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Dipyridamole inhibits platelet phosphodiesterase, causing an increase in cyclic AMP with potentiation of the action of PGI 2 – opposes actions of TXA 2 Epoprostenol is a prostacyclin that is used to inhibit platelet aggregation during renal dialysis (with or without heparin) and is also used in primary pulmonary hypertension.
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). It was discovered while screening for a new anti-inflammatory drug based on tinoridine.
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.
Direct thrombin inhibitors bind to the active sites of free or clot-bound thrombin to inhibit its effects. Dabigatran etexilate is a common example which has a rapid onset of action. [ 40 ] Whereas direct factor Xa inhibitors including apixaban and rivaroxaban directly bind to clotting factor Xa to block its activity, thus inhibiting thrombin ...
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 ...
Vorapaxar is an antiplatelet drug of the PAR-1 antagonist family. It functions by inhibiting thrombin-related platelet aggregation. This mechanism works by a different pathway from other antiplatelet medications, such as aspirin and P2Y12 inhibitors. Vorapaxar does not affect ADP-mediated platelet aggregation, coagulation parameters, or ...