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# Ticagrelor (Brilinta) ## Overview Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor. It prevents adenosine triphosphate (ATP) from binding to the P2Y12 receptor on platelets, thereby inhibiting platelet activation and aggregation. ## Primary Indications * **Acute Coronary Syndrome (ACS):** To reduce the rate of thrombotic cardiovascular events, all-cause mortality, stroke, and myocardial infarction (MI) in patients with ACS, including unstable angina (UA), non-ST-elevation MI (NSTEMI), or STEMI, managed medically or with percutaneous coronary intervention (PCI) or coronary artery bypass grafting (CABG). * **Myocardial Infarction (MI):** In patients with a history of MI (at least 1 month prior to treatment initiation) who are at risk for an ischemic event, to reduce the rate of thrombotic cardiovascular events. ## Adult Dosing * **ACS:** * **Loading Dose:** 180 mg orally once. * **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. For patients who are treated with PCI, continue for up to 12 months. * **Consider reducing to 60 mg twice daily:** For patients who are at least 1 year after ACS, have completed at least 6 months of treatment with ticagrelor 90 mg twice daily, and are at high risk for ischemic events but low risk for bleeding. * **History of MI (at least 1 month prior):** 60 mg orally twice daily. ## Pediatric Dosing Ticagrelor is not recommended for use in pediatric patients. Safety and efficacy have not been established. ## Dose Adjustments * **Hepatic Impairment:** No dose adjustment required for mild to moderate hepatic impairment. Use with caution in severe hepatic impairment. * **Renal Impairment:** No dose adjustment required for mild to moderate renal impairment. Use with caution in severe renal impairment. ## Contraindications * **Active pathological bleeding:** Such as peptic ulcer or intracranial hemorrhage. * **History of intracerebral hemorrhage.** * **Hypersensitivity** to ticagrelor or any of its components. ## Adverse Effects * **Common:** Dyspnea, bleeding (including fatal and life-threatening), bruising, hypercholesterolemia, hypertension. * **Serious:** Major bleeding, non-major clinically relevant bleeding, ventricular pauses, bradyarrhythmias. ## Key Drug Interactions * **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors can increase ticagrelor levels; strong inducers can decrease them. Avoid co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin). * **CYP3A4 Substrates:** Ticagrelor can increase concentrations of CYP3A4 substrates. * **P-glycoprotein (P-gp) Inhibitors:** Ticagrelor is a P-gp substrate. Co-administration with P-gp inhibitors may increase ticagrelor exposure. * **Aspirin:** Generally co-administered with aspirin. The combination increases the risk of bleeding. * **Other Antithrombotics:** Concomitant use with other antithrombotic agents increases the risk of bleeding. * **Omeprazole:** Co-administration with omeprazole may reduce ticagrelor exposure; consider PPI timing if used concurrently. ## Monitoring * **Bleeding:** Closely monitor for signs and symptoms of bleeding. * **Efficacy:** Assess for reduction in thrombotic cardiovascular events. * **Electrolytes:** Monitor potassium levels, especially in patients with risk factors for hyperkalemia. ## Clinical Pearls * Ticagrelor's reversible binding allows for potentially faster platelet function recovery compared to clopidogrel, which may be advantageous if urgent surgery is required. However, this is not definitively established in clinical practice. * Dyspnea is a common side effect and is typically transient. It should be distinguished from cardiac causes of dyspnea. * When switching from other P2Y12 inhibitors to ticagrelor, initiate ticagrelor as soon as the last dose of the previous agent is administered. * When switching from ticagrelor to another P2Y12 inhibitor, start the new agent 24 hours after the last dose of ticagrelor. * Consider risks and benefits of ticagrelor 60 mg twice daily in patients with a history of MI who are at high risk for ischemic events but low risk for bleeding. This information is intended for clinical pharmacists and healthcare professionals. It is essential to consult the most current prescribing information and relevant guidelines for complete details and to make individualized patient care decisions.