Ticagrelor in Ischemic Stroke Management

Mechanism and Clinical Rationale

Ticagrelor is a direct-acting, reversible P2Y12 receptor antagonist with more rapid onset and more consistent inhibition of platelet aggregation compared to clopidogrel, which is a prodrug requiring metabolism by the cytochrome P450 enzyme system, as recommended by the American College of Cardiology 1, 2
Unlike clopidogrel, ticagrelor does not require metabolic activation, making it effective in patients with genetic polymorphisms affecting clopidogrel metabolism, according to the American College of Cardiology 2

For patients switching from clopidogrel to ticagrelor due to resistance, a loading dose of 180 mg ticagrelor is recommended, followed by 90 mg twice daily, as suggested by the American College of Cardiology and the American Heart Association 3, 4
When used with ticagrelor, the aspirin maintenance dose should be limited to ≤100 mg daily (preferably 81 mg) to optimize efficacy and minimize bleeding risk, as recommended by the American College of Cardiology 3, 2

Ticagrelor is associated with an increased risk of non-CABG major bleeding compared to clopidogrel, according to the American College of Cardiology 5
Ticagrelor is contraindicated in patients with a history of intracranial hemorrhage, as stated by the American College of Cardiology 2
Special caution is needed in patients ≥75 years of age, as recommended by the American College of Cardiology and the American Heart Association 5, 6
Special caution is also needed in patients with low body weight (<60 kg), according to the American College of Cardiology 5

Ticagrelor requires twice-daily dosing, which may affect patient adherence compared to once-daily clopidogrel, as noted by the American College of Cardiology 3, 2
Ticagrelor should be discontinued at least 5 days before planned surgical procedures to reduce bleeding risk, as recommended by the American College of Cardiology and the American Heart Association 3, 2
Patients should be monitored for dyspnea, which is a known side effect of ticagrelor, according to the American Heart Association 6