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## Ticagrelor (Brilinta)
### Overview
Ticagrelor is an oral, direct-acting, reversible P2Y12 platelet inhibitor. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
### Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, to prevent thrombotic events.
* **Myocardial Infarction (MI) (History):** In patients with a history of MI (at least 12 months prior) and at high risk for an atherothrombotic event, in combination with aspirin, to reduce the rate of thrombotic cardiovascular events.
### Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months, followed by 60 mg orally twice daily.
* **History of MI:**
* **Maintenance Dose:** 60 mg orally twice daily.
### Pediatric Dosing
Dosing in pediatric patients is not established.
### Dose Adjustments
* **Renal Impairment:** No dose adjustment is recommended in patients with mild, moderate, or severe renal impairment.
* **Hepatic Impairment:** No dose adjustment is recommended in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
### Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Hypersensitivity to ticagrelor or any of its components.
### Adverse Effects
* **Most Common:** Dyspnea, bradycardia, accidental injury, rash, diarrhea.
* **Serious:** Bleeding (major, minor, clinically significant non-CABG major bleeding, CABG-related major bleeding), ventricular pauses, angioedema.
* **Other:** Hyperuricemia, creatinine increase.
### Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) and strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin).
* **CYP3A4 Substrates (e.g., simvastatin, atorvastatin):** Ticagrelor can increase plasma concentrations of CYP3A4 substrates. Consider lower doses of these agents.
* **Aspirin:** Concomitant use with aspirin (beyond the initial loading dose in ACS) can increase the risk of bleeding.
* **Other Antithrombotics:** Concomitant use with other antiplatelet agents or anticoagulants may increase the risk of bleeding.
### Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding.
* **Renal Function:** Monitor periodically, especially in patients with pre-existing renal impairment.
* **Uric Acid:** Monitor periodically as hyperuricemia can occur.
### Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel.
* Dyspnea is a common side effect, often transient and not indicative of underlying cardiac dysfunction.
* Ticagrelor should be continued for at least 12 months in ACS patients, even if transitioned to a lower maintenance dose.
* The 60 mg dose is indicated for patients with a history of MI at least 12 months prior.
* For patients unable to swallow the tablet whole, it can be crushed and mixed in water or orange juice.
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*Disclaimer: This information is intended for healthcare professionals. Always consult the most current prescribing information and relevant clinical guidelines for complete details and to verify dosages and recommendations.*
