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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally active, direct-acting P2Y$_{12}$ receptor antagonist. It is a member of the cyclopentyltriazolopyrimidine (CPTP) class.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the reduction of thrombotic cardiovascular events (e.g., cardiovascular death, myocardial infarction, stroke) in patients with a history of ACS.
* **Myocardial Infarction (MI) with ST-segment elevation:** In patients who have had a myocardial infarction with ST-segment elevation (STEMI) and are treated with percutaneous coronary intervention (PCI).
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months, or up to 30 months if tolerated and indicated.
* **MI with STEMI:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* **Secondary Prevention (after MI):** For patients with a history of MI, ticagrelor 60 mg twice daily can be considered in addition to aspirin in select patients who are at high risk of occlusive events.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is necessary in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment is necessary in patients with mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Common:** Dyspnea, bradycardia, ventricular pauses, bleeding (including fatal and life-threatening).
* **Serious:** Hemorrhage, clinically significant bradycardia, ventricular pauses.
## 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 and risk of bleeding. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease ticagrelor exposure.
* **CYP3A4 Substrates:** Ticagrelor can inhibit P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). Coadministration with substrates of these transporters may increase their plasma concentrations (e.g., digoxin, rosuvastatin).
* **Aspirin:** Increased risk of bleeding. Generally used in combination.
* **Anticoagulants (e.g., warfarin, heparin, direct oral anticoagulants):** Increased risk of bleeding. Combination therapy is generally not recommended unless clinically indicated and with careful monitoring.
* **NSAIDs:** Increased risk of bleeding.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Heart Rate:** Ticagrelor can cause asymptomatic bradycardia.
## Clinical Pearls
* Ticagrelor is a reversible P2Y$_{12}$ inhibitor, unlike clopidogrel.
* Discontinuation of ticagrelor prematurely increases the risk of thrombotic events.
* Patients experiencing dyspnea should have their cardiac and pulmonary status evaluated. Dyspnea often resolves with continued treatment.
* Dose of aspirin: Ticagrelor should be used in combination with aspirin. The maintenance dose of aspirin should generally not exceed 100 mg daily. Higher doses of aspirin have been associated with increased bleeding risk.
* The 60 mg twice daily dose is indicated for secondary prevention after MI in select high-risk patients.
This information is intended for educational purposes only and does not constitute medical advice. Always consult current prescribing information and your healthcare provider for definitive guidance.
