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Mechanism of action. Clopidogrel is activated via a 2 steps reaction to an active thiol-containing metabolite. 3 This active form is a platelet inhibitor that irreversibly binds to P2Y 12 ADP receptors on platelets. 9 This binding prevents ADP binding to P2Y 12 receptors, activation of the glycoprotein GPIIb/IIIa complex, and platelet ...
10 Ιουλ 2023 · Mechanism of Action. Clopidogrel is an irreversible inhibitor of the platelet P2Y12 adenosine diphosphate receptor. Inhibition of this receptor prevents the downstream activation of the glycoprotein IIb/IIIa receptor complex, which leads to reduced platelet aggregation.
Production of clopidogrel active metabolite and its effect on platelet aggregation. Clopidogrel is metabolized in the liver by cytochrome P450 enzymes, producing Act-Met. Act-Met irreversibly binds and disables the platelet receptor P2Y12.
The antiaggregating property of clopidogrel is caused by an inhibition of the binding of ADP to its platelet receptors, and more specifically to the low affinity receptors, the high affinity binding sites being unaffected by clopidogrel.
Mechanism of action of clopidogrel. Clopidogrel is a prodrug, the majority of which is metabolized into inactive metabolites by esterases. About 15% is converted to active metabolites by various hepatic cytochrome P450 enzymes (CYP3A4, CYP3A5, and CYP2C19).
17 Φεβ 2020 · Mechanism of Action. Clopidogrel requires in vivo biotransformation to an active thiol metabolite. The active metabolite irreversibly blocks the P2Y 12 component of ADP receptors on the platelet surface, which prevents activation of the GPIIb/IIIa receptor complex, thereby reducing platelet aggregation.
7 Νοε 2022 · Antiplatelet medications are divided into oral and parenteral agents. Oral agents subdivide further based on the mechanism of action. Aspirin was the first antiplatelet medication and is a cyclooxygenase inhibitor. Other oral antiplatelet agents include clopidogrel, ticagrelor, prasugrel, pentoxifylline, cilostazol, and dipyridamole.
