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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the prevention of thrombotic events (e.g., myocardial infarction, stroke) in patients with ACS.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. May be continued beyond 12 months if the risk of ischemic events outweighs the risk of bleeding.
* **History of MI (1 year or more ago) and at least one additional risk factor for occlusive vascular disease:**
* **Maintenance Dose:** 60 mg orally twice daily.
## Pediatric Dosing
* Ticagrelor is **not recommended** for use in pediatric patients due to a lack of data.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment needed for mild to moderate hepatic impairment. Data in severe hepatic impairment is limited; use with caution.
* **Renal Impairment:** No dose adjustment needed for mild to moderate renal impairment. Data in severe renal impairment is limited; use with caution.
## Contraindications
* Active bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its components.
## Adverse Effects
* **Bleeding:** Dyspnea, bruising, hematuria, epistaxis, gastrointestinal bleeding, and intracranial hemorrhage. This is the most common and serious adverse effect.
* **Dyspnea:** Often mild and transient.
* **Bradycardia:**
* **Increased Serum Creatinine:**
* **Increased Uric Acid:**
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor exposure. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin) may decrease ticagrelor exposure.
* **P-glycoprotein (P-gp) Inhibitors:** Ticagrelor is also a substrate of P-gp. Concomitant use with strong P-gp inhibitors may increase ticagrelor exposure.
* **Other Antiplatelet Agents/Anticoagulants:** Increased risk of bleeding. Use with caution and monitor closely.
* **Aspirin:** Used concurrently in ACS, but prolonged use of aspirin >100 mg daily may increase bleeding risk.
* **Simvastatin/Atorvastatin:** Ticagrelor inhibits OATP1B1/1B3, leading to increased statin exposure. Consider reducing the dose of simvastatin or atorvastatin.
## Monitoring
* **Bleeding:** Assess for signs and symptoms of bleeding (e.g., hematuria, melena, bruising, epistaxis).
* **Renal Function:** Monitor serum creatinine.
* **Uric Acid Levels:**
* **ECG:** For bradycardia.
## Clinical Pearls
* Ticagrelor is a direct-acting, reversibly binding P2Y12 inhibitor, distinguishing it from clopidogrel (irreversible) and prasugrel (irreversible).
* The most significant risk with ticagrelor is bleeding. Risk stratification is crucial when initiating therapy.
* Dyspnea is a common side effect and usually does not require discontinuation. Assess for other causes if severe or persistent.
* Aspirin is recommended lifelong with ticagrelor in ACS patients unless contraindicated. However, the dose of aspirin should be kept as low as clinically appropriate.
* Dose of ticagrelor is 90 mg BID for ACS and 60 mg BID for those with prior MI and additional risk factors.
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**Disclaimer:** This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult with a qualified healthcare provider and refer to the most current prescribing information for ticagrelor before making any treatment decisions.
