension and Hypertension].

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment Of Fertility

Regadenoson was negative in the Ames bacterial mutation assay, chromosomal aberration assay in Chinese hamster ovary (CHO) cells, and mouse bone marrow micronucleus assay. Long-term animal studies have not been conducted to evaluate Lexiscan's carcinogenic potential or potential effects on fertility.

Use In Specific Populations

Pregnancy

Pregnancy Category C

There are no adequate well-controlled studies with Lexiscan in pregnant women. Lexiscan should be used during pregnancy only if the potential benefit to the patient justifies the potential risk to the fetus.

Reproductive studies in rats showed that regadenoson doses 10 and 20 times the maximum recommended human dose (MRHD) based on body surface area, caused reduced fetal body weights and significant ossification delays in fore-and hind limb phalanges and metatarsals; however, maternal toxicity also occurred at these doses. Skeletal variations were increased in all treated groups. In rabbits, there were no teratogenic effects in offspring at regadenoson doses 4 times the MRHD, although signs of maternal toxicity occurred at this dose. At regadenoson doses equivalent to 12 and 20 times the MRHD, maternal toxicity occurred along with increased embryo-fetal loss and fetal malformations. It is not clear whether malformations that occurred at maternally toxic doses of regadenoson in both animal species were due to fetal drug effects or only to the maternal toxic effects.

Because animals received repeated doses of regadenoson, their exposure was significantly higher than that achieved with the standard single dose administered to humans [see Nonclinical Toxicology].

Nursing Mothers

It is not known whether Lexiscan is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions from Lexiscan in nursing infants, the decision to interrupt nursing after administration of Lexiscan or not to administer Lexiscan, should take into account the importance of the drug to the mother. Based on the pharmacokinetics of Lexiscan, it should be cleared 10 hours after administration. Therefore, nursing women may consider interrupting nursing for 10 hours after administration.

Pediatric Use

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

Geriatric Use

Of the 1,337 patients receiving Lexiscan in Studies 1 and 2, 56% were 65 years of age and over and 24% were 75 years of age and over. Older patients ( ≥ 75 years of age) had a similar adverse event profile compared to younger patients ( < 65 years of age), but had a higher incidence of hypotension (2% vs. ≤ 1%).

Renal Impairment

Lexiscan was assessed in a randomized, placebo-controlled trial of patients with NKFK/DOQI Stage III or IV renal impairment (defined as a GFR 15-59 mL/min/1.73 m²). No serious adverse events were reported through the 24-hour follow-up period [see ADVERSE REACTIONS].

Last reviewed on RxList: 10/3/2014
This monograph has been modified to include the generic and brand name in many instances.

Warnings
Precautions
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