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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 receptor antagonist. It is used to reduce the rate of thrombotic cardiovascular events, such as cardiovascular death, myocardial infarction, and stroke, in patients with acute coronary syndrome (ACS) or a history of myocardial infarction.
## Primary Indications
* Treatment of acute coronary syndrome (ACS).
* Reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) and at least one additional risk factor for occlusive atherothrombotic events.
## Adult Dosing
* **ACS:** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily.
* **History of MI:** 60 mg orally twice daily.
## Pediatric Dosing
* Safety and efficacy have not been established in pediatric patients.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment needed in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to potential for increased exposure.
* **Renal Impairment:** No dose adjustment needed in mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Known hypersensitivity to ticagrelor or any of its components.
* Active pathological bleeding (e.g., peptic ulcer or intracranial hemorrhage).
## Adverse Effects
* **Most Common:** Bleeding (e.g., ecchymosis, epistaxis, gastrointestinal bleeding, genitourinary bleeding), dyspnea, bradycardia.
* **Serious:** Major bleeding, ventricular pauses.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor exposure and risk of bleeding. Coadministration with strong CYP3A4 inducers (e.g., rifampin, phenytoin) can decrease ticagrelor exposure and efficacy.
* **CYP3A4 Substrates:** Ticagrelor can inhibit OATP1B1/3, potentially increasing plasma concentrations of statins metabolized by these transporters.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use concurrently with caution and consider risks and benefits.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea.
* Consider baseline and periodic assessment of renal and hepatic function.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor with a faster onset and offset of action compared to clopidogrel.
* The 180 mg loading dose is crucial for optimal efficacy in ACS.
* Dyspnea is a common side effect, usually transient and not associated with underlying pulmonary disease.
* Ticagrelor should be continued for at least 12 months in ACS patients unless contraindicated.
* For patients with a history of MI, the 60 mg twice-daily dose is used.
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*This information is intended for healthcare professionals. It is essential to consult the most current prescribing information and relevant clinical guidelines for complete details and to ensure patient safety.*
