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# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, for the prevention of thrombotic events in patients with ACS (unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction).
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months, or as long as the patient is at risk for a thrombotic event. Some patients may benefit from continued therapy beyond 12 months.
* **Note:** Dosing beyond 12 months for ACS should be individualized based on risk of stent thrombosis versus bleeding.
## Pediatric Dosing
Dosing has not been established in pediatric patients.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is needed for mild to severe renal impairment.
* **Hepatic Impairment:** No dose adjustment is needed for mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to lack of data.
## Contraindications
* Active bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its components.
## Adverse Effects
* **Common:** Dyspnea, bradycardia, increased creatinine, hyperkalemia, diarrhea, rash.
* **Serious:** Bleeding (major or minor), ventricular pauses.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor concentrations. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease ticagrelor concentrations.
* **Strong CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with drugs that are substrates of CYP3A4 (e.g., simvastatin, lovastatin) may increase their concentrations. Limit doses of these substrates.
* **Aspirin:** When used in ACS, aspirin is given concurrently.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* **Clinical signs of bleeding:** Monitor for any signs of bleeding (e.g., hematuria, melena, epistaxis).
* **Renal function and electrolytes:** Especially in patients with pre-existing renal impairment or those at risk for hyperkalemia.
* **Heart rate:** For symptomatic bradycardia.
## Clinical Pearls
* Ticagrelor is administered twice daily, unlike clopidogrel and prasugrel.
* The most common side effect is dyspnea, which is usually mild and transient and does not require discontinuation.
* Dosing of concomitant statins should be limited to 40 mg daily or less for simvastatin and 10 mg daily or less for atorvastatin.
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*This information is intended for healthcare professionals and does not replace the need to consult the official prescribing information or local protocols.*
