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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.
Clopidogrel is in the thienopyridine -class of antiplatelets. [10] . It works by irreversibly inhibiting a receptor called P2Y 12 on platelets. [10] Clopidogrel was patented in 1982, and approved for medical use in 1997. [6][11] It is on the World Health Organization's List of Essential Medicines. [12] .
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.
The antiaggregating properties of this compound are well known and, very recently, new results have clarified its mechanism of action. Clopidogrel is active only after intravenous or oral administration, and no circulating activity has been found in the plasma of treated animals or human volunteers.
MECHANISM OF ACTION. inhibition of the ADP platelet receptor and subsequent ADP-mediated activation of the glycoprotein IIb/IIIa complex -> inhibits platelet aggregation. PHARMACEUTICS.
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.
