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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or ACS.
* **Prevention of stent thrombosis:** In patients treated with percutaneous coronary intervention (PCI).
## 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 risk of ischemic events outweighs the risk of bleeding. If bleeding risk is high, consider 60 mg twice daily.
* **Maintenance:** Patients who have completed at least 12 months of treatment with 90 mg twice daily, may transition to 60 mg twice daily for up to an additional 24 months (total treatment duration of up to 36 months) if the benefit outweighs the risk.
## Pediatric Dosing
The safety and efficacy of ticagrelor in pediatric patients have not been established.
## Dose Adjustments
No dose adjustment is required for patients with hepatic or renal impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Concomitant use with strong CYP3A4 inhibitors.
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (including major and minor), contusion.
* **Serious:** Severe bleeding, ventricular pauses, bradycardia.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir).
* **CYP3A4 Inducers:** May decrease ticagrelor exposure. Monitor for reduced efficacy.
* **P-glycoprotein (P-gp) Substrates:** Ticagrelor is a P-gp inhibitor. Monitor for increased concentrations of P-gp substrates (e.g., digoxin).
* **Aspirin:** Generally used concomitantly. However, prolonged use of higher-dose aspirin (>100 mg) may reduce the antiplatelet effect of ticagrelor and increase bleeding risk.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Dyspnea:** Monitor for new-onset or worsening dyspnea.
* **Bradycardia:** ECG monitoring may be considered, especially in patients with risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor's onset of action is rapid, and its effect is reversible upon discontinuation.
* It is not a prodrug and does not require metabolic activation.
* Patients should be advised to continue ticagrelor treatment as prescribed and not to stop prematurely, even if they feel better, as this can increase the risk of stent thrombosis or other thrombotic events.
* Management of bleeding requires assessment of severity and consideration of discontinuation and/or reversal strategies.
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**Disclaimer:** This information is intended for clinical pharmacists and should not be considered a substitute for comprehensive prescribing information. Always consult the official product monograph and local protocols for complete and up-to-date guidance.
