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# Ticagrelor (Brilinta) ## Overview - Antiplatelet agent; reversible P2Y12 receptor inhibitor (direct-acting, no need for metabolic activation). - Fast onset, offset (~3-5 days platelet function recovery). ## Primary Indications - Acute coronary syndrome (ACS): STEMI, NSTEMI, unstable angina. - History of MI and high risk for thrombotic events (long-term secondary prevention). - Note: Not for use with aspirin >100 mg daily (increases bleeding risk). ## Adult Dosing - **Loading dose (ACS):** 180 mg once (2 × 90 mg tablets). - **Maintenance (ACS or secondary prevention):** 90 mg twice daily. - **Long-term secondary prevention (post-MI ≥1 year):** 60 mg twice daily (if aspirin ≤100 mg daily). - Administer with or without food. ## Pediatric Dosing - **Safety and efficacy not established** in children (<18 years). No approved dosing. ## Dose Adjustments - **No renal dose adjustment** needed; no hemodialysis data. - **Mild hepatic impairment:** No adjustment. **Moderate/severe hepatic impairment:** Contraindicated (Child-Pugh B/C). - **Concomitant strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir):** Avoid use or consider dose reduction if unavoidable (expert consult). ## Contraindications - Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage). - History of intracranial hemorrhage. - Severe hepatic impairment (Child-Pugh C). - Hypersensitivity to ticagrelor or any component. - Concurrent strong CYP3A4 inducers (e.g., rifampin, phenytoin). ## Adverse Effects - **Bleeding (major/minor):** Epistaxis, ecchymosis, GI bleeding, intracranial hemorrhage. - **Dyspnea:** Common (14–20%), usually mild and transient; evaluate if severe. - **Bradyarrhythmias:** Especially sinus pauses (use caution with AV block, pacemaker). - **Increased serum creatinine/uric acid** (reversible; not nephrotoxic). ## Key Drug Interactions - **Aspirin >100 mg/day:** Increases bleeding risk; maintain <100 mg. - **CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, grapefruit juice):** Increase ticagrelor exposure; avoid. - **CYP3A4 inducers (e.g., rifampin, carbamazepine, dexamethasone):** Decreased efficacy; avoid. - **Simvastatin/lovastatin:** Ticagrelor increases statin levels; limit simvastatin to ≤20 mg daily. - **Digoxin:** Ticagrelor may raise digoxin levels; monitor. ## Monitoring - Platelet function tests not routinely required. - Monitor for signs of bleeding (e.g., bruising, black stools, hematuria). - Assess dyspnea: differentiate from pulmonary causes. - Periodic serum creatinine and uric acid (especially if renal impairment or gout). - ECG for bradycardia in high-risk patients (especially first week). ## Clinical Pearls - **Do not miss a dose;** ticagrelor has twice-daily dosing – half-life ~7 hours. - **Hold before elective surgery** (5 days for major surgery, 3–5 days for minor). - **Loading dose alternative:** 180 mg if >6 hours since last maintenance dose (bypass PCI timing). - **Switching from clopidogrel:** Give 180 mg loading immediatley (no overlap needed). - **Uncertainty:** Pediatric safety/efficacy unestablished; use only in trials. - **Consider PPI co-therapy** if GI bleeding risk; avoid omeprazole (weak CYP2C19 interaction, but minimal effect on ticagrelor; pantoprazole preferred). *Educational disclaimer: This information is for educational purposes and not a substitute for current prescribing guidelines. Always verify dosing and contraindications with the latest approved product labeling and institutional protocols.*