Update on platelet glycoprotein IIb/IIIa inhibitors: recommendations for clinical practice

Abstract

Antiplatelet therapy is the cornerstone of treatment for patients with acute coronary syndrome (ACS) and undergoing percutaneous coronary intervention (PCI). Glycoprotein IIb/IIIa receptors mediate platelet aggregation, representing the final common pathway of platelet-mediated thrombosis. Therefore, agents blocking this pathway may be desirable for the treatment of patients with ACS and PCI. Glycoprotein IIb/IIIa receptor inhibitors have been widely investigated and have been key to the pharmacological advancements in the field. However, although GPIs have been important to reduce ischemic complications, their elevated risk of bleeding complications remains a major limitation. The poor prognostic implications, including increased mortality, associated with bleeding complication underscores the need for alternative treatment options. Over the past years there have been several advancements in antithrombotic pharmacology which have led to changes in recommendations for GPI usage in clinical practice. This is an overview of the most recent clinical trial data on GPIs, and provides practical insight on their modern day use in ACS therapy.

International Expert Consensus on Switching Platelet P2Y 12 Receptor–Inhibiting Therapies

“…Clopidogrel therapy is the standard of care in patients treated with thrombolytics who require P2Y 12 inhibitor therapy. Escalation of P2Y 12 inhibitors is discouraged within 24 hours of thrombolysis because the combination of lytics with potent platelet inhibitors (ie, glycoprotein IIb/IIIa inhibitors) increases bleeding 98 ; after this duration, any escalation to a more potent regimen should occur with an LD regimen (prasugrel 60 mg or ticagrelor 180 mg).…”

Pharmacotherapy in the Cardiac Catheterization Laboratory

“…In the era before DAPT, trials of adequately dosed GP IIb/IIIa inhibitors in patients undergoing balloon angioplasty and coronary stent implantation demonstrated a lower incidence of composite ischemic events in favor of GP IIb/IIIa treatment in combination with UFH, than with UFH alone, primarily through a reduction in MI (16). However, there is no evidence for an additional benefit of routine upstream use of GP IIb/IIIa inhibitors in NSTEMI patients scheduled for coronary angiography [16][17][18]. Therefore, GP IIb/IIIa antagonists should be considered for bail-out situation or thrombotic complications.…”

Antiplatelet therapy – a summary for the general physicians

“…18 However, because of the fast onset of action and relatively quick elimination (approximately 4 hours), GPIs are increasingly being considered as a 'bridging' strategy for patients on dual antiplatelet therapy needing surgical procedures. 18,19 In the peri-procedure setting, discontinuation of antiplatelet therapy for a considerable period can be associated with an increase in thrombosis. Randomised controlled trials are underway in this area.…”

“…17 The latter two have a shorter half-life, and are renally excreted, while abciximab has a higher affinity for the receptor, and does not require dose adjustments in renal impairment. 18 With the availability of potent antiplatelet agents in oral formulation, the use of GPI is currently restricted to patients with unstable angina who require percutaneous coronary intervention (PCI) and cannot be pretreated with a P2Y12 blocker. 18 However, because of the fast onset of action and relatively quick elimination (approximately 4 hours), GPIs are increasingly being considered as a 'bridging' strategy for patients on dual antiplatelet therapy needing surgical procedures.…”

“…18 With the availability of potent antiplatelet agents in oral formulation, the use of GPI is currently restricted to patients with unstable angina who require percutaneous coronary intervention (PCI) and cannot be pretreated with a P2Y12 blocker. 18 However, because of the fast onset of action and relatively quick elimination (approximately 4 hours), GPIs are increasingly being considered as a 'bridging' strategy for patients on dual antiplatelet therapy needing surgical procedures. 18,19 In the peri-procedure setting, discontinuation of antiplatelet therapy for a considerable period can be associated with an increase in thrombosis.…”