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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor. It prevents adenosine triphosphate from binding to its P2Y12 receptor on platelets, thus inhibiting platelet activation and aggregation.
## Primary Indications
* **Acute Coronary Syndromes (ACS):** To reduce the rate of thrombotic cardiovascular events, in combination with aspirin, in patients with ACS (unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction).
* **Myocardial Infarction (MI):** Following an MI with known history of MI, to reduce the rate of thrombotic cardiovascular events.
## Adult Dosing
* **ACS:** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily for at least 12 months. A lower dose of 60 mg twice daily may be considered for long-term maintenance therapy (beyond 12 months) in patients who have been treated with ticagrelor and aspirin and are not at high risk of bleeding or stent thrombosis.
* **Post-MI:** 60 mg orally twice daily.
## Pediatric Dosing
Ticagrelor is not recommended for use in pediatric patients due to a lack of data.
## Dose Adjustments
No dose adjustments are required for renal or hepatic impairment. However, caution is advised in patients with severe hepatic impairment.
## Contraindications
* History of intracranial hemorrhage.
* Active serious bleeding (e.g., gastrointestinal bleed, intracerebral hemorrhage).
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Common:** Dyspnea, bleeding (including major and minor), contusion.
* **Serious:** Life-threatening bleeding, cardiac arrest, ventricular arrhythmia.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors may increase ticagrelor levels (e.g., ketoconazole, clarithromycin). Strong inducers may decrease ticagrelor levels (e.g., rifampin, phenytoin).
* **Strong CYP3A4 Substrates:** Ticagrelor may increase concentrations of some strong CYP3A4 substrates (e.g., simvastatin, lovastatin - maximum dose 40 mg daily recommended).
* **Aspirin:** Concomitant use with aspirin increases the risk of bleeding. Maintenance aspirin dose should be at the lowest effective dose, generally not exceeding 100 mg.
* **P-gp Inhibitors:** May increase ticagrelor exposure.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Assess for dyspnea.
* Consider monitoring for any new or worsening symptoms of cardiac events.
## Clinical Pearls
* Ticagrelor should be taken with or without food.
* Patients on ticagrelor should be advised to stop aspirin before initiating ticagrelor if they are not indicated for combination therapy, or to use the lowest effective dose of aspirin if used concurrently.
* Discontinuation of ticagrelor prematurely increases the risk of stent thrombosis, MI, and death.
* Dyspnea is a common side effect and is typically not associated with worsening cardiac function.
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**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 professional guidelines before making any clinical decisions.
