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## Ticagrelor (Brilinta)
### Overview
Ticagrelor is an oral antiplatelet medication that reversibly inhibits the P2Y12 receptor on platelets, preventing platelet activation and aggregation.
### Primary Indications
* Reduction of thrombotic cardiovascular events (including myocardial infarction and stroke) in patients with acute coronary syndrome (ACS) or a history of myocardial infarction.
### Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. In some patients, continuation beyond 12 months may be considered, balancing benefit against bleeding risk.
* **Post-Myocardial Infarction (MI):**
* **Maintenance Dose:** 60 mg orally twice daily for up to 36 months.
### Pediatric Dosing
* Ticagrelor is **not recommended** for use in pediatric patients. Safety and efficacy have not been established.
### Dose Adjustments
* **Hepatic Impairment:** No dose adjustment needed in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment needed.
### Contraindications
* Active bleeding.
* History of intracerebral hemorrhage.
* Hypersensitivity to ticagrelor or any component of the formulation.
### Adverse Effects
* **Most Common:** Bleeding (including fatal and major bleeding), dyspnea, bradycardia.
* **Other Significant:** Ventricular pauses, increased serum creatinine, increased uric acid levels, cough.
### Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) may increase ticagrelor exposure; caution and potential dose reduction of the interacting drug may be warranted. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure.
* **Other Antiplatelet Agents/Anticoagulants:** Increased risk of bleeding. Use with caution and consider the net clinical benefit.
* **Proton Pump Inhibitors (PPIs):** Some data suggest PPIs may reduce ticagrelor efficacy, potentially via CYP2C19 inhibition. The clinical significance is debated, and guidelines vary; consult local protocols.
* **Simvastatin/Atorvastatin:** Ticagrelor can increase statin concentrations. Limit simvastatin to 40 mg daily and atorvastatin to 80 mg daily.
### Monitoring
* **Bleeding:** Closely monitor for signs and symptoms of bleeding.
* **Renal Function:** Monitor serum creatinine periodically.
* **Uric Acid:** Monitor uric acid levels periodically.
* **Heart Rate:** Monitor for bradycardia, especially in patients with predisposing factors.
### Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, distinguishing it from clopidogrel and prasugrel.
* It has a faster onset and offset of action compared to clopidogrel.
* The most common side effect is dyspnea, which is often transient and not necessarily indicative of cardiac dysfunction.
* Discontinuation of ticagrelor increases the risk of thrombotic events; ensure appropriate duration of therapy based on patient indication and risk assessment.
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*This information is intended for healthcare professionals and does not substitute for comprehensive drug information resources or clinical judgment. Always verify current prescribing information with the manufacturer's official product insert or other reliable sources before making clinical decisions.*
