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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.
When ticlopidine and clopidogrel were first brought to the market, ticlodipine in 1978 and clopidogrel in 1998, the mechanism of action of these two major antithrombotic drugs was not fully understood. What had been shown was that they were potent inhibitors of ADP-induced platelet aggregation, but the P2Y 12 receptor
70839 Ensembl ENSG00000169313 ENSMUSG00000036353 UniProt Q9H244 Q9CPV9 RefSeq (mRNA) NM_176876 NM_022788 NM_027571 NM_001357007 NM_001357008 NM_001357010 RefSeq (protein) NP_073625 NP_795345 NP_081847 NP_001343936 NP_001343937 NP_001343939 Location (UCSC) Chr 3: 151.34 – 151.38 Mb Chr 3: 59.12 – 59.17 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse P2Y 12 is a chemoreceptor for ...
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).
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.
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 ...