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# Ticagrelor
## Overview
Ticagrelor is an orally active, direct-acting P2Y12 receptor antagonist 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):** To reduce the rate of thrombotic cardiovascular events (including myocardial infarction and stroke) in patients with ACS.
* **History of Myocardial Infarction (MI):** To reduce the rate of thrombotic cardiovascular events in patients with a history of MI who are at high risk for an atherothrombotic event.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for up to 12 months.
* **For patients transitioning from clopidogrel:** Dosing depends on the reason for transition and local protocol.
* **History of MI:**
* **Maintenance Dose:** 60 mg orally twice daily.
* **Duration:** For patients who have had an MI more than 1 year ago and are treated with ticagrelor 60 mg twice daily, continue for an additional 12 months, for a total of up to 36 months of dual antiplatelet therapy (DAPT).
## Pediatric Dosing
No established pediatric dosing.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment necessary in mild to severe renal impairment.
* **Hepatic Impairment:** Use with caution in patients with severe hepatic impairment. No dose adjustment necessary in mild to moderate hepatic impairment.
## Contraindications
* Active pathological bleeding.
* History of intracerebral hemorrhage.
* Hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Common:** Dyspnea, bradycardia, non-fatal MI, accidental injury.
* **Serious:** Bleeding (major, minor), ventricular pauses.
* **Other:** Cough, diarrhea, headache, hypercholesterolemia, rash.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor exposure. Co-administration with strong CYP3A4 inducers (e.g., rifampin, phenytoin) can decrease ticagrelor exposure.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Avoid co-administration with other potent antiplatelet agents or anticoagulants unless clinically indicated and if so, monitor closely for bleeding.
* **Digoxin:** Ticagrelor can increase digoxin concentrations. Monitor digoxin levels and adjust dose as needed.
* **Statins:** Increased risk of simvastatin/atorvastatin-related myopathy. Limit simvastatin and atorvastatin doses.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding, especially during the initial months of therapy.
* **Bradycardia:** Monitor heart rate; symptomatic bradycardia may require dose adjustment or discontinuation.
* **Lipid Profile:** Periodic monitoring of lipid levels may be beneficial.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel.
* Dyspnea is a common side effect, and patients should be reassured. If severe, consider underlying causes.
* The 90 mg twice daily dose is indicated for ACS patients. The 60 mg twice daily dose is for patients with a history of MI treated beyond 1 year.
* Ticagrelor can be taken with or without food.
* Discontinue ticagrelor at least 5 days prior to elective surgery if possible, unless the patient is at high risk for stent thrombosis.
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**Disclaimer:** This information is intended for healthcare professionals and does not replace a thorough review of the most current prescribing information, clinical guidelines, or patient-specific assessment. Always verify current drug information and dosages with official sources and consider local protocols.
