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# Ticagrelor ## Overview Ticagrelor is an oral, direct-acting, reversibly binding P2Y12 platelet inhibitor. It is used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS). ## Primary Indications * Acute Coronary Syndrome (ACS) - typically in combination with aspirin. ## Adult Dosing * **ACS:** Loading dose of 180 mg orally once, followed by 90 mg orally twice daily. * **Maintenance dose for patients who have completed treatment for ACS:** In some regions, a lower maintenance dose of 60 mg twice daily may be used for patients on long-term therapy after ACS, provided they are not at high risk for bleeding. Consult local guidelines. ## Pediatric Dosing * Dosing in pediatric patients has not been established. ## Dose Adjustments * No dose adjustment is required for patients with mild to moderate hepatic impairment. * Use with caution in severe hepatic impairment. * No dose adjustment is required for patients with mild to moderate renal impairment. * Use with caution in severe renal impairment or end-stage renal disease. ## Contraindications * Active pathological bleeding. * History of intracranial hemorrhage. * Known hypersensitivity to ticagrelor or any of its excipients. * Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) is generally contraindicated due to increased ticagrelor exposure. ## Adverse Effects * **Most Common:** Dyspnea, bleeding (including major and minor), bradycardia, contusion, rash. * **Serious:** Major bleeding, life-threatening bleeding, ventricular pauses. * **Other:** Hyperuricemia, increased serum creatinine. ## Key Drug Interactions * **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Coadministration with sensitive CYP3A4 substrates (e.g., simvastatin, lovastatin) may increase their exposure. Limit statin dose to 40 mg daily for simvastatin and lovastatin. * **CYP3A4 Inducers:** Potent CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure. * **P-glycoprotein (P-gp) Substrates:** Ticagrelor can inhibit P-gp. Coadministration with P-gp substrates (e.g., digoxin) may increase their plasma concentrations. * **Aspirin:** Concurrent use of ticagrelor with aspirin is recommended for ACS. Higher doses of aspirin may reduce ticagrelor's efficacy. * **Other Antiplatelets/Anticoagulants:** Increased risk of bleeding. Use with caution and monitor closely. ## Monitoring * Monitor for signs and symptoms of bleeding. * Monitor for signs and symptoms of dyspnea. * Renal and hepatic function may be monitored periodically. ## Clinical Pearls * Ticagrelor is a P2Y12 inhibitor, not a thienopyridine (like clopidogrel), and does not require metabolic activation. * The 90 mg twice-daily dose is generally preferred for ACS patients due to superior efficacy compared to 60 mg twice daily, particularly in preventing stent thrombosis. * Discontinuation of ticagrelor increases the risk of thrombotic events. If premature discontinuation is necessary, consider the underlying thrombotic risk and the time elapsed since the index event. * Dyspnea is a common side effect and may resolve on its own. If persistent or severe, investigate other causes. *** *Disclaimer: This information is for educational purposes only and does not constitute medical advice. Always consult the most current prescribing information and relevant clinical guidelines for complete details and to confirm drug information before making any treatment decisions.*