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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an oral, direct-acting, reversible P2Y12 platelet inhibitor. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** To reduce the rate of thrombotic cardiovascular events in patients with ACS (unstable angina, non-ST-elevation MI, or ST-elevation MI).
* **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor, in combination with aspirin, is indicated to decrease the rate of cardiovascular death, MI, and stroke.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* **Duration:** For at least 12 months, or longer in select patients based on risk assessment, in combination with aspirin.
* **History of MI:**
* **Maintenance Dose:** 60 mg orally twice daily.
* **Duration:** For patients who have had an MI more than 1 year ago and are currently treated with ticagrelor 90 mg twice daily and aspirin. Therapy may be continued as long as the patient is free of further ischemic events and has a low bleeding risk.
* **Aspirin Dose:** Ticagrelor is used in combination with aspirin. The recommended maintenance dose of aspirin is typically 75-100 mg once daily. The dose of aspirin should not exceed 100 mg once daily when used with ticagrelor.
## Pediatric Dosing
Ticagrelor is not approved for use in pediatric patients.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is recommended in patients with mild to moderate hepatic impairment. Ticagrelor has not been studied in severe hepatic impairment and should be used with caution.
* **Renal Impairment:** No dose adjustment is recommended in patients with mild to moderate renal impairment. In patients with severe renal impairment, consider the 60 mg twice daily dose after the initial loading dose for ACS.
## Contraindications
* Hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke. (For the 180 mg loading dose in ACS, patients with a history of stroke or TIA should receive 90 mg twice daily.)
## Adverse Effects
* **Most Common:** Bleeding (major and minor), dyspnea, bradyarrhythmia, accidental trauma.
* **Serious:** Life-threatening or fatal bleeding, severe dyspnea, ventricular pauses.
* **Other:** Bruising, hypercholesterolemia, hypertension, nausea, diarrhea.
* **Rare:** Angioedema, interstitial lung disease.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor exposure. Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) can decrease ticagrelor exposure.
* **CYP3A4 Substrates:** Ticagrelor can inhibit CYP3A4 and increase the exposure of substrates like simvastatin and atorvastatin. Avoid concomitant use of ticagrelor with simvastatin or atorvastatin at doses greater than 40 mg.
* **Other Antiplatelet Agents/Anticoagulants:** Increased risk of bleeding. Exercise caution.
* **Omeprazole/Esomeprazole:** Concomitant administration may reduce ticagrelor exposure. Administer ticagrelor at least 12 hours after omeprazole or esomeprazole.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Assess for dyspnea, especially if severe or persistent.
* Monitor lipid profiles.
* Consider cardiac monitoring for patients with risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, meaning its effect can be more rapidly reversed upon discontinuation compared to clopidogrel.
* The 180 mg loading dose in ACS is crucial for rapid platelet inhibition.
* Ticagrelor is associated with a higher rate of dyspnea compared to clopidogrel. This is often transient but requires evaluation.
* Discontinue ticagrelor 5 days prior to elective surgery if possible.
* The 60 mg twice daily dose is indicated for long-term maintenance in patients with a history of MI who have completed 1 year of treatment with ticagrelor 90 mg twice daily, particularly if they are at higher risk of bleeding.
**Disclaimer:** This information is intended for clinical pharmacy professionals and is not a substitute for professional medical judgment. Always consult the most current prescribing information and relevant clinical guidelines before making therapeutic decisions.
