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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, thus inhibiting platelet activation and aggregation.
## Primary Indications
* Reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI) with management of ACS.
## Adult Dosing
* **ACS:** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily for at least 12 months. After 12 months, consider continuing 90 mg twice daily if the patient is at high risk for further thrombotic events and low risk for bleeding.
* **History of MI (with >1 year elapsed since ACS/MI):** For patients with a history of MI at least one year ago who are at high risk for an atherothrombotic event, ticagrelor 60 mg orally twice daily may be considered.
## Pediatric Dosing
* Ticagrelor is not recommended for use in pediatric patients due to a lack of data.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary.
* **Renal Impairment:** No dose adjustment necessary.
## Contraindications
* Hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding.
## Adverse Effects
* **Common:** Bleeding (major and minor, including intracranial and fatal bleeding), dyspnea, bradycardia, ventricular pauses, hyperuricemia, and elevated serum creatinine.
* **Serious:** Severe bleeding, anaphylaxis.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) may increase ticagrelor concentrations. Co-administration with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor concentrations.
* **Other Antiplatelet Agents:** Increased risk of bleeding.
* **Anticoagulants (e.g., warfarin, direct oral anticoagulants):** Increased risk of bleeding.
* **Aspirin:** While often used concurrently, the risk of bleeding increases. Discontinuation of aspirin should be based on clinical assessment.
* **Potent CYP3A4 Inhibitors (e.g., Simvastatin, Atorvastatin):** Ticagrelor can increase plasma concentrations of statins metabolized by CYP3A4, increasing the risk of myopathy. Dose reductions of certain statins may be necessary.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea.
* Consider monitoring uric acid and creatinine levels periodically.
## Clinical Pearls
* Ticagrelor has a more rapid onset and offset of action compared to clopidogrel.
* Dyspnea is a common side effect and may require discontinuation if severe or persistent.
* Avoid concomitant use with strong CYP3A4 inhibitors or inducers unless clinically necessary and closely monitored.
* Discontinuation of ticagrelor should be carefully considered, especially within the first year after ACS/MI, due to increased risk of thrombotic events.
* The 60 mg twice daily dose is indicated for secondary prevention in patients with established MI at least one year prior.
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***Disclaimer:** This information is intended for healthcare professionals. Always consult the most current prescribing information and institutional protocols for complete details and to ensure patient safety.*
