[Update on the treatment with platelet antiaggregation agents].
Antiplatelet agents are primarily used to prevent and treat arterial thrombosis. Their mechanism of action is related to the interaction with metabolism of arachidonic acid, the increase of intraplatelet cAMP or the antagonism of ADP or GP IIb/IIIa receptors. Aspirin was one of the first agents to be adopted and it remains as the standard therapy with the higher amount of available clinical information. Following aspirin, ADP receptor antagonists like ticlopidine and more recently clopidogrel have been introduced. In the CAPRIE study, clopidogrel was shown to be more effective than aspirin in the prevention of vascular events in patients with atherothrombotic disease. The newer antiplatelet agents are GP IIb/IIIa receptor antagonists like eptifibatide, tirofiban and abciximab, which act at the end of the common pathway of platelet aggregation. Their benefits after intravenous administration have been shown in the treatment of acute coronary syndrome and percutaneous coronary angioplasty. The potential application of GIIb/IIIa targeted therapy might theortically be expanded by the new class of oral GP IIb/IIIa antagonists. However, their performance in clinical trials has been disappointing.
Rodrigues
H L
HL
Instituto de Farmacologia, Faculdade de Medicina de Lisboa, Lisboa, Portugal.
D000077284:Abciximab; D000244:Adenosine Diphosphate / Q000378:metabolism; D000911:Antibodies, Monoclonal / Q000494:pharmacology; D016718:Arachidonic Acid / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D000077542:Eptifibatide; D006801:Humans; D007140:Immunoglobulin Fab Fragments / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology; D015539:Platelet Activation / Q000502:physiology; D010975:Platelet Aggregation Inhibitors / Q000627:therapeutic use*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D013928:Thromboxane A2 / Q000378:metabolism; D000077466:Tirofiban; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000911:Antibodies, Monoclonal; D007140:Immunoglobulin Fab Fragments; D010455:Peptides; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D016718:Arachidonic Acid; D014443:Tyrosine; D013928:Thromboxane A2; D000244:Adenosine Diphosphate; D011451:Prostaglandin-Endoperoxide Synthases; D000077466:Tirofiban; D000077542:Eptifibatide; D000077284:Abciximab