Antiplatelet drugs play a crucial role in the treatment of patients with myocardial infarction, particularly in association with percutaneous coronary intervention. Their main advantage is the reduction of adverse ischemic incidents and the major disadvantage is the increase in the frequency of hemorrhages. Thus, the choice of appropriate drug depends on the right risk assessment of the develop...

Ticlopidine, clopidogrel, and prasugrel are thienopyridine prodrugs that inhibit adenosine-5'-diphosphate (ADP)-mediated platelet aggregation in vivo. These compounds are converted to thiol-containing active metabolites through a corresponding thiolactone. The 3 compounds differ in their metabolic pathways to their active metabolites in humans. Whereas ticlopidine and clopidogrel are metabolize...

Clinical studies with clopidogrel or prasugrel show that although increased inhibition of P2Y(12) and platelet function improves efficacy, bleeding is also increased. Other preclinical and clinical studies have suggested a greater therapeutic index (TI) with reversible inhibitors and disproportionate effects of thienopyridines on bleeding at high doses. We used multiple in vivo (FeCl(3)-induced...

Despite advancements in treatments for acute coronary syndromes over the last 10 years, they continue to be life-threatening disorders. Currently, the standard of treatment includes dual antiplatelet therapy consisting of aspirin plus a P2Y12 receptor antagonist. The thienopyridine class of P2Y12 receptor antagonists, clopidogrel and prasugrel, have demonstrated efficacy. However, their use is ...

Antiplatelet therapy in acute coronary syndromes is essential for preventing stent thrombosis and for reducing major adverse cardiovascular events. Treatment strategy has changed over the last years by frequent use of more active agents inhibiting the ADP mediated activation of platelets instead of clopidogrel, such as prasugrel and ticagrelor. Compared to clopidogrel these modern antiplatelet ...

Thrombosis and Haemostasis 108.2/2012 The development of oral inhibitors of the platelet P2Y12 receptor has improved outcomes in patients with acute coronary syndromes (ACS) and in patients with coronary artery disease undergoing percutaneous coronary intervention (PCI) with stenting. The first thienopyridine drug, ticlopidine, proved to be effective after coronary stenting, but because of many...

Dermatology topics include agents for psoriasis, urticaria, and infantile hemangiomas. The pros and cons of antiplatelet drugs prasugrel (Effient) and ticagrelor (Brilinta) are discussed, and an investigational agent, cangrelor, shows promise in reducing ischemic events when compared with clopidogrel (Plavix).

The thienopyridine antiplatelet drugs, such as ticlopidine, clopidogrel, and prasugrel, require activation by cytochromes P450 in vivo to effectively block platelet aggregation. The study of the metabolic activation of these compounds has been hampered by the lability and reactivity of the ring-opened active metabolite (AM) and by the numerous metabolites that can be formed in such a transforma...

Diabetics have a prothrombotic state that includes increased platelet reactivity. This contributes to the less favorable clinical outcomes observed in diabetics experiencing acute coronary syndromes as well as stable coronary artery disease. Many diabetics are relatively resistant to or have insufficient response to several antithrombotic agents. In the setting of percutaneous coronary interven...

BackgroundDespite recommendations for standardized preoperative waiting of at least 3, 5, and 7 days ticagrelor, clopidogrel, prasugrel, respectively, there is still substantial interinstitutional variation in discontinuation dual antiplatelet therapy patients needing coronary artery bypass grafting (CABG).MethodsIn 299 undergoing CABG with or without valve intervention less than after last P2Y...