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# Ticagrelor (Brilinta) ## Overview Ticagrelor is an oral P2Y12 platelet inhibitor that reversibly binds to the P2Y12 receptor. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS). ## Primary Indications * Acute Coronary Syndrome (ACS): Unstable angina, non-ST-elevation myocardial infarction (NSTEMI), or ST-elevation myocardial infarction (STEMI) in patients treated medically or with percutaneous coronary intervention (PCI). ## Adult Dosing * **ACS:** * **Loading Dose:** 180 mg orally once. * **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. * **After 12 months of treatment (or if treated with a drug-eluting stent during ACS):** Dose may be reduced to 60 mg orally twice daily. * **History of MI (at least 1 year post-MI):** For patients with a history of MI at least 1 year ago and at least one additional risk factor for occlusive thrombotic events, ticagrelor 60 mg orally twice daily can be considered to reduce the rate of new thrombotic cardiovascular events. This should be used in combination with aspirin. ## Pediatric Dosing * Safety and efficacy in pediatric patients have not been established. ## Dose Adjustments * **Renal Impairment:** No dose adjustment required for mild to severe renal impairment. * **Hepatic Impairment:** No dose adjustment required for mild to moderate hepatic impairment. Use with caution in severe hepatic impairment. ## Contraindications * Active bleeding. * History of transient ischemic attack (TIA) or stroke. * Known hypersensitivity to ticagrelor or any component of the formulation. ## Adverse Effects * **Common:** Dyspnea, bleeding (including fatal and life-threatening, particularly gastrointestinal and intracranial), bradycardia, increased serum creatinine, and uric acid. * **Serious:** Major bleeding, significant bradyarrhythmia. ## Key Drug Interactions * **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Avoid concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin) and inducers (e.g., rifampin, carbamazepine, phenytoin). * **Proton Pump Inhibitors (PPIs):** Some studies suggest that PPIs, particularly omeprazole and esomeprazole, may reduce ticagrelor exposure and efficacy. Consider alternative acid suppressants if possible, though the clinical significance is debated. * **Anticoagulants (e.g., warfarin, direct oral anticoagulants):** Increased risk of bleeding. Use concomitantly with caution and monitor for signs of bleeding. * **Aspirin:** Concomitant use is generally recommended in ACS, but increases bleeding risk. Dose-dependent effect on ticagrelor's P2Y12 inhibition. Aspirin doses >100 mg may reduce ticagrelor's efficacy. ## Monitoring * **Bleeding:** Monitor for signs and symptoms of bleeding (e.g., bruising, hematuria, melena, epistaxis). * **Renal Function:** Assess serum creatinine periodically. * **Heart Rate:** Monitor for symptomatic bradycardia. ## Clinical Pearls * Ticagrelor provides faster and more consistent platelet inhibition compared to clopidogrel. * Unlike clopidogrel, ticagrelor does not require metabolic activation by CYP enzymes and is not subject to genetic polymorphisms affecting CYP2C19. * Dyspnea is a common side effect and often transient; it does not necessarily indicate underlying cardiac or pulmonary disease. * Discontinuation of ticagrelor prematurely increases the risk of stent thrombosis, myocardial infarction, and death. * For patients undergoing PCI, ticagrelor should be administered as a loading dose as soon as possible, regardless of whether it is given before or after balloon inflation. *** **Disclaimer:** This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines for definitive guidance. The specific management of patients, including dosing and duration of therapy, should be individualized based on patient characteristics and clinical judgment.