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# Ticagrelor
## Overview
Ticagrelor is an orally administered, direct-acting, reversible P2Y12 receptor antagonist. It is 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
* Acute Coronary Syndrome (ACS): In combination with aspirin, for the reduction of thrombotic cardiovascular events.
* Patients with a history of MI: For the prevention of further thrombotic cardiovascular events.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* **History of MI (at least 1 year after ACS or MI):**
* **Maintenance Dose:** 60 mg orally twice daily.
* **Duration of Therapy:** Generally recommended for at least 12 months in ACS patients. For patients with a history of MI, 60 mg twice daily can be continued long-term if there is no increased risk of bleeding.
## Pediatric Dosing
No established pediatric dosing. Ticagrelor is not recommended for use in pediatric patients.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary in mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment necessary in mild to severe renal impairment.
## Contraindications
* Hypersensitivity to ticagrelor or any excipient.
* Active pathological bleeding.
## Adverse Effects
* **Common:** Bleeding (including life-threatening and fatal bleeding, especially with concomitant aspirin use), dyspnea, contusion.
* **Serious:** Major bleeding, ventricular pauses, increased serum creatinine, increased uric acid.
## Key Drug Interactions
* **Strong CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole, clarithromycin):** May increase ticagrelor plasma concentrations. Coadministration is generally not recommended.
* **Strong CYP3A4 Inducers (e.g., rifampin, phenytoin, carbamazepine):** May decrease ticagrelor plasma concentrations.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and monitor closely.
* **Aspirin:** Coadministration is standard for ACS but increases bleeding risk. Maintain aspirin dose at 75-100 mg daily for patients on ticagrelor 90 mg twice daily. For patients on ticagrelor 60 mg twice daily after MI, low-dose aspirin is typically continued, but the optimal dose is not definitively established.
* **CYP3A4 Substrates:** Ticagrelor is a moderate CYP3A4 inhibitor and may increase concentrations of CYP3A4 substrates (e.g., simvastatin, atorvastatin).
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding, especially during the first few months of therapy.
* **Renal Function:** Monitor serum creatinine periodically.
* **Uric Acid:** Monitor uric acid levels periodically.
* **Ventricular Pauses:** ECG monitoring may be considered, especially in patients with risk factors for bradycardia.
## Clinical Pearls
* Ticagrelor has a faster onset and offset of action compared to clopidogrel, which may be advantageous in situations requiring urgent intervention or if surgery is anticipated.
* Patients should be advised to inform all healthcare providers they are taking ticagrelor before any surgery or dental procedure.
* Discontinuation of ticagrelor may increase the risk of stent thrombosis, MI, and death. If ticagrelor must be discontinued, resuming after a brief interruption is preferred over permanent discontinuation, especially within the first year post-ACS.
* Dose of aspirin when used with ticagrelor 60 mg twice daily is not definitively established but typically low-dose aspirin is continued.
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*This information is intended for healthcare professionals. Always consult the official prescribing information and current clinical guidelines for the most up-to-date and comprehensive drug information.*
