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# Ticagrelor ## Overview Ticagrelor is an orally active, direct-acting P2Y12 receptor antagonist. It is a member of the cyclopentyltriazolopyrimidine (CPTP) class of drugs. ## Primary Indications * **Acute Coronary Syndromes (ACS):** To reduce the rate of thrombotic cardiovascular events, including cardiovascular death, myocardial infarction, and stroke, in patients with ACS. * **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor is used to reduce the rate of cardiovascular death, MI, and stroke. ## Adult Dosing * **ACS:** * **Loading Dose:** 180 mg orally once. * **Maintenance Dose:** 90 mg orally twice daily. * **History of MI:** * **Maintenance Dose:** 60 mg orally twice daily. * **Duration of Therapy:** For ACS, typically for at least 12 months. For patients with a history of MI, continued therapy beyond 1 year may be considered. * **Maximum Dose:** Not explicitly defined, but doses higher than 90 mg BID have not been shown to be more effective and increase bleeding risk. ## Pediatric Dosing There is no established pediatric dosing for ticagrelor. ## Dose Adjustments * **Hepatic Impairment:** No dose adjustment is recommended in mild to moderate hepatic impairment. Ticagrelor has not been studied in severe hepatic impairment and should be used with caution. * **Renal Impairment:** No dose adjustment is recommended in mild to severe renal impairment. ## Contraindications * Active bleeding. * History of intracerebral hemorrhage. * Known hypersensitivity to ticagrelor or any of its components. ## Adverse Effects * **Most Common:** Bleeding (major and minor), dyspnea. * **Serious:** Fatal bleeding, intracranial hemorrhage, ventricular arrhythmia, bradyarrhythmia, angioedema. * **Other:** Hypotension, atrial fibrillation, rash, pruritus, elevated serum creatinine, elevated uric acid. ## Key Drug Interactions * **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor plasma concentrations. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine) may decrease ticagrelor plasma concentrations. * **CYP3A4 Substrates (Administered to Ticagrelor):** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors may increase plasma concentrations of these substrates. * **Aspirin:** Ticagrelor is generally used in combination with aspirin. However, the combination of ticagrelor and aspirin at doses higher than 100 mg daily increases the risk of bleeding. * **Anticoagulants (e.g., Warfarin, DOACs):** Concomitant use increases the risk of bleeding. * **P-glycoprotein (P-gp) Substrates:** Ticagrelor inhibits P-gp. Caution is advised when co-administering ticagrelor with P-gp substrates that have a narrow therapeutic index (e.g., digoxin). * **Statins:** Ticagrelor can increase simvastatin and atorvastatin exposure, potentially increasing the risk of myopathy. ## Monitoring * **Bleeding:** Monitor for signs and symptoms of bleeding. * **Renal Function:** Monitor serum creatinine, especially in patients with pre-existing renal impairment or those at risk for renal dysfunction. * **Cardiac Rhythm:** Monitor for bradyarrhythmia, particularly in patients with risk factors. ## Clinical Pearls * Ticagrelor is a P2Y12 inhibitor with rapid onset and offset of action. * The 90 mg BID dose is indicated for ACS patients and is generally preferred over the 60 mg BID dose unless specific criteria are met (e.g., history of stroke/TIA or high bleeding risk). * For patients with a history of MI, the 60 mg BID dose is indicated. * Discontinuation of ticagrelor may increase the risk of thrombotic events. If ticagrelor must be discontinued, consider the risks and benefits of restarting or switching to an alternative antiplatelet agent. * Dyspnea is a common side effect and may be related to the drug itself or underlying cardiac conditions. It typically resolves with continued treatment. *** *This information is intended for healthcare professionals. Always consult the current prescribing information and relevant guidelines for complete details before making clinical decisions.*