Ticagre (ticagrelor)

# Ticagre (ticagrelor) ## Overview Ticagrelor is a reversible, non-thienopyridine P2Y12 receptor antagonist. Unlike clopidogrel, it does not require metabolic activation and has a faster onset and offset of action. ## Primary Indications * Reduction of thrombotic cardiovascular events (CV death, MI, and stroke) in patients with Acute Coronary Syndrome (ACS). * Reduction of risk of a first MI or stroke in patients with high-risk coronary artery disease (CAD). ## Adult Dosing * **ACS (Loading):** 180 mg PO once, followed by maintenance. * **ACS (Maintenance):** 90 mg PO twice daily. After 12 months, may reduce to 60 mg twice daily if high ischemic risk (e.g., history of prior MI). * **CAD (High Risk):** 60 mg PO twice daily. ## Pediatric Dosing * **Safety/Efficacy:** Not established. Use is generally avoided in pediatric patients unless specified by institutional protocol for off-label use in specific cardiac conditions. ## Dose Adjustments * **Renal Impairment:** No dose adjustment required. * **Hepatic Impairment:** Avoid in severe hepatic impairment. No adjustment required for mild impairment. * **Aspirin Dosing:** Limit maintenance aspirin to ≤100 mg daily; higher doses reduce ticagrelor efficacy. ## Contraindications * Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage). * History of intracranial hemorrhage. * Severe hepatic impairment. * Known hypersensitivity to ticagrelor. ## Adverse Effects * **Bleeding:** Major and minor bleeding (epistaxis, hematomas, GI bleeds). * **Dyspnea:** Very common; usually mild to moderate, transient, and rarely requires discontinuation. * **Bradyarrhythmias:** Ventricular pauses reported in the first week of therapy. * **Uric Acid:** Increases in serum uric acid levels; rarely associated with gout. ## Key Drug Interactions * **CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin, ritonavir):** Avoid concomitant use; significantly increases ticagrelor exposure. * **CYP3A4 Inducers (e.g., rifampin, phenytoin):** Avoid concomitant use; significantly decreases ticagrelor efficacy. * **Simvastatin/Lovastatin:** Limit doses to ≤40 mg daily due to increased risk of myopathy. * **Digoxin:** Increased exposure; monitor digoxin levels closely upon initiation or dose change of ticagrelor. ## Monitoring * **Signs/Symptoms of Bleeding:** Monitor for bruising, dark stools, or hematuria. * **Dyspnea:** Assess if patient develops new or worsening respiratory symptoms. * **Cardiac Rhythm:** In patients with preexisting high-degree AV block, monitor via ECG during the first week of therapy. ## Clinical Pearls * **Reversibility:** Unlike clopidogrel and prasugrel, ticagrelor inhibition is reversible. Discontinue at least 5 days prior to any elective surgery to reduce bleeding risk. * **Adherence:** Twice-daily dosing is required; missing doses significantly increases the risk of stent thrombosis. * **Dyspnea Management:** If dyspnea is intolerable, consider switching to clopidogrel, but assess for high ischemic risk first. * **ACS Setting:** Should be administered as soon as possible after ACS presentation. *** **Educational Disclaimer:** This information is for educational purposes only. Clinical practice protocols vary by institution. Always verify current prescribing information, contraindications, and drug interactions through official resources (e.g., FDA-approved labeling, Lexicomp, or UpToDate) before prescribing or administering medication.