Please check your internet connection and try again.
# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversible P2Y12 receptor antagonist used to inhibit platelet aggregation.
## Primary Indications
* **Acute Coronary Syndromes (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).
* **Myocardial Infarction (MI) with Subsequent Ischemic Stroke or Transient Ischemic Attack (TIA):** To reduce the rate of new thrombotic stroke, MI, cardiovascular death, and all-cause death in patients who have had an MI with a history of stroke or TIA.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* *Note:* For patients with ACS, ticagrelor should be continued for at least 12 months, or longer if clinically indicated. For patients who have not had an ACS event and are treated with percutaneous coronary intervention (PCI), the dose is 60 mg twice daily.
* **History of Stroke or TIA:** 90 mg orally twice daily.
* *Note:* Dosing duration for this indication varies and should be based on individual patient risk factors and clinical judgment.
## Pediatric Dosing
* Dosing in pediatric patients has not been established.
## Dose Adjustments
* **Hepatic Impairment:**
* Severe hepatic impairment: Use with caution.
* Mild to moderate hepatic impairment: No dose adjustment needed.
* **Renal Impairment:** No dose adjustment needed.
## Contraindications
* Active bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its excipients.
* Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin).
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (including fatal bleeding), contusion.
* **Serious:** Bleeding, ventricular pauses, increased serum creatinine, hyperkalemia.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor inhibits CYP3A4. Co-administration with potent CYP3A4 substrates (e.g., simvastatin, atorvastatin, cyclosporine) can increase the concentration of these substrates. Use caution and consider dose reduction of the CYP3A4 substrate.
* **CYP3A4 Inhibitors/Inducers:** Avoid strong CYP3A4 inhibitors. Use caution with moderate inhibitors and inducers.
* **Aspirin:** Concurrent use is indicated in ACS. Prolonged concomitant use may increase bleeding risk.
* **Other Antithrombotics:** Increased risk of bleeding.
* **Digoxin:** Ticagrelor can increase digoxin levels. Monitor digoxin levels and for signs of toxicity.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding (e.g., hematuria, melena, epistaxis, ecchymosis).
* **Renal Function:** Monitor serum creatinine periodically.
* **Electrolytes:** Monitor serum potassium periodically, especially in patients with risk factors for hyperkalemia.
* **Digoxin Levels:** If co-administered with digoxin.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel and prasugrel.
* Dyspnea is a common side effect and may not be indicative of underlying cardiac disease.
* Discontinuation of ticagrelor increases the risk of thrombotic events. If interruption is necessary, consider bridging therapy.
* Ticagrelor should be taken twice daily, with or without food.
***
*This information is intended for clinical decision support and does not replace a thorough review of the current prescribing information and clinical guidelines. Always consult the most up-to-date drug monograph and institutional protocols before making any prescribing decisions.*
