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# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor. It prevents adenosine triphosphate from binding to platelet receptors, thereby inhibiting platelet activation and aggregation.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
* Reduction of thrombotic cardiovascular events in patients with ACS undergoing percutaneous coronary intervention (PCI).
## Adult Dosing
* **ACS:** 180 mg orally once, followed by 90 mg orally twice daily. Treatment duration is typically 12 months.
* **ACS with PCI:** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily. Treatment duration is typically 12 months.
* **Maintenance therapy after ACS/MI (secondary prevention):** 90 mg orally twice daily. Duration depends on individual risk assessment and local guidelines. In certain populations (e.g., patients with prior MI), ticagrelor 60 mg twice daily may be considered after at least 1 year of 90 mg twice daily, based on risk assessment.
## Pediatric Dosing
No established pediatric dosing for ticagrelor.
## Dose Adjustments
* **Hepatic Impairment:** Caution advised in patients with moderate to severe hepatic impairment. No dose adjustment is recommended in mild hepatic impairment.
* **Renal Impairment:** No dose adjustment is recommended in patients with mild to severe renal impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Hypersensitivity to ticagrelor or any of its excipients.
* Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) is generally not recommended, except for specific indications like strong CYP3A4 inhibitors used as part of HIV therapy.
## Adverse Effects
* **Common:** Dyspnea, bleeding (major, minor, procedural), bruising, hypercholesterolemia.
* **Serious:** Major bleeding, intracranial hemorrhage, ventricular pauses.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid concomitant use with potent CYP3A4 substrates where therapeutic effect is dependent on plasma concentration (e.g., simvastatin, lovastatin).
* **CYP3A4 Inhibitors/Inducers:** Concurrent use with strong CYP3A4 inhibitors increases ticagrelor exposure; use with caution. Strong CYP3A4 inducers may decrease ticagrelor exposure.
* **Aspirin:** Concurrent use with aspirin is recommended for ACS, but increases bleeding risk.
* **Other Antiplatelets/Anticoagulants:** Concomitant use increases bleeding risk.
* **Digoxin:** Ticagrelor can increase digoxin concentrations. Monitor digoxin levels.
## Monitoring
* **Bleeding:** Closely monitor for signs and symptoms of bleeding.
* **Lipid Panel:** Baseline and periodic monitoring of lipid levels.
* **ECG:** Monitor for ventricular pauses, especially in patients with relevant risk factors.
## Clinical Pearls
* Ticagrelor should be initiated as soon as possible in patients with ACS, regardless of whether they are managed medically or with PCI.
* A loading dose is required for initiation in ACS.
* Ticagrelor is a twice-daily medication. Patient adherence is crucial.
* Consider discontinuation of ticagrelor in patients with a history of TIA or stroke due to increased risk of intracranial hemorrhage.
* Dyspnea is a common side effect, but usually mild and does not necessitate discontinuation unless severe.
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*Disclaimer: This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and local institutional guidelines before making any treatment decisions.*
