Please check your internet connection and try again.
# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with acute coronary syndrome (ACS).
* In combination with aspirin, for the prevention of atherothrombotic events in patients with ACS.
## Adult Dosing
* **Acute Coronary Syndrome (ACS):**
* Loading Dose: 180 mg orally once.
* Maintenance Dose: 90 mg orally twice daily for up to 12 months.
* **History of Myocardial Infarction (MI):**
* 90 mg orally twice daily.
* May be considered for longer than 12 months in select patients based on risk assessment, and for patients not at high risk of bleeding.
* **Patients < 40 kg:**
* Dosing in patients < 40 kg has not been well established and should be guided by clinical judgment and local protocols.
## Pediatric Dosing
Ticagrelor is **not recommended** for use in pediatric patients.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment necessary for mild to severe renal impairment.
* **Hepatic Impairment:** No dose adjustment necessary for mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
## Contraindications
* Known hypersensitivity to ticagrelor or any component of the formulation.
* Active pathological bleeding.
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (major and minor, including fatal hemorrhage), bradycardia, ventricular pauses.
* **Serious:** Severe bleeding, anaphylaxis, angioedema, CNS hemorrhage.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor levels; strong inducers (e.g., rifampin, carbamazepine) may decrease levels. Avoid coadministration with strong CYP3A4 inhibitors where possible.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Concurrent use requires careful monitoring.
* **Statins:** Ticagrelor can increase rosuvastatin and simvastatin concentrations. Consider dose adjustments of these statins.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea.
* Monitor heart rate, particularly in patients with risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor, not a thienopyridine, and does not require metabolic activation.
* The onset of action is rapid.
* Discontinuation of ticagrelor increases the risk of stent thrombosis, MI, and death.
* Aspirin dose greater than 100 mg/day may reduce the efficacy of ticagrelor.
* Ticagrelor has a higher incidence of dyspnea compared to clopidogrel, which is generally transient and not associated with significant pulmonary impairment.
***
*Disclaimer: This information is intended for clinical use and does not replace professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines before making any treatment decisions.*
