Please check your internet connection and try again.
# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
* Prevention of stent thrombosis in patients treated with coronary stents.
## Adult Dosing
* **ACS:**
* Loading Dose: 180 mg orally once.
* Maintenance Dose: 90 mg orally twice daily for at least 12 months. Duration may be extended based on clinical assessment.
* **History of MI (≥ 1 year post-ACS/MI):**
* 90 mg orally twice daily. In patients with a history of MI, ticagrelor 90 mg twice daily has been shown to further reduce the risk of MI or stroke compared to placebo. Consider adding low-dose aspirin if not otherwise contraindicated.
* **Stent Thrombosis (in patients treated with coronary stents):**
* Dose adjustment is not specified in current guidelines. Standard ACS dosing is typically used.
## Pediatric Dosing
* Dosing for pediatric patients has not been established.
## Dose Adjustments
* No dose adjustment is needed for patients with mild to moderate hepatic impairment.
* No dose adjustment is needed for patients with mild to moderate renal impairment.
* Caution is advised in severe hepatic impairment; use is not recommended.
* Caution is advised in severe renal impairment; use is not recommended.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Common:** Dyspnea, bleeding (including fatal and life-threatening), bruising.
* **Serious:** Major bleeding, intracranial hemorrhage, ventricular pauses, hyperkalemia, angioedema.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) can increase ticagrelor exposure; avoid or use with caution. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) can decrease ticagrelor exposure; avoid.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and consider risk-benefit.
* **Aspirin:** Generally co-administered with aspirin in ACS. High-dose aspirin may reduce ticagrelor's efficacy.
* **Statins:** Concomitant use with moderate to strong CYP3A4 inhibiting statins (e.g., simvastatin, atorvastatin) can increase statin exposure. Limit simvastatin and atorvastatin doses to 40 mg daily (or equivalent).
## Monitoring
* **Bleeding:** Monitor closely for signs and symptoms of bleeding.
* **Renal Function:** Monitor periodically.
* **Hepatic Function:** Monitor periodically, especially in patients with severe impairment.
* **Potassium:** Monitor periodically, especially in patients with risk factors for hyperkalemia.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor, distinct from clopidogrel and prasugrel, and does not require metabolic activation.
* The recommended maintenance dose in ACS is 90 mg twice daily. For patients established on ticagrelor for at least 1 year post-ACS, a switch to 90 mg twice daily +/- low-dose aspirin may be considered for secondary prevention.
* Dyspnea is a common side effect and may require discontinuation if severe.
* Ticagrelor should be taken for at least 12 months in ACS patients regardless of stent type.
* Discontinuation of ticagrelor should be avoided if possible, especially within the first few months after ACS or stenting, due to increased risk of thrombotic events. If discontinuation is necessary, consider the risks of stopping dual antiplatelet therapy.
***
*This information is intended for clinical use and does not replace the need to consult the official prescribing information and current clinical guidelines.*
