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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally administered, direct-acting, reversible P2Y12 platelet inhibitor.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI).
* In combination with aspirin, for patients with acute coronary syndrome (ACS).
## Adult Dosing
* **Following ACS:** 180 mg orally twice daily for the first week, followed by 90 mg orally twice daily.
* **Following MI (at least 1 year ago):** 90 mg orally twice daily.
* **Maintenance Dose:** If initiated in the hospital for ACS, continued maintenance dose is 90 mg twice daily. If continued after 1 year post-MI, may be reduced to 60 mg twice daily (consult prescribing information for specific criteria).
* **Dose Reduction:** For patients who have experienced an ACS and are at increased risk of bleeding, a maintenance dose of 60 mg twice daily may be considered after 12 months of treatment with 90 mg twice daily (consult prescribing information for specific criteria).
## Pediatric Dosing
There is no established pediatric dosing for ticagrelor.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment necessary in mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (including major and minor), bradycardia, ventricular pauses.
* **Serious:** Major bleeding, clinically significant bradyarrhythmias, intracranial bleeding, respiratory issues.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor levels. Strong inducers (e.g., rifampin, phenytoin) can decrease ticagrelor levels. Coadministration with strong CYP3A4 inhibitors is generally not recommended.
* **CYP3A4 Substrates:** Ticagrelor can increase the concentration of CYP3A4 substrates (e.g., simvastatin, atorvastatin). Limit doses of statins metabolized by CYP3A4 to 40 mg daily for simvastatin and 80 mg daily for atorvastatin.
* **Other Antithrombotics:** Concomitant use with other antithrombotics (e.g., aspirin, warfarin, heparin, clopidogrel, NSAIDs) increases the risk of bleeding.
* **Digoxin:** Ticagrelor can increase digoxin concentrations. Monitor digoxin levels and adjust dose as needed.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Bradycardia:** ECG monitoring may be considered, particularly in patients with pre-existing risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor with a faster onset and offset of action compared to clopidogrel, and it is not a prodrug, meaning it does not require metabolic activation.
* Dyspnea is a common side effect, often transient, and may require discontinuation if persistent or severe.
* Consider the bleeding risk versus thrombotic risk when deciding on duration of therapy and dose reduction.
* Avoid concomitant use with strong CYP3A4 inhibitors.
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*This information is intended for healthcare professionals. Always consult the most current prescribing information and relevant guidelines before making treatment decisions.*
