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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 receptor antagonist. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin and other antiplatelet agents.
* **History of Myocardial Infarction (MI):** To prevent other thrombotic cardiovascular events in patients with a history of MI and high risk for an atherothrombotic event.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for up to 12 months. After 12 months, or if patient is on a bare-metal stent, consideration may be given to switching to a P2Y12 inhibitor such as clopidogrel.
* **Patients treated with ticagrelor 90 mg twice daily who are switched to ticagrelor 60 mg twice daily:** This switch should occur after at least 12 months of treatment with ticagrelor 90 mg twice daily.
* **History of MI (at least 1 year post-MI):** 60 mg orally twice daily.
## Pediatric Dosing
* Ticagrelor is **not** approved for use in pediatric patients. Safety and efficacy have not been established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment necessary in mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Active bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any of its components.
## Adverse Effects
* **Common:** Bleeding (including fatal and life-threatening), dyspnea, bradyarrhythmia.
* **Serious:** Major bleeding, intracranial hemorrhage, ventricular dysfunction.
## Key Drug Interactions
* **Strong CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin):** May increase ticagrelor plasma concentrations. Avoid co-administration.
* **Strong CYP3A4 Inducers (e.g., rifampin, carbamazepine):** May decrease ticagrelor plasma concentrations. Consider alternative agents.
* **CYP3A4 Substrates (e.g., simvastatin, atorvastatin):** Ticagrelor can inhibit CYP3A4 and increase concentrations of these substrates. Dose adjust statins as needed.
* **Aspirin:** Concurrent use increases bleeding risk.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Monitor closely.
* **Proton Pump Inhibitors (PPIs):** Some data suggest potential for reduced ticagrelor efficacy with omeprazole/esomeprazole. Clinical significance is uncertain. Consider antacids or H2 blockers if acid suppression is needed.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Renal Function:** Monitor periodically, especially in patients with pre-existing renal impairment.
* **Liver Function:** Monitor periodically, especially in patients with pre-existing hepatic impairment or those with concerning clinical symptoms.
## Clinical Pearls
* Ticagrelor is a potent antiplatelet agent and increases bleeding risk.
* Discontinue at least 5 days prior to elective surgery.
* The 90 mg twice-daily dose is recommended for ACS, while the 60 mg twice-daily dose is for secondary prevention in patients with established MI.
* Dyspnea is a common side effect and can be dose-limiting for some patients. It does not appear to be related to underlying cardiac or pulmonary disease.
* Ticagrelor is not a P2Y12 prodrug like clopidogrel or prasugrel, and thus does not require hepatic activation.
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*Disclaimer: This information is intended for healthcare professionals and is not a substitute for clinical judgment. Always refer to the most current prescribing information and relevant guidelines for complete details before making any treatment decisions.*
