Ticagrelor
Ticagrelor
Brilinta
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Summary
Common uses
Acute coronary syndrome (with aspirin)0, Post-PCI dual antiplatelet therapy0, Secondary prevention >12 months post-MI (60 mg BID, PEGASUS-derived)0
Pharmacy
Starting dose
ACS/PCI: 180 mg PO loading dose, then 90 mg PO BID for 12 months; long-term post-MI: 60 mg BID
Preparations
60, 90 mg tablets
US FDA Max
90 mg BID (acute year); 60 mg BID (chronic post-MI)
Pharmacology
Routes
Oral
Onset
Antiplatelet effect within 30 minutes of loading dose (faster than clopidogrel)
Duration
12 hours
Half-life
~7 hours (parent); ~9 hours (active AR-C124910XX metabolite, accounts for ~30-40% of activity)[1]
Bioavailability
~36% (oral)[1]
Pregnancy
Limited data; weigh against alternatives.[citation needed]
Legal status
Purported mechanism
Ticagrelor is a reversible direct-acting P2Y12 receptor antagonist; unlike clopidogrel and prasugrel it does not require CYP-mediated bioactivation, so antiplatelet effect onset is faster, more predictable, and less CYP2C19-genotype-dependent.0 PLATO (2009) established mortality benefit over clopidogrel in ACS, but the requirement for BID dosing, increased dyspnea (~14%), and bradyarrhythmia signal complicate adherence. CYP3A4 substrate AND moderate inhibitor — strong CYP3A4 inhibitors raise exposure substantially[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Brilinta (ticagrelor), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022433s029lbl.pdf