Please check your internet connection and try again.
# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an oral P2Y12 platelet inhibitor 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
* Prevention of thrombotic cardiovascular events in patients with ACS (unstable angina, NSTEMI, STEMI).
* Prevention of thrombotic cardiovascular events in patients with a history of MI (at least one year ago) and at least one risk factor for occlusive vascular disease.
## Adult Dosing
* **ACS:**
* Loading dose: 180 mg orally once.
* Maintenance dose: 90 mg orally twice daily for up to 12 months. In certain cases, the maintenance dose may be reduced to 60 mg twice daily after 12 months of treatment, particularly in patients with a history of MI who are at higher risk of bleeding.
* **History of MI (at least 1 year ago):**
* Maintenance dose: 60 mg orally twice daily. This indication is for patients who have had an MI at least one year prior and have at least one additional risk factor for occlusive vascular disease.
## Pediatric Dosing
No established pediatric dosing recommendations. Ticagrelor is not typically used in pediatric populations.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is recommended in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to lack of specific data.
* **Renal Impairment:** No dose adjustment is recommended for mild, moderate, or severe renal impairment.
## Contraindications
* Known hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding.
* History of intracerebral hemorrhage.
## Adverse Effects
* **Most Common:** Bleeding (including fatal and life-threatening), dyspnea, bradyarrhythmia.
* **Serious:** Significant bleeding events, ventricular pauses.
## 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, carbamazepine) can decrease ticagrelor exposure.
* **CYP3A4 Substrates:** Ticagrelor can inhibit CYP3A4, increasing the exposure of co-administered CYP3A4 substrates (e.g., simvastatin, atorvastatin).
* **UGT Inhibitors/Inducers:** Ticagrelor is a substrate of UGT1A9.
* **Other Antithrombotics:** Concomitant use with other antithrombotic agents (e.g., anticoagulants, other antiplatelets, NSAIDs) increases the risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding (e.g., bruising, hematuria, melena, epistaxis).
* Monitor for dyspnea.
* Monitor for bradycardia.
* Evaluate risk/benefit for continued therapy in patients experiencing significant bleeding or persistent dyspnea.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel.
* The 90 mg twice-daily dose is typically used for ACS and should be continued for 12 months unless contraindicated. A lower 60 mg twice-daily dose may be considered after 12 months for patients with a history of MI at higher bleeding risk.
* The 60 mg twice-daily dose is indicated for patients with a history of MI at least one year ago who have at least one additional risk factor.
* Discontinuation of ticagrelor, especially within the first year of ACS treatment, increases the risk of stent thrombosis, MI, and death.
* Aspiring is recommended as maintenance therapy in combination with ticagrelor, but the optimal dose of aspirin is debated and generally the lowest effective dose (e.g., 75-100 mg daily) should be used.
***
**Disclaimer:** This information is intended for healthcare professionals. Always consult the current prescribing information and relevant clinical guidelines for complete and up-to-date guidance before making any treatment decisions.
