Αποτελέσματα Αναζήτησης
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.
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 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).
6 Ιαν 2015 · A recent in vitro study reported that the enzymatic activity of the CES1 variant G143E in catalysing the hydrolysis of clopidogrel and 2-oxo-clopidogrel was completely impaired; suppression of CES1 activity greatly enhanced generation of 2-oxo-clopidogrel and clop-AM from clopidogrel in human liver S9 fractions .
The therapeutic efficiency of clopidogrel is manipulated by the actions of hepatic cytochrome P450 (CYP) enzymes and influenced by individual genetic variations.
Clopidogrel is a pro-drug that is metabolised by the cytochrome P450 system to generate the active metabolite which irreversibly inhibits the adenosine diphosphate (ADP) P2Y 12 receptor.
