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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an oral, direct-acting, reversibly binding P2Y12 platelet inhibitor. It prevents adenosine triphosphate from binding to its platelet receptor and blocks platelet activation and aggregation.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS), including patients who are managed medically, with percutaneous coronary intervention (PCI), or with coronary artery bypass grafting (CABG).
* Reduction of new thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) and at least one additional risk factor for cardiovascular events.
## Adult Dosing
* **ACS:** 180 mg loading dose once, followed by 90 mg twice daily.
* **History of MI (≥ 1 year ago) with risk factors:** 60 mg twice daily.
* **Duration of therapy:** Generally recommended for at least 12 months in ACS, unless contraindications arise. For patients with a history of MI, continue as long as benefits outweigh risks.
## Pediatric Dosing
Dosing for pediatric patients has not been established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to limited data.
* **Renal Impairment:** No dose adjustment necessary in mild, moderate, or severe renal impairment.
## Contraindications
* Active serious bleeding (e.g., intracranial hemorrhage, gastrointestinal 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, itraconazole, voriconazole, clarithromycin) for the 180 mg dose regimen.
## Adverse Effects
* **Most Common:** Bleeding (major and minor), dyspnea, bradycardia, rash, diarrhea.
* **Serious:** Life-threatening bleeding, ventricular pauses, increased serum creatinine.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid concomitant use of strong CYP3A4 inhibitors with the 180 mg dose regimen. Caution with other CYP3A4 substrates (e.g., statins, calcium channel blockers) due to potential for increased exposure.
* **P-glycoprotein (P-gp) Substrates:** Ticagrelor is a P-gp inhibitor. Use with caution with P-gp substrates (e.g., digoxin) due to potential for increased concentrations.
* **Antiplatelets/Anticoagulants:** Increased risk of bleeding. Consider risks and benefits of coadministration.
* **Aspirin:** While often used concomitantly, higher doses of aspirin (e.g., maintenance doses >100 mg) may reduce the efficacy of ticagrelor.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Renal Function:** Monitor serum creatinine.
* **Electrolytes:** Monitor for hyperkalemia, especially in patients with risk factors.
* **Heart Rate:** Monitor for symptomatic bradycardia.
## Clinical Pearls
* Ticagrelor should be initiated as soon as possible in patients with ACS.
* A loading dose of aspirin (300-325 mg) is recommended at the time of percutaneous coronary intervention unless contraindicated.
* Patients should be advised to swallow the tablet whole. If the tablet is broken or crushed, they should consume all particles immediately.
* Discontinuation of ticagrelor may increase the risk of thrombotic events. Only discontinue if absolutely necessary or if there is a contraindication.
* Dyspnea is a common side effect and may not be related to underlying cardiac or pulmonary disease.
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*Disclaimer: This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and guidelines, and exercise your professional judgment.*
