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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally active, direct-acting P2Y$_{12}$ platelet inhibitor. It is reversible and not a prodrug.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** For the reduction of thrombotic cardiovascular events (including myocardial infarction and stroke) in patients with ACS.
* **Myocardial Infarction (MI) with ST-segment Elevation (STEMI):** In patients treated with fibrinolytic therapy, or with initial medical management, ticagrelor is indicated for the reduction of thrombotic cardiovascular events in patients with STEMI.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily for at least 12 months, or until completion of a planned drug-eluting stent (DES) retreatment or coronary artery bypass grafting (CABG).
* **After completion of 12 months of treatment:** Consider continuing 90 mg orally twice daily if the patient remains at high risk for a thrombotic cardiovascular event and is not at high risk for bleeding.
* **If previously treated with a P2Y$_{12}$ inhibitor:** If the patient is switching from another P2Y$_{12}$ inhibitor, administer ticagrelor at the time of the next scheduled dose of the previous agent.
* **STEMI:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily. Treatment should be continued for at least 12 months, or until completion of a planned DES retreatment or CABG.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment necessary.
* **Renal Impairment:** No dose adjustment necessary.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Hypersensitivity to ticagrelor or any component of the formulation.
## Adverse Effects
* **Most Common:** Bleeding (major and minor), dyspnea, bradycardia, ventricular pauses.
* **Serious:** Life-threatening bleeding, significant symptomatic bradycardia, permanent disabling stroke.
## Key Drug Interactions
* **Strong CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole, clarithromycin):** Avoid concomitant use as they can increase ticagrelor exposure.
* **Strong CYP3A4 Inducers (e.g., rifampin, phenytoin, carbamazepine):** Avoid concomitant use as they can decrease ticagrelor exposure.
* **CYP3A4 Substrates (e.g., simvastatin, atorvastatin):** Ticagrelor can increase plasma concentrations of these drugs. Use lower doses of statins or consider alternative agents if necessary.
* **Other Antiplatelet Agents or Anticoagulants (e.g., aspirin, clopidogrel, warfarin, heparin, NOACs):** Concomitant use increases the risk of bleeding.
* **Digoxin:** Ticagrelor can increase digoxin levels. Monitor digoxin levels and for signs of toxicity.
## Monitoring
* **Bleeding:** Closely monitor for signs and symptoms of bleeding.
* **Cardiac Rhythm:** Monitor for bradycardia and ventricular pauses, especially in patients with pre-existing risk factors.
* **Renal Function:** Monitor renal function, particularly in patients with pre-existing renal impairment.
## Clinical Pearls
* Ticagrelor should be initiated as a 180 mg loading dose as soon as the diagnosis of ACS is made or in STEMI patients eligible for reperfusion therapy.
* Ticagrelor is not a prodrug and does not require activation by the liver.
* Dyspnea is a common side effect and may require discontinuation if severe or persistent.
* Discontinuation of ticagrelor before completion of therapy can increase the risk of thrombotic events. Premature discontinuation should be avoided unless absolutely necessary (e.g., active bleeding, planned surgery requiring cessation). If temporary discontinuation is needed, consider resuming as soon as possible.
* If CABG surgery is planned, it is generally recommended to stop ticagrelor at least 5 days prior to surgery to reduce bleeding risk.
* Consider a lower maintenance dose of 60 mg twice daily for patients who have completed 12 months of treatment and are continuing for secondary prevention, provided they are not at high risk for thrombotic events or bleeding. (This is an off-label consideration in some regions, and current guidelines and product labeling should be consulted).
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*Disclaimer: This information is intended for clinical use and is based on currently available prescribing information. However, prescribing information may vary by region, and drug formulations and indications can change. Always consult the most current official prescribing information and relevant clinical guidelines before making any treatment decisions.*
