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# Ticagrelor
## Overview
Ticagrelor is an oral P2Y12 platelet inhibitor. It is a direct-acting, reversible antagonist of the P2Y12 receptor.
## Primary Indications
* In combination with aspirin, for the prevention of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI).
* In combination with aspirin, for the prevention of stent thrombosis in patients treated with a coronary stent.
* In combination with aspirin and clopidogrel (or other P2Y12 inhibitor), for the prevention of thrombotic events in patients with acute coronary syndrome (ACS).
## Adult Dosing
* **Acute Coronary Syndrome (ACS):** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily.
* **Post-Myocardial Infarction (MI) and Stent Thrombosis Prevention:** 90 mg orally twice daily.
* **Maintenance Therapy:** For patients already on ticagrelor 90 mg twice daily, following ACS, the dose may be reduced to 60 mg twice daily after at least 12 months of treatment if the risk of ischemic events outweighs the risk of bleeding.
## Pediatric Dosing
* Ticagrelor is not recommended in pediatric patients. Safety and efficacy have not been established.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is required for patients with mild, moderate, or severe renal impairment.
* **Hepatic Impairment:** No dose adjustment is required for patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
## Contraindications
* Concomitant use with strong CYP3A4 inhibitors.
* History of hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (including fatal and life-threatening).
* **Serious:** Bleeding, ventricular pauses, bradyarrhythmias.
## Key Drug Interactions
* **CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin):** Increased ticagrelor exposure; avoid concomitant use.
* **CYP3A4 Inducers (e.g., rifampin, phenytoin):** Decreased ticagrelor exposure; use with caution.
* **Strong CYP3A4 Substrates (e.g., simvastatin, atorvastatin):** Ticagrelor can increase the exposure of these drugs.
* **Aspirin:** Concurrent use is recommended for primary indications. Higher maintenance doses of aspirin (>100 mg) may decrease the efficacy of ticagrelor and increase bleeding risk.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for bradycardia; electrocardiogram (ECG) monitoring may be considered during the initial treatment period, especially in patients with risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel and prasugrel which are irreversible.
* Dyspnea is a common side effect and typically resolves with continued treatment. If severe, consider alternative therapy.
* Discontinuation of ticagrelor increases the risk of thrombotic events. If ticagrelor must be discontinued for any reason, resume as soon as possible.
* Patients who are CYP2C19 poor metabolizers may have reduced response to clopidogrel, making ticagrelor a potentially more effective alternative.
* Avoid concomitant use of ticagrelor with a high maintenance dose of aspirin (greater than 100 mg daily) in patients with ACS.
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*Disclaimer: This information is intended for healthcare professionals and does not replace the need to consult the official prescribing information or other relevant resources for the most current and comprehensive drug details.*
