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# Ticagrelor
## Overview
Ticagrelor is an oral, direct-acting, reversibly binding P2Y12 receptor antagonist. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** Prevention of thrombotic cardiovascular events (including stent thrombosis) in patients with ACS managed with percutaneous coronary intervention (PCI) or medically managed.
## Adult Dosing
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* For patients with a history of myocardial infarction (MI) more than 1 year prior to starting ticagrelor, the dose may be reduced to 60 mg orally twice daily.
* **Duration of Therapy:** Typically for at least 12 months. Duration beyond 12 months should be individualized based on patient risk factors and local protocols.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* No dose adjustment is required for patients with mild to moderate hepatic impairment.
* Caution is advised in severe hepatic impairment.
* No dose adjustment is required for patients with mild to moderate renal impairment.
* Caution is advised in severe renal impairment or end-stage renal disease.
## Contraindications
* Hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
* History of transient ischemic attack (TIA) or stroke while on ticagrelor therapy (when used for ACS).
## Adverse Effects
* **Most Common:** Bleeding (including fatal and life-threatening), dyspnea, bradycardia, atrial fibrillation, syncope, dizziness.
* **Serious:** Major bleeding, ventricular pauses.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin) can increase ticagrelor exposure and should be used with caution. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) can decrease ticagrelor exposure.
* **UGT1A1/UGT2B7 Substrates:** Ticagrelor is a substrate for UGT1A1 and UGT2B7. Concomitant use with drugs that inhibit UGT1A1 or UGT2B7 may increase ticagrelor exposure.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea.
* Monitor heart rate.
## Clinical Pearls
* Ticagrelor should be administered as part of a regimen including aspirin and other appropriate therapies for ACS.
* If a dose is missed, the patient should take the next dose at the regularly scheduled time. Do not double the dose.
* Discontinuation of ticagrelor should be avoided unless clinically indicated due to an increased risk of thrombotic events.
* Ticagrelor is a reversible P2Y12 inhibitor, which may be beneficial in situations where platelet function needs to be rapidly restored.
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*This information is intended for healthcare professionals and does not replace the need to consult the official prescribing information and current clinical guidelines. Always verify current drug information with the manufacturer's package insert or other reliable sources.*
