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# Ticagrelor (Ticagrelor)
## Overview
Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor. It prevents the activation of platelets by adenosine diphosphate (ADP).
## 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 a history of MI who are at high risk for an event.
## Adult Dosing
* **ACS:** 180 mg orally once as a loading dose, followed by 90 mg orally twice daily for at least 12 months.
* **History of MI (at high risk):** 90 mg orally twice daily. Duration of therapy should be individualized based on patient risk.
* **Patients already on clopidogrel and aspirin for ACS:** Can be switched to ticagrelor 90 mg twice daily.
## Pediatric Dosing
There is no established pediatric dosing for ticagrelor.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment needed for mild to moderate hepatic impairment. Use with caution in severe hepatic impairment.
* **Renal Impairment:** No dose adjustment needed for mild to moderate renal impairment. Use with caution in severe renal impairment.
## Contraindications
* Hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
* Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin).
## Adverse Effects
* **Most Common:** Bleeding (including fatal and serious bleeding), dyspnea, bradycardia, ventricular pauses.
* **Other:** Contusion, hypertension, rash, diarrhea, nausea.
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor inhibits CYP3A4, increasing concentrations of co-administered CYP3A4 substrates (e.g., statins, calcium channel blockers). Monitor for increased adverse effects of these drugs.
* **CYP3A4 Inducers:** Inducers of CYP3A4 (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor concentrations.
* **Strong CYP3A4 Inhibitors:** Contraindicated due to increased ticagrelor exposure and risk of bleeding.
* **Aspirin:** Concomitant use is generally recommended, but increases bleeding risk.
* **Anticoagulants (e.g., Warfarin, DOACs):** Increased risk of bleeding.
* **NSAIDs:** Increased risk of bleeding.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding, especially during the initial treatment period.
* **Heart Rate:** Monitor for bradycardia.
* **Renal Function:** Monitor periodically, especially in patients with pre-existing renal impairment.
* **Hepatic Function:** Monitor periodically, especially in patients with pre-existing hepatic impairment.
## Clinical Pearls
* Ticagrelor should be initiated as soon as possible after the onset of ACS, or in patients with a history of MI at high risk.
* The maintenance dose of 90 mg twice daily should be continued for at least 12 months in ACS patients, unless discontinued due to bleeding or other clinical reasons.
* If a dose is missed, patients should take the missed dose immediately and then return to their regular dosing schedule. Do not double the dose.
* Patients experiencing dyspnea should be evaluated for underlying causes. If no other cause is identified, discontinuation may be considered.
* Ticagrelor does not require a loading dose or dose adjustment in patients with mild to moderate hepatic or renal impairment.
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*This information is intended for healthcare professionals. Always consult the most current prescribing information for complete details and to ensure patient safety.*
