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# Ticagrelor
## Overview
Ticagrelor is an oral, direct-acting, reversibly binding P2Y12 platelet inhibitor.
## Primary Indications
* Inhibition of platelet aggregation to reduce the rate of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI).
* Inhibition of platelet aggregation in patients with acute coronary syndrome (ACS).
## Adult Dosing
* **Following ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months.
* **Following MI (at least 1 year after ACS):**
* **Maintenance Dose:** 60 mg orally twice daily. Duration of therapy should be individualized.
## Pediatric Dosing
The use of ticagrelor in pediatric patients has not been established.
## Dose Adjustments
No dose adjustments are required for patients with mild to severe renal impairment or mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack or stroke.
* Known hypersensitivity to ticagrelor or any of its components.
* Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir).
## Adverse Effects
* **Major Bleeding:** Including fatal and intracranial bleeding.
* **Dyspnea:** Often transient.
* **Ventricular pauses:** Usually asymptomatic.
* **Bradycardia.**
* **Hypersensitivity reactions.**
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid concomitant use with strong CYP3A4 inhibitors. Consider potential for increased exposure to statins (e.g., simvastatin, atorvastatin) and other CYP3A4 substrates.
* **CYP3A4 Inducers:** May decrease ticagrelor exposure and efficacy.
* **Other Antiplatelet Agents/Anticoagulants:** Increased risk of bleeding.
* **Aspirin:** While often co-administered, higher doses of aspirin (>100 mg) may reduce the efficacy of ticagrelor.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea and bradycardia.
* Assess for drug interactions, particularly with CYP3A4 inhibitors/inducers and other antithrombotic agents.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor that is not a thienopyridine and does not require metabolic activation.
* Its reversibility of binding may allow for faster platelet function recovery compared to clopidogrel.
* If a dose is missed, the patient should take the next dose at the regularly scheduled time. Do not double the dose.
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*This information is intended for healthcare professionals. Please refer to the most current prescribing information for complete details.*
