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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally administered, direct-acting, reversibly binding P2Y12 receptor antagonist.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
* **Off-label:** Prevention of stent thrombosis in patients with coronary artery stents.
## Adult Dosing
* **ACS:** A 180 mg loading dose on day 1, followed by 90 mg twice daily for at least 12 months, then potentially 60 mg twice daily.
* **History of MI (at least 1 year post-MI and ACS event):** 60 mg twice daily.
* **Duration of therapy:** Typically 12 months for ACS, but may be extended in certain patient populations. Longer duration should be individualized based on bleeding risk and ischemic benefit.
## Pediatric Dosing
There is no established pediatric dosing for ticagrelor.
## Dose Adjustments
No dose adjustments are needed for renal or hepatic impairment. However, caution is advised in severe hepatic impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any component of the formulation.
* Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir).
## Adverse Effects
* **Most common:** Dyspnea, bleeding (major, minor, including fatal), bradycardia.
* **Serious:** Significant bleeding events, ventricular pauses.
* **Other:** Hypersensitivity reactions, elevated serum creatinine and uric acid.
## Key Drug Interactions
* **CYP3A4 substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concurrent use with statins (especially simvastatin and atorvastatin at high doses) may increase statin concentrations; use lower doses of statins or avoid.
* **CYP3A4 inducers:** May decrease ticagrelor efficacy (e.g., rifampin, carbamazepine, phenytoin).
* **Strong CYP3A4 inhibitors:** Contraindicated due to increased ticagrelor exposure and risk of bleeding.
* **Other antiplatelets/anticoagulants:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea.
* Renal and hepatic function may be monitored periodically.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor and should be part of a dual antiplatelet therapy (DAPT) regimen following ACS or PCI.
* The 180 mg loading dose is crucial for rapid platelet inhibition.
* Dyspnea is a common side effect, often transient and not clinically significant, but should be assessed for underlying cardiac causes.
* Switching from clopidogrel to ticagrelor requires a loading dose. Switching from ticagrelor to clopidogrel does not require a loading dose.
* Discontinuation of ticagrelor, especially within the first year after ACS, increases the risk of thrombotic events.
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*This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines before making any treatment decisions.*
