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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally administered, direct-acting, reversible P2Y12 platelet inhibitor. It is used to reduce the rate of thrombotic cardiovascular events.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In patients with a history of myocardial infarction (MI) or ACS, ticagrelor is indicated to reduce the rate of cardiovascular death, MI, and stroke. It is typically used in combination with aspirin.
* **Secondary Prevention in MI:** For patients with a history of MI, ticagrelor may be used to reduce the rate of thrombotic cardiovascular events.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months. In certain patients, after 12 months of therapy, a maintenance dose of 60 mg twice daily may be considered.
* **Secondary Prevention in MI (if not treated for ACS):**
* **Maintenance Dose:** 60 mg orally twice daily. This indication is for patients with a history of MI at least one year prior and who are treated with aspirin.
## Pediatric Dosing
Dosing for pediatric patients is not established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is needed. However, caution is advised due to lack of specific studies in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment is needed.
## Contraindications
* Active pathological bleeding (e.g., peptic ulcer or intracranial hemorrhage).
* History of transient ischemic attack (TIA) or stroke. (Specific guidance for ticagrelor 60 mg dosing in patients with prior stroke/TIA exists and should be reviewed).
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Bleeding:** This is the most common and significant adverse effect. Includes fatal bleeding, intracranial bleeding, and gastrointestinal bleeding.
* **Dyspnea:** Shortness of breath is common and usually mild and transient.
* **Bradycardia:** Transient and asymptomatic.
* **Ventricular pauses:** May occur.
* **Hyperuricemia:** Can lead to gout.
* **Cutaneous hypersensitivity reactions.**
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong inhibitors (e.g., ketoconazole, ritonavir) may increase ticagrelor exposure and risk of bleeding. Strong inducers (e.g., rifampin, phenytoin) may decrease ticagrelor exposure.
* **Aspirin:** Concurrent use with aspirin is recommended for ACS and some secondary prevention indications. High-dose aspirin may decrease the efficacy of ticagrelor.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and consider dose adjustments or interruptions of other agents.
* **Statins:** Ticagrelor can increase the exposure of some statins metabolized by CYP3A4 (e.g., simvastatin, atorvastatin).
* **Digoxin:** Ticagrelor can increase digoxin levels. Monitor digoxin levels and clinical signs of toxicity.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding (e.g., hematuria, melena, bruising, epistaxis).
* **Renal and Hepatic Function:** Baseline and periodic monitoring.
* **Uric Acid:** Periodic monitoring.
* **Digoxin Levels:** If used concurrently.
## Clinical Pearls
* Ticagrelor is dosed twice daily, regardless of indication.
* Discontinuation of ticagrelor prematurely increases the risk of stent thrombosis, MI, and death.
* The decision to use ticagrelor 60 mg twice daily beyond 12 months for ACS or for secondary prevention in patients with a history of MI should be individualized based on patient risk factors for ischemic events versus bleeding.
* Patients experiencing dyspnea should not typically have ticagrelor discontinued unless other causes are ruled out and symptoms are severe or persistent.
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*This information is intended for clinical use and does not substitute for professional medical judgment. Always consult the most current prescribing information and relevant clinical guidelines before making treatment decisions.*
