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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversible P2Y12 platelet inhibitor used to prevent thrombotic events. It is part of dual antiplatelet therapy (DAPT).
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with 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 recurrent events.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. Following this, consider 60 mg orally twice daily based on individual patient risk assessment.
* **History of MI with risk factors:** 60 mg orally twice daily.
## Pediatric Dosing
No established pediatric dosing. Use in pediatric patients is not recommended.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary in mild to moderate hepatic impairment. Safety and efficacy in severe hepatic impairment have not been studied.
* **Renal Impairment:** No dose adjustment necessary in mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Hypersensitivity to ticagrelor or any of its components.
## Adverse Effects
* **Common:** Dyspnea, bradycardia, hypotension, hyperkalemia, increased serum creatinine, diarrhea, rash.
* **Serious:** Bleeding (major, minor, intracranial, fatal), ventricular pauses, angioedema.
## 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 with narrow therapeutic index:** Avoid concomitant use with strong CYP3A4 substrates with a narrow therapeutic index (e.g., simvastatin, lovastatin).
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and monitor closely.
* **Proton Pump Inhibitors (PPIs):** Some studies suggest PPIs may decrease ticagrelor efficacy, particularly omeprazole and esomeprazole. The clinical significance is uncertain.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Heart Rate:** Ticagrelor can cause asymptomatic bradycardia.
* **Renal Function:** Monitor serum creatinine.
* **Electrolytes:** Monitor potassium levels, especially in patients with risk factors for hyperkalemia.
## Clinical Pearls
* Ticagrelor is dosed twice daily, regardless of loading or maintenance dose.
* The 90 mg twice daily dose is generally used for 12 months after ACS, then a 60 mg twice daily dose can be considered based on risk.
* Dyspnea is a common side effect and is usually mild and transient, but consider underlying cardiac causes if persistent.
* Discontinuation of ticagrelor should be carefully considered, as it increases the risk of thrombotic events. If interruption is necessary, weigh the risks of bleeding against the risks of thrombosis.
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*Please verify current prescribing information and local protocols for the most up-to-date recommendations.*
