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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally active, direct-acting P2Y$_{12}$ receptor antagonist that reversibly inhibits platelet aggregation.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the reduction of thrombotic cardiovascular events in patients with ACS (unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction).
* **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor is indicated in combination with aspirin to reduce the rate of cardiovascular death, myocardial infarction, and stroke, following an appropriate loading dose and treatment of acute coronary syndrome.
## Adult Dosing
* **ACS:** 180 mg loading dose once, followed by 90 mg twice daily for at least 12 months. After 12 months, consider continuing 90 mg twice daily if the patient is at high risk for ischemic events and low risk for bleeding. In patients who have not had an in-stent restenosis, doses of 60 mg twice daily may be considered after at least 12 months of treatment.
* **History of MI:** 60 mg twice daily.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* No dose adjustment is necessary for patients with mild to moderate renal or hepatic impairment.
* For patients with severe renal impairment or end-stage renal disease (ESRD), consider the risks and benefits, as data are limited.
* For patients with severe hepatic impairment, ticagrelor should be used with caution.
## Contraindications
* Active pathological bleeding.
* History of intracerebral hemorrhage.
* Hypersensitivity to ticagrelor or any of its components.
* Concomitant administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin).
## Adverse Effects
* **Common:** Bleeding (major and minor), dyspnea, bradycardia, hyperuricemia, elevated serum creatinine.
* **Serious:** Life-threatening bleeding, anaphylaxis.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Coadministration with sensitive CYP3A4 substrates (e.g., simvastatin, atorvastatin) may increase exposure to these drugs.
* **CYP3A4 Inducers (e.g., rifampin, phenytoin, carbamazepine, St. John's wort):** May decrease ticagrelor exposure and efficacy.
* **P-glycoprotein (P-gp) Substrates (e.g., digoxin):** Ticagrelor is an inhibitor of P-gp; coadministration may increase plasma concentrations of P-gp substrates.
* **Aspirin:** Long-term coadministration with aspirin >100 mg daily increases bleeding risk and may reduce ticagrelor efficacy.
* **Strong CYP3A4 Inhibitors:** Contraindicated due to increased ticagrelor exposure.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for signs and symptoms of dyspnea.
* Periodically monitor serum creatinine, uric acid, and liver enzymes.
## Clinical Pearls
* Ticagrelor has a faster onset and offset of action compared to clopidogrel.
* Discontinuation of ticagrelor increases the risk of thrombotic events.
* Maintenance dose of aspirin should be limited to 100 mg daily to balance efficacy and bleeding risk.
* When switching from another P2Y$_{12}$ inhibitor, start ticagrelor as soon as the previous drug is discontinued.
* Patients experiencing dyspnea should be thoroughly evaluated for underlying causes, and ticagrelor should be continued if the benefits outweigh the risks.
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**Disclaimer:** This information is intended for healthcare professionals. Prescribing decisions should always be based on current, approved prescribing information, patient-specific factors, and institutional protocols. Always verify current guidelines and drug information from authoritative sources.
