Brilinta, as a P2Y12 receptor antagonist, exerts antithrombotic effects by irreversibly inhibiting platelet aggregation. Its drug interactions mainly involve the CYP3A4 metabolic pathway and the synergistic effect of bleeding risk. The following is a layered explanation of pharmacological mechanisms and interactions.

1. Effect of action

(1) Pharmacological mechanism: Ticagrelor selectively and reversibly binds to platelet P2Y12 receptors, blocking ADP mediated platelet activation and aggregation, and acting faster than clopidogrel. The maximum platelet inhibition rate was reached 2 hours after taking the medication, and the inhibition rate remained above 80% at the maintenance dose.

(2) Clinical efficacy

Compared with clopidogrel, it significantly reduces the composite endpoint risk of cardiovascular death/myocardial infarction/stroke by 16%, but may increase the risk of non CABG related major bleeding. The therapeutic advantage is particularly significant in emergency PCI patients.

2 drug interactions

(3) Strong CYP3A4 inhibitors (such as ketoconazole) can increase the AUC of ticagrelor by 5 times and should be avoided in combination; Inducing agents (such as rifampicin) can reduce exposure by 86% and should not be used together. Intermediate acting inhibitors (such as diltiazem) should be used with caution.

(4) Anticoagulant/antiplatelet drugs

The combination of warfarin, heparin, or NSAIDs increases the risk of bleeding and requires close monitoring. Aspirin doses exceeding 100mg/day may weaken the efficacy of ticagrelor and increase the risk of gastrointestinal bleeding.

(5) Other interactions

PPI such as omeprazole may slightly reduce the absorption of ticagrelor, but it does not affect clinical efficacy. The combination of digoxin requires monitoring of blood drug concentration, as ticagrelor may inhibit P-gp transport.

(6) Special precautions

Combination therapy with ticagrelor may increase blood concentrations of simvastatin and lovastatin, and it is recommended to switch to statins that are not metabolized by CYP3A4. The combination of beta blockers should be cautious of the risk of worsening bradycardia.