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# Ticagrelor
## Overview
Ticagrelor is an orally active, direct-acting P2Y12 receptor antagonist used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
## Primary Indications
* Prevention of thrombotic events in patients with ACS (unstable angina, non-ST-elevation MI, or ST-elevation MI).
* Prevention of thrombotic events in patients with a history of MI (at least one year after the event).
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* **History of MI (≥1 year post-MI):**
* **Maintenance Dose:** 60 mg orally twice daily.
* **Duration of Therapy:** Generally recommended for at least 12 months in ACS patients, or as per local guidelines and individual risk assessment. For patients with a history of MI, it is typically continued long-term as long as benefit outweighs risk.
## Pediatric Dosing
* There is no established pediatric dosing for ticagrelor. Its use in pediatric populations is not recommended.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is required in patients with mild to severe renal impairment.
* **Hepatic Impairment:** No dose adjustment is required in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to limited data.
## Contraindications
* Hypersensitivity to ticagrelor or any of its excipients.
* Active pathological bleeding.
* History of intracranial hemorrhage.
## Adverse Effects
* **Most Common:** Bleeding (including fatal and life-threatening), dyspnea.
* **Other:** Bruising, hematuria, epistaxis, gastrointestinal hemorrhage, dizziness, headache. Ventricular pauses and bradycardia have also been reported.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase ticagrelor exposure. Strong CYP3A4 inducers (e.g., rifampin, phenytoin) can decrease ticagrelor exposure.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding when used concurrently with other antiplatelets (e.g., aspirin, clopidogrel) or anticoagulants (e.g., warfarin, heparin, direct oral anticoagulants). Use aspirin doses of 100 mg or less for secondary prevention with ticagrelor.
* **OATP1B1/1B3 Inhibitors:** Concomitant use with strong OATP1B1/1B3 inhibitors (e.g., cyclosporine) can increase ticagrelor plasma concentrations.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Consider discontinuation if significant bleeding occurs or if a patient requires concomitant therapy with strong CYP3A4 inducers.
* Assess for dyspnea, especially in patients with pre-existing respiratory conditions.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel.
* The 90 mg twice-daily dose is recommended for ACS patients. The 60 mg twice-daily dose is used for long-term maintenance in patients with a history of MI.
* When used with aspirin, limit aspirin to 100 mg daily for secondary prevention to minimize bleeding risk.
* If a dose is missed, the patient should take the next dose at the scheduled time. Do not double the dose.
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*Disclaimer: This information is intended for educational purposes and is not a substitute for professional medical advice. Always consult with a qualified healthcare provider and refer to the most current prescribing information for definitive guidance.*
