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# Ticagrelor
## Overview
Ticagrelor is an orally active, direct-acting P2Y12 receptor antagonist. It is reversible and does not require metabolic activation.
## Primary Indications
* Reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI).
## Adult Dosing
* **Acute Coronary Syndrome (ACS):**
* Loading dose: 180 mg orally once.
* Maintenance dose: 90 mg orally twice daily for at least 12 months.
* Consider extending treatment beyond 12 months in select patients based on risk assessment, but not to exceed 30 months.
* **History of Myocardial Infarction (MI):**
* For patients with a history of MI at least 1 year ago and at high risk for occlusive vascular events, 60 mg orally twice daily. Duration of treatment should be individualized.
## Pediatric Dosing
* Ticagrelor is not recommended in pediatric patients. Safety and efficacy have not been established.
## Dose Adjustments
* **Hepatic Impairment:**
* Mild to moderate hepatic impairment: No dose adjustment needed.
* Severe hepatic impairment: Use with caution.
* **Renal Impairment:**
* Mild to moderate renal impairment: No dose adjustment needed.
* Severe renal impairment or end-stage renal disease: Use with caution.
* **Concomitant medications:** Refer to Key Drug Interactions.
## Contraindications
* Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Most Common:** Dyspnea, bleeding (including fatal and serious bleeding), bradycardia, ventricular pauses.
* **Serious:** Major bleeding, life-threatening bleeding, transient ischemic attacks, stroke, ventricular pauses, dyspnea, hypersensitivity reactions.
## 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 >40 mg daily, atorvastatin >80 mg daily).
* **CYP3A4 Inducers:** Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure and efficacy.
* **CYP3A4 Inhibitors:** Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor exposure.
* **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and consider risks versus benefits.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Monitor for dyspnea, especially in patients with a history of asthma or COPD.
* Monitor heart rate for bradycardia.
## Clinical Pearls
* Ticagrelor is dosed twice daily, unlike other P2Y12 inhibitors.
* Dyspnea is a common side effect and may be dose-limiting for some patients, but it is usually transient and not associated with underlying pulmonary disease.
* Discontinuation of ticagrelor prematurely increases the risk of thrombotic events.
* If possible, discontinue ticagrelor 5 days prior to elective surgery.
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*This information is intended for healthcare professionals. Always consult the current prescribing information and relevant literature for complete and up-to-date guidance.*
