Please check your internet connection and try again.
# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 receptor antagonist used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
## Primary Indications
* Treatment of patients with acute coronary syndrome (ACS).
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months, or until advised otherwise by the prescribing physician.
* **Note:** If a loading dose of aspirin is given with ticagrelor, it should be 300 mg to 325 mg. However, routine long-term use of aspirin beyond the initial post-ACS treatment period is not recommended.
## Pediatric Dosing
* Dosing for pediatric patients has not been established.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is recommended.
* **Hepatic Impairment:** No dose adjustment is recommended. However, ticagrelor has not been studied in patients with severe hepatic impairment.
## Contraindications
* Active bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Major Bleeding:** Most common serious adverse effect.
* **Dyspnea:** Common, often transient.
* **Bradyarrhythmias:** Common.
* **Hyperuricemia:** Can occur.
* **Increased serum creatinine:** Can occur.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor exposure. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure.
* **P-glycoprotein (P-gp) Substrates:** Ticagrelor inhibits P-gp. Concomitant use with P-gp substrates that have a narrow therapeutic index (e.g., digoxin) may increase exposure to these substrates.
* **Aspirin:** Concomitant use of ticagrelor with aspirin is recommended for patients with ACS, but routine long-term use of aspirin beyond initial treatment is not recommended. Increased risk of bleeding.
* **Other Antithrombotic Agents:** Concomitant use with other antithrombotic agents (e.g., anticoagulants, other antiplatelets) increases the risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding (e.g., hematuria, melena, ecchymosis, epistaxis).
* Monitor for dyspnea and bradycardia.
* Consider monitoring uric acid levels, especially in patients with a history of gout.
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor with a faster onset and offset of action compared to clopidogrel.
* It is dosed twice daily, which is important for patient adherence.
* The risk of bleeding is increased, particularly when used with aspirin or other antithrombotic agents.
* Patients may experience dyspnea, which is usually not a contraindication to continuing therapy but warrants evaluation.
* In patients undergoing PCI, the decision to continue ticagrelor beyond 12 months should be individualized based on the patient's risk for stent thrombosis versus bleeding.
***
*This information is intended for healthcare professionals. Please consult the full prescribing information and relevant guidelines for complete details and to ensure the most up-to-date recommendations.*
