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# Ticagrelor
## Overview
Ticagrelor is an oral, direct-acting, reversible P2Y12 platelet inhibitor. It prevents adenosine diphosphate (ADP) from binding to its platelet receptor P2Y12, thereby inhibiting platelet activation and aggregation.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
* Reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) and at least one additional risk factor for cardiovascular events.
## Adult Dosing
* **ACS:** 180 mg orally once as a loading dose, followed by 90 mg orally twice daily.
* **History of MI (at least one risk factor):** 90 mg orally twice daily.
* Aspirin (ASA) is typically co-administered. The optimal dose of ASA has not been established, but doses up to 100 mg once daily are generally recommended. Higher doses of ASA may reduce the efficacy of ticagrelor and increase bleeding risk.
## Pediatric Dosing
* Dosing for pediatric patients has not been established.
## Dose Adjustments
* No dose adjustment is necessary for patients with hepatic or renal impairment.
## Contraindications
* Active pathological bleeding.
* History of intracranial hemorrhage.
* Known hypersensitivity to ticagrelor or any of its components.
* Concomitant administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, nefazodone).
## Adverse Effects
* **Most Common:** Dyspnea, bradyarrhythmia, bleeding (including fatal and life-threatening), contusion.
* **Serious:** Bleeding, ventricular pauses, increased serum creatinine, increased serum uric acid.
* **Other:** Hypotension, dizziness, headache, rash.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid concomitant use with strong CYP3A4 substrates with narrow therapeutic indices (e.g., simvastatin, lovastatin). Consider reducing the dose of other CYP3A4 substrates (e.g., atorvastatin, cyclosporine).
* **CYP3A4 Inhibitors:** Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor exposure and should be avoided.
* **CYP3A4 Inducers:** Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) can decrease ticagrelor exposure and may reduce efficacy.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea, especially in patients with a history of asthma or COPD.
* Periodically monitor serum creatinine and uric acid.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, meaning platelet inhibition wears off more quickly after discontinuation compared to clopidogrel. This may be advantageous in patients who require urgent surgery.
* Dyspnea is a common side effect, often transient and not indicative of underlying cardiac or pulmonary disease. However, it should be evaluated.
* Patients who are unable to swallow pills can open the capsule and dissolve the contents in water. Do not use other liquids.
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*Disclaimer: This information is intended for healthcare professionals. Always consult the most current prescribing information and relevant clinical guidelines before making any treatment decisions.*
