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# Ticagrelor (Brilinta) ## Overview Ticagrelor is an orally administered, direct-acting P2Y12 receptor antagonist used to prevent thrombotic events. It is a member of the cyclopentyltriazolopyrimidine (CPTP) class. Unlike clopidogrel, ticagrelor is a reversible antagonist and does not require metabolic activation. ## Primary Indications * **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the prevention of thrombotic events (e.g., myocardial infarction, stroke) in patients with ACS, including unstable angina, non-ST-elevation myocardial infarction (NSTEMI), and ST-elevation myocardial infarction (STEMI). * **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor has been shown to reduce the rate of cardiovascular death, MI, and stroke in combination with aspirin. ## Adult Dosing * **ACS:** * **Loading Dose:** 180 mg orally once. * **Maintenance Dose:** 90 mg orally twice daily. * **History of MI:** * **Maintenance Dose:** 60 mg orally twice daily. **Note:** Aspirin dose should be individualized but is typically continued at a maintenance dose of 75-100 mg daily when used with ticagrelor for ACS. For patients with a history of MI, the 60 mg dose is used in combination with low-dose aspirin. The optimal duration of therapy depends on the clinical context and patient risk factors. ## Pediatric Dosing Dosing for pediatric patients has not been established. ## Dose Adjustments * **Hepatic Impairment:** No dose adjustment is required in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment. * **Renal Impairment:** No dose adjustment is required for mild, moderate, or severe renal impairment. ## Contraindications * Active pathological bleeding. * Known history of intracranial hemorrhage. * Hypersensitivity to ticagrelor or any of its excipients. ## Adverse Effects * **Most Common:** Bleeding (including major and minor), dyspnea, bradycardia, ventricular pauses, hyperuricemia, increased serum creatinine. * **Serious:** Significant bleeding events, potentially life-threatening hemorrhage. ## Key Drug Interactions * **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) can increase ticagrelor concentrations. Co-administration with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) can decrease ticagrelor concentrations. * **CYP3A4 Substrates:** Ticagrelor can increase plasma concentrations of CYP3A4 substrates (e.g., simvastatin, atorvastatin), potentially increasing the risk of adverse effects from these drugs. * **Other Antiplatelets/Anticoagulants:** Concurrent use increases the risk of bleeding. ## Monitoring * **Bleeding:** Closely monitor for signs and symptoms of bleeding. * **Renal Function:** Monitor serum creatinine periodically, especially in patients with pre-existing renal impairment. * **Uric Acid:** Monitor serum uric acid levels, especially in patients with a history of gout or hyperuricemia. * **Heart Rate:** Monitor for bradycardia. ## Clinical Pearls * Ticagrelor is a reversible P2Y12 inhibitor and has a more rapid onset and offset of action compared to clopidogrel. * Dyspnea is a common side effect and is usually not clinically significant, but it should be evaluated to rule out other causes. * Discontinuation of ticagrelor prematurely increases the risk of thrombotic events. If antiplatelet therapy must be interrupted for any reason (e.g., surgery), it should be done as soon as clinically feasible. * Ticagrelor is not recommended for use in patients with a history of stroke or transient ischemic attack (TIA) due to an increased risk of intracranial bleeding. *** **Disclaimer:** This information is intended for clinical use and should not be considered a substitute for professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines before making any treatment decisions. Dosing and management may vary based on individual patient factors and local protocols.