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Clopidogrel's antiplatelet effect is hindered by the slow and variable biotransformation of the prodrug and by impaired response in a small minority of patients. Ticagrelor, a reversible, direct-acting, oral P2Y12 antagonist, inhibits more platelet aggregation faster and more consistently than clopidogrel.
In a manufacturer-sponsored, double-blind, randomized trial, investigators compared the efficacy and safety of ticagrelor (180–270 mg loading dose followed by 90 mg twice daily) and clopidogrel (300–600 mg loading dose followed by 75 mg daily) in 18,624 patients with acute coronary syndromes. Concomitant medications included aspirin (in >97%), beta-blockers (in >89%), ACE inhibitors (in >75%), statins (in >89%), and proton-pump inhibitors …