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# Ticagrelor (Brilinta) ## Overview - Antiplatelet agent; reversible, direct-acting P2Y12 receptor antagonist. - Prodrug not requiring metabolic activation; onset faster than clopidogrel. ## Primary Indications - Acute coronary syndrome (ACS) – with aspirin. - History of myocardial infarction (MI) – for long-term secondary prevention. - High-risk transient ischemic attack (TIA) or minor ischemic stroke – within 24 hours (dual antiplatelet therapy with aspirin for 30 days, then monotherapy). ## Adult Dosing - **ACS loading dose:** 180 mg orally once. - **Maintenance:** 90 mg twice daily with aspirin 81–100 mg daily. - **Post-MI secondary prevention (long-term):** 60 mg twice daily (after initial 12 months of ACS dosing or as per local protocol). - **TIA/ischemic stroke (high-risk):** 180 mg loading dose on day 1, then 90 mg twice daily for 30 days, with aspirin; followed by ticagrelor monotherapy 60 mg twice daily (exact duration per local guidelines). ## Pediatric Dosing - **Safety and efficacy not established** in patients <18 years. No routine pediatric dosing. - Limited data: some off-label use in children with thrombotic events (e.g., after Fontan procedure) – consult specialist. ## Dose Adjustments - **Renal impairment:** No adjustment for mild–moderate; avoid in severe (CrCl <15 mL/min) or dialysis (lack of data). - **Hepatic impairment:** Avoid in severe hepatic disease (risk of bleeding). - **Elderly:** No specific dose adjustment, but increased bleeding risk. - **Switching from prasugrel or clopidogrel:** Administer ticagrelor loading dose as above. ## Contraindications - Active pathological bleeding. - History of intracranial hemorrhage. - Severe hepatic impairment. - Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir). ## Adverse Effects - Bleeding (major/minor; dyspnea is common, usually mild, resolves with continued use). - Bradyarrhythmias, ventricular pauses (monitor if high-risk). - Increased uric acid (rarely gout). - Hematologic: thrombotic thrombocytopenic purpura (very rare). ## Key Drug Interactions - **Aspirin:** High-dose (>300 mg) reduces ticagrelor efficacy – maintain ≤100 mg. - **CYP3A4 inhibitors:** Increase ticagrelor exposure – avoid strong inhibitors. - **CYP3A4 inducers** (e.g., rifampin, phenytoin): Reduce ticagrelor exposure – avoid. - **Anticoagulants/NSAIDs/antiplatelets:** Increase bleeding risk. - **Digoxin:** Modest increase in digoxin levels (monitor). ## Monitoring - Signs/symptoms of bleeding (especially GI, intracranial). - CBC, renal/hepatic function periodically. - Serum uric acid if symptomatic. - ECG in patients with history of bradycardia or syncope. ## Clinical Pearls - **Dyspnea** occurs in ~15% – assess if new or worsening; if intolerable, may switch agent. - **Twice-daily dosing** (not once daily) – miss >2 doses increases thrombotic risk. - **Hold for 5–7 days** before elective surgery (per local protocol). - **Plavix PlAVIX?** Ticagrelor has faster onset and offset than clopidogrel; preferred in ACS with high-risk features. - **Do not crush** – only whole tablets. - **Loading dose timing:** Give as soon as possible in ACS; for stroke/TIA, within 24 hours. *This information is for educational purposes. Always verify current prescribing information from the manufacturer's labeling and local clinical guidelines.*