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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an oral, direct-acting P2Y12 receptor antagonist used to reduce thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** For the prevention of thrombotic events in patients with ACS (unstable angina, non-ST-elevation myocardial infarction [NSTEMI], or ST-elevation myocardial infarction [STEMI]) undergoing percutaneous coronary intervention (PCI) or medical management.
* **History of Myocardial Infarction (MI):** In patients with a history of MI (at least 6 months ago) and at least one other risk factor for occlusive vascular disease, to reduce the rate of cardiovascular death, MI, and stroke.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for up to 12 months. In certain situations (e.g., lower risk of stent thrombosis), a maintenance dose of 60 mg twice daily may be considered after the initial 12-month treatment period, especially in patients who have had an MI within the last year or have other risk factors for atherothrombotic events.
* **History of MI (≥ 6 months ago) with risk factors:** 60 mg orally twice daily.
## Pediatric Dosing
Ticagrelor is not recommended for use in pediatric patients. Safety and efficacy have not been established.
## Dose Adjustments
No dose adjustments are required for hepatic or renal impairment.
## Contraindications
* Active pathological bleeding (e.g., intracranial hemorrhage, gastrointestinal bleeding).
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
**Common:** Bleeding (especially gastrointestinal and ecchymosis), dyspnea, bradycardia, elevated serum creatinine, hyperuricemia.
**Serious:** Major bleeding events, ventricular pauses, reversible posterior leukoencephalopathy syndrome (RPLS).
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor exposure. Strong inducers (e.g., rifampin, carbamazepine) may decrease ticagrelor exposure. Concomitant use with strong CYP3A4 inhibitors should be avoided, especially in ACS patients.
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with CYP3A4 substrates (e.g., simvastatin, atorvastatin) may increase exposure to these drugs.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Renal Function:** Assess serum creatinine.
* **Bradycardia:** Monitor heart rate, especially if taking concomitant medications that cause bradycardia.
## Clinical Pearls
* Ticagrelor is a direct-acting P2Y12 inhibitor and does not require activation by the liver.
* Discontinue ticagrelor 5 days before elective surgery.
* The dyspnea experienced by some patients is generally mild and does not necessitate discontinuation.
* Avoid concomitant use of ticagrelor with St. John's wort or grapefruit juice.
* If a patient misses a dose, they should take the next dose at its scheduled time. They should not double the dose.
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*Disclaimer: This information is intended for healthcare professionals. Prescribing decisions should always be based on the most current prescribing information, institutional protocols, and individual patient factors. Please verify the information with the official product labeling and other reliable sources.*
