TABLE 1

Interventional Medications Used for Cardiac Stress Testing (712,1517)

DrugIndicationDosePharmacokineticsMechanism of actionContraindications/cautionsAdverse effects/interactions
AdenosineVasodilator stressAlternative approaches are 140 μg/kg/min for 6 or 4 min with radiopharmaceutical administered at 3 or 2 min, respectivelyRapid onset, peak < 1 min; half-life < 10 s; duration < 5 min constant infusion; no plasma protein boundVasodilation through activation of adenosine receptor A2aContraindicated in atrioventricular block, severe bronchospasm or asthma, known hypersensitivity; use with caution in hypotension, unstable angina, oral dipyridamole therapy, and medications that suppress sinoatrial or atrioventricular nodes; long-standing methylxanthines need cessation for 5 half-livesAdverse effects include chest, neck, jaw, or arm pain, headache, flushing, dyspnea and electrocardiogram changes; bronchospasm is possible, especially in asthmatics; adverse reactions reversed with cessation of infusion; interactions include caffeine/xanthine drugs or foods
DipyridamoleVasodilator stress0.56 mg/kg intravenously in 20–40 mL of saline over 4 min with radiopharmaceutical administered at end of 4-min infusion or 2 min after completion of infusion1–2 min until onset; peak at 4 min; half-life of 10–12 h; duration can be prolonged without reversal; 90%–99% plasma protein boundInhibition of cellular uptake of adenosine to increase availability of endogenous adenosine; vasodilation through activation of adenosine receptor A2aAs for adenosineAs for adenosine except adverse reactions reversed with aminophylline
RegadenosonVasodilator stress0.4 mg in 5-mL intravenous bolus followed by 5-mL saline flush and immediate administration of radiopharmaceutical0.5–2.3 min until onset; duration of 2.3 min; triphasic half-life, with 2–4, 30, and 120 min, respectively; 20%–30% plasma protein boundVasodilation through selective activation of adenosine receptor A2aAs for adenosine except potentially more flexible in mild to moderate airway diseaseAs for adenosine except less bronchoconstriction but does have risk of seizures
DobutamineStress testing through increasing oxygen demand10 μg/kg/min intravenously, increasing to 20, 30, and 40 μg/kg/min every 3 min1–2 min until onset; duration of 10 min; half-life of 2–3 min; 40% plasma protein boundSynthetic catecholamine β2-adrenoreceptor agonist that produces increased rate and force of contractionContraindicated in hypertrophic cardiomyopathy, uncontrolled hypertension, unstable angina, atrial fibrillation, β-blocker use, and known hypersensitivity; use with caution in myocardial infarction and cardiogenic shock; β-blockers need cessation for 5 half-livesAdverse effects include angina, palpitations, headache, nausea, tachycardia; adverse reactions reversed with cessation of infusion or β-blockers; interactions include blood pressure medications, β-blockers, tricyclic antidepressants, MAOIs, CNS stimulants, potassium-depleting drugs
  • MAOI = monoamine oxidase inhibitors.

  • Duration is period of significant or measurable effect. Some adverse effects are more likely when used therapeutically than in single interventional doses.