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# Ticagrelor
## Overview
Ticagrelor is a 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):** To reduce the rate of thrombotic cardiovascular events in patients with ACS.
* **Post-Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor reduces 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 at least 12 months. Some patients may benefit from continued therapy beyond 12 months.
* **Post-MI (with history of MI):**
* **Maintenance Dose:** 60 mg orally twice daily.
## Pediatric Dosing
There is no established pediatric dosing for ticagrelor.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary for mild to moderate hepatic impairment. Caution in severe hepatic impairment as data is limited.
* **Renal Impairment:** No dose adjustment necessary for mild to moderate renal impairment. Caution in severe renal impairment (eGFR <30 mL/min/1.73m²) as data is limited.
* **Age and Weight:** In patients with ACS and a body weight <40 kg, consider a loading dose of 135 mg (2.25 mg/kg) and a maintenance dose of 45 mg twice daily.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Common:** Dyspnea, bleeding (including fatal and life-threatening), bradycardia, ventricular pauses.
* **Serious:** Major bleeding, intracranial bleeding, severe allergic reactions.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor exposure. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin) may decrease ticagrelor exposure.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and consider risk-benefit.
* **Statins:** Ticagrelor can increase simvastatin and atorvastatin concentrations. Limit simvastatin to 40 mg daily and atorvastatin to 80 mg daily.
* **Proton Pump Inhibitors (PPIs):** May reduce ticagrelor efficacy. If co-administration is necessary, consider timing of doses or alternative therapy.
* **Opioids:** May reduce the absorption and efficacy of ticagrelor.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding, especially in patients with risk factors.
* **Heart Rate:** Ticagrelor can cause bradycardia. Assess for symptoms of bradycardia.
* **Renal and Hepatic Function:** Monitor periodically, especially in patients with severe impairment.
## Clinical Pearls
* Ticagrelor should be initiated as soon as possible after the onset of ACS or following an MI.
* Discontinuation of ticagrelor prematurely increases the risk of stent thrombosis, MI, and death.
* If possible, stop ticagrelor at least 5 days before elective surgery.
* Aspirin is recommended as part of dual antiplatelet therapy (DAPT) with ticagrelor. The optimal dose of aspirin is not well-defined; lower doses (e.g., 75-100 mg daily) are generally preferred.
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*This information is intended for clinical use and does not replace comprehensive prescribing information. Always consult the official product monograph and current guidelines for complete details before making clinical decisions.*
