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 (including stent thrombosis) in patients with a history of myocardial infarction (MI).
* In combination with aspirin, for the treatment of acute coronary syndrome (ACS).
## Adult Dosing
* **Acute Coronary Syndrome (ACS):**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for up to 12 months. Some patients may benefit from longer treatment; duration should be individualized.
* **History of Myocardial Infarction (MI):**
* **Maintenance Dose:** 60 mg orally twice daily.
* **Duration:** Continued treatment beyond 12 months should be considered based on individual patient risk for thrombotic events and bleeding.
## Pediatric Dosing
* Ticagrelor is not approved for use in pediatric patients.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is necessary in mild to moderate hepatic impairment. Data in severe hepatic impairment is limited; caution is advised.
* **Renal Impairment:** No dose adjustment is necessary in mild to moderate renal impairment. Data in severe renal impairment is limited; caution is advised.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its components.
## Adverse Effects
* **Most Common:** Dyspnea, bradycardia, bleeding (including gastrointestinal, subcutaneous, and genitourinary).
* **Serious:** Major bleeding, life-threatening bleeding, ventricular pauses, serious skin reactions (e.g., Stevens-Johnson syndrome).
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor inhibits CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor exposure; consider dose reduction of the interacting drug or increased monitoring. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure; consider alternative antiplatelet therapy if coadministration is necessary.
* **P-glycoprotein (P-gp) Substrates:** Ticagrelor inhibits P-gp. Concomitant use with P-gp substrates with narrow therapeutic index (e.g., digoxin, cyclosporine) may increase exposure to the substrate; monitor therapeutic drug levels.
* **Aspirin:** Increased risk of bleeding. Continue aspirin for ACS indication. For patients with a history of MI, ticagrelor 60 mg twice daily is approved for use with aspirin. Long-term use of ticagrelor with aspirin at doses higher than 100 mg daily increases the risk of bleeding.
* **Other Antithrombotics:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea and bradycardia, especially in patients with underlying conditions.
* Consider monitoring of drug concentrations in select cases (e.g., poor response, suspected non-adherence), though not routinely recommended.
## Clinical Pearls
* Ticagrelor's onset of action is rapid.
* If a dose is missed, the patient should take the next dose at the scheduled time. Do not double doses.
* Discontinuation of ticagrelor, especially within the first few days of ACS, increases the risk of stent thrombosis, MI, and death. If discontinuation is necessary, consider the risks versus benefits.
***
**Disclaimer:** This information is intended for clinical professionals and is not exhaustive. Always consult the official prescribing information and relevant clinical guidelines for complete and current information before making treatment decisions.
