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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an oral, direct-acting P2Y12 platelet inhibitor 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
* Treatment of patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI) with a low to moderate risk of stent thrombosis and other thrombotic events.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months.
* **For patients who are switching from clopidogrel or prasugrel:** Initiate ticagrelor 90 mg twice daily.
* **For patients who have had a prior treatment of ticagrelor 180 mg loading dose followed by 90 mg twice daily:** Consider continuing 90 mg twice daily.
* **History of MI (≥1 year):** For patients with a history of MI, ticagrelor 60 mg twice daily can be considered to reduce the rate of thrombotic cardiovascular events.
* **Duration:** Continue for at least 12 months, in addition to aspirin and other standard therapies. The optimal duration of treatment is not well-defined and depends on individual patient risk.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* No dose adjustment is necessary for patients with mild to moderate hepatic impairment.
* No dose adjustment is necessary for patients with renal impairment.
## Contraindications
* Active pathological bleeding.
* History of intracerebral hemorrhage.
* Known hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Common:** Dyspnea, bradycardia, non-ischemic chest pain, accidental injury, contusions, rash, diarrhea, headache, fatigue.
* **Serious:** Bleeding (major, minor, including fatal), ventricular pauses.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor exposure. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure.
* **CYP3A4 Substrates (e.g., simvastatin, atorvastatin):** Ticagrelor can increase plasma concentrations of statins metabolized by CYP3A4.
* **P-glycoprotein (P-gp) Substrates:** Ticagrelor can increase plasma concentrations of P-gp substrates (e.g., digoxin).
* **Aspirin:** Combination with aspirin is generally recommended for ACS patients. However, increased risk of bleeding.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for symptomatic bradycardia.
## Clinical Pearls
* Ticagrelor is dosed twice daily, unlike clopidogrel and prasugrel.
* Dyspnea is a common side effect and is usually not indicative of underlying cardiac or pulmonary disease.
* Discontinuation of ticagrelor increases the risk of stent thrombosis, MI, and death. If possible, resume ticagrelor as soon as possible after discontinuation due to a bleeding event.
* Ticagrelor is not a prodrug and does not require metabolic activation, leading to more rapid and consistent platelet inhibition compared to clopidogrel.
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*This information is intended for healthcare professionals. Please consult the most current prescribing information for complete details.*
