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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversible P2Y12 receptor antagonist. It is part of dual antiplatelet therapy (DAPT) used to reduce the rate of thrombotic cardiovascular events.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In patients with a history of myocardial infarction (MI) or ACS, ticagrelor is indicated to reduce the rate of cardiovascular death, MI, and stroke. It is typically used in combination with aspirin.
* **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor is indicated to reduce the rate of thrombotic cardiovascular events. It is used in combination with aspirin.
## Adult Dosing
* **ACS:** 180 mg orally once, followed by 90 mg orally twice daily for up to 12 months. Maintenance therapy with 90 mg twice daily can be extended beyond 12 months in select patients.
* **History of MI:** 60 mg orally twice daily.
## Pediatric Dosing
Dosing for pediatric patients is not established.
## Dose Adjustments
No dose adjustments are recommended based on age, sex, or renal/hepatic impairment. However, discontinuation of ticagrelor should be managed carefully due to increased risk of thrombotic events.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
## Adverse Effects
* **Common:** Dyspnea, bleeding (including fatal and life-threatening), bruising.
* **Serious:** Severe bleeding, ventricular pauses, bradyarrhythmias, anaphylaxis.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor exposure. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin) may decrease ticagrelor exposure.
* **CYP3A4 Substrates:** Ticagrelor can increase the plasma concentration of CYP3A4 substrates (e.g., simvastatin, atorvastatin). Limit the dose of statins metabolized by CYP3A4.
* **Aspirin:** Co-administration with aspirin increases bleeding risk.
* **Anticoagulants (e.g., Warfarin, Heparin, DOACs):** Increased risk of bleeding.
* **Nonsteroidal Anti-inflammatory Drugs (NSAIDs):** Increased risk of bleeding.
* **Prophylactic Antithrombotic Therapy:** Concomitant use with other antithrombotic agents should be carefully considered and managed by a clinician.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for signs and symptoms of dyspnea, particularly in patients with a history of asthma or COPD.
* Monitor for bradyarrhythmias.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel and prasugrel which are irreversible. This may lead to a faster offset of action upon discontinuation.
* A loading dose is required for ACS patients.
* Ticagrelor should be taken twice daily, with or without food.
* Patients should be advised to inform their healthcare provider before surgery or if they experience any new bleeding or bruising.
* Long-term use beyond 12 months may be considered in select high-risk patients, but the optimal duration of therapy should be individualized.
* The dose of ticagrelor is not affected by aspirin dose, however, concomitant use of aspirin above 100 mg daily has not been shown to provide additional cardiovascular benefits and may increase bleeding risk.
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***Disclaimer:** This information is intended for healthcare professionals. Always consult the most current prescribing information and relevant clinical guidelines before making therapeutic decisions. This response does not substitute for professional medical advice.*
