Please check your internet connection and try again.
# Ticagrelor (Brilinta)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y$_{12}$ platelet inhibitor.
## Primary Indications
* Reduction of thrombotic cardiovascular events (e.g., myocardial infarction, stroke) in patients with acute coronary syndrome (ACS) or a history of myocardial infarction.
* In combination with aspirin for the prevention of further arterial thromboembolic events in patients with ACS or with a history of myocardial infarction and at least one risk factor for occlusive vascular disease.
## Adult Dosing
* **ACS:** 180 mg orally once, then 90 mg orally twice daily. Loading dose is crucial.
* **Post-MI with risk factors:** 60 mg orally twice daily.
## Pediatric Dosing
The safety and efficacy of ticagrelor in pediatric patients have not been established.
## Dose Adjustments
No dose adjustments are typically required based on age, sex, or renal/hepatic impairment, although caution is advised in severe hepatic impairment.
## Contraindications
* Active pathological bleeding.
* History of intracerebral hemorrhage.
* Hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Most Common:** Bleeding (including fatal and life-threatening), dyspnea, ventricular pauses, bradycardia.
* **Serious:** Major bleeding, non-major clinically relevant bleeding, hypersensitivity reactions.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with potent CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase ticagrelor exposure.
* **CYP3A4 Inducers:** Potent CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease ticagrelor exposure.
* **Aspirin:** Can be used concomitantly. Long-term maintenance doses of aspirin greater than 100 mg may reduce the efficacy of ticagrelor.
* **Other Antithrombotics:** Increased risk of bleeding.
* **DPP-4 Inhibitors:** Ticagrelor can increase serum uric acid levels, potentially leading to gout. Caution with DPP-4 inhibitors which can also increase uric acid.
## Monitoring
* **Bleeding:** Assess for signs and symptoms of bleeding regularly.
* **Dyspnea:** Monitor for new or worsening dyspnea.
* **Electrolytes:** Monitor serum potassium levels, particularly in patients with risk factors for hyperkalemia.
* **Uric Acid:** Monitor serum uric acid levels.
## Clinical Pearls
* A loading dose of 180 mg is recommended for ACS patients.
* Ticagrelor is dosed twice daily, except for the 60 mg maintenance dose which is also twice daily.
* Discontinue if active pathological bleeding occurs.
* Consider stopping ticagrelor 5-7 days before elective surgery if clinically appropriate, but weigh the risk of thrombotic events.
* Avoid concomitant use with strong CYP3A4 inhibitors.
---
*Disclaimer: This information is intended for healthcare professionals. Always consult the most current prescribing information and relevant guidelines before making clinical decisions.*
