Please check your internet connection and try again.
# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally administered, direct-acting, reversible P2Y12 platelet inhibitor. It is a member of the cyclopentyltriazolopyrimidine (CPTP) class.
## Primary Indications
* Inhibition of thrombotic events (myocardial infarction, stroke, and cardiovascular death) in patients with acute coronary syndrome (ACS) or a history of myocardial infarction.
## Adult Dosing
* **ACS:** 180 mg orally once as a 30 mg loading dose, followed by 90 mg orally twice daily for at least 12 months. Continue for as long as clinically indicated, particularly in patients treated with aspirin.
* **Post-MI (at least 1 year after ACS):** In patients with a history of myocardial infarction at least one year prior and at high risk for a thrombotic event, ticagrelor 60 mg twice daily can be considered.
## Pediatric Dosing
* The safety and efficacy of ticagrelor in pediatric patients have not been established.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is necessary for patients with mild to moderate renal impairment. In severe renal impairment, use with caution due to limited data.
* **Hepatic Impairment:** No dose adjustment is necessary for patients with mild to moderate hepatic impairment. Ticagrelor is not recommended in patients with severe hepatic impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack or stroke.
* Hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Common:** Dyspnea, bruising, bleeding (including fatal and severe bleeding).
* **Serious:** Major bleeding, non-major clinically relevant bleeding, ventricular pauses, bradyarrhythmia.
## 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, carbamazepine) may decrease ticagrelor exposure.
* **Aspirin:** Concomitant use increases the risk of bleeding. Dose should be individualized based on risk, but generally aspirin should be continued for the duration of ticagrelor therapy in ACS patients. Maximum maintenance dose of aspirin is generally recommended as 100 mg.
* **Other Antithrombotics:** Concomitant use increases the risk of bleeding.
* **Statins:** Ticagrelor can increase the exposure of some statins metabolized by CYP3A4 (e.g., simvastatin, atorvastatin).
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for signs and symptoms of dyspnea.
* Evaluate the need for continued dual antiplatelet therapy based on individual patient risk for thrombotic events versus bleeding.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, meaning platelet aggregation returns to normal levels more quickly after discontinuation compared to clopidogrel.
* The 90 mg twice daily dose is indicated for ACS patients for at least 12 months.
* The 60 mg twice daily dose is for long-term use in post-MI patients at high risk for thrombotic events.
* Dyspnea is a common side effect and is generally not an indication to discontinue ticagrelor unless severe or bothersome.
* Consider discontinuation of ticagrelor prior to elective surgery, with the timing dependent on the thrombotic risk and bleeding risk.
***
*Disclaimer: This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the current prescribing information and relevant guidelines before administering any medication.*
