Why We Need Intravenous Antiplatelet Agents

Abstract

Oral ADP-receptor antagonists combined with aspirin are the standard for dual antiplatelet therapy (DAPT) during percutaneous coronary intervention (PCI). However, the oral route of administration of ADP-receptor antagonists leaves them vulnerable to unpredictable and often inadequate platelet inhibition at the time of PCI, while their prolonged effects often lead to the decision not to load them prior to PCI. Intravenous antiplatelet agents, including glycoprotein IIb/IIIa inhibitors (GPI) and cangrelor, a reversible P2Y12 inhibitor, address these shortcomings. In June 2015, the US FDA approved cangrelor for the prevention of thrombotic events associated with coronary stenting. This review examines the current state of peri-PCI DAPT and demonstrates that the selective use of GPIs and intravenous ADP-antagonist agents reduces the risk of periprocedural thrombosis.

Adenosine Receptor Agonists Exhibit Anti-Platelet Effects and the Potential to Overcome Resistance to P2Y12 Receptor Antagonists

“…Thienopyridines are prodrugs: their short-lived active metabolites irreversibly inactivate the receptor and consequently inhibit ADP-induced platelet activation. Cangrelor is the first (recently approved) intravenous P2Y 12 receptor inhibitor that reversibly and non-competitively blocks ADP signalling [6].Adenosine is an important purine metabolite, serving not only as a component of nucleic acids and ATP, the most important energy carrier in the cell, but also as a signalling molecule regulating many cell processes [7,8]. Adenosine receptors (AR) are a subfamily of highly conserved G protein-coupled receptors located in the membranes of various cells and with different physiological functions.…”

“…Thienopyridines are prodrugs: their short-lived active metabolites irreversibly inactivate the receptor and consequently inhibit ADP-induced platelet activation. Cangrelor is the first (recently approved) intravenous P2Y 12 receptor inhibitor that reversibly and non-competitively blocks ADP signalling [6].…”

Blood Platelet Adenosine Receptors as Potential Targets for Anti-Platelet Therapy

“…Although all three agents have an indication for use in acute coronary syndromes, current guidelines suggest the preferential use of prasugrel and ticagrelor over clopidogrel because of their superior clinical benefits, i.e., the improved efficacy, lowered individual variation in response, and less frequent and severe side effects [6]. Cangrelor, in turn, as the recently approved, first P2Y 12 inhibitor administered intravenously, seems to be the most promising in percutaneous coronary interventions [7].…”