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An antiplatelet drug (antiaggregant), also known as a platelet agglutination inhibitor or platelet aggregation inhibitor, is a member of a class of pharmaceuticals that decrease platelet aggregation [1] and inhibit thrombus formation.
Glycoprotein IIb/IIIa inhibitors are frequently used during percutaneous coronary intervention (angioplasty with or without intracoronary stent placement). They work by preventing platelet aggregation and thrombus formation. They do so by inhibition of the GpIIb/IIIa receptor on the surface of the platelets.
Platelet aggregation plays a critical role in the genesis of a resulting thrombus. Adhesion should remain local, but platelet aggregation must grow exponentially to form a platelet thrombus and prevent blood loss. Platelet aggregation factors are the regulators that enhance the adhesion and stimulate the platelets to secrete its granules.
The first P2Y 12 inhibitors were of the thienopyridine family. They are indirect antagonists, which block the ADP-induced platelet aggregation and activation. The first drug of this class was ticlopidine and was discovered in 1972 at Porcor (now Sanofi).
The complex is formed via calcium-dependent association of gpIIb and gpIIIa, a required step in normal platelet aggregation and endothelial adherence. [ 2 ] [ 3 ] Platelet activation by ADP (blocked by clopidogrel ) leads to the aforementioned conformational change in platelet gpIIb/IIIa receptors that induces binding to fibrinogen. [ 1 ]
Abciximab, a glycoprotein IIb/IIIa receptor antagonist manufactured by Janssen Biologics BV and distributed by Eli Lilly under the trade name ReoPro, is a platelet aggregation inhibitor mainly used during and after coronary artery procedures like angioplasty to prevent platelets from sticking together and causing thrombus formation within the coronary artery.
[34] [35] ADP-induced platelet aggregation and activation are hence hindered. Examples include clopidogrel, prasugrel and ticagrelor. Clopidogrel has a common drug interaction with CYP2C19 inhibitors, particularly omeprazole and esomeprazole which are indicated for treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Aggregation of platelets is highly regulated by cyclic nucleotides. PDE3A is a regulator of this process, and PDE3 inhibitors effectively prevent aggregation of platelets. Cilostazol is approved for treatment of intermittent claudication and is thought to involve inhibition of platelet aggregation and also inhibition of smooth muscle ...