Prasugrel hydrochloride for the treatment of acute coronary syndromes

Expert Opin Pharmacother. 2015 Mar;16(4):585-96. doi: 10.1517/14656566.2015.1005602. Epub 2015 Jan 29.

Abstract

Introduction: P2Y12 receptor antagonists, by inhibiting platelet activation and subsequent aggregation, are critical to prevent ischemic event recurrence after an acute coronary syndrome (ACS). Prasugrel is a third-generation thienopyridine whose metabolites target the P2Y12 receptor. Compared with clopidogrel, prasugrel has a more potent, faster in onset, and more consistent P2Y12 receptor inhibition.

Areas covered: This review describes prasugrel chemistry, pharmacokinetics, pharmacodynamics and clinical studies. In a Phase III randomized clopidogrel-controlled trial, prasugrel improved cardiovascular outcome (risk reduction of cardiovascular death, non-fatal heart attack and non-fatal stroke) at the cost of increased major and fatal bleeding complications. Prasugrel, in combination with aspirin, has been approved by European and American regulatory agencies for the prevention of atherothrombotic events in patients with ACS who undergo percutaneous coronary intervention (PCI).

Expert opinion: Prasugrel is effective for managing ACS patients with planned PCI and it offers an alternative with potential benefits over clopidogrel. Prasugrel is currently challenged by ticagrelor, a P2Y12 receptor antagonist with different pharmacokinetic/pharmacodynamic properties. The superiority of one drug to the other cannot be reliably estimated from the current trials. Ongoing randomized and observational studies may help to provide valuable information on the safety and efficacy of these two drugs and their respective places with ACS patients.

Keywords: acute coronary syndrome; platelet reactivity; prasugrel.

Publication types

  • Review

MeSH terms

  • Acute Coronary Syndrome / drug therapy*
  • Animals
  • Aspirin / therapeutic use
  • Clinical Trials, Phase III as Topic
  • Clopidogrel
  • Drug Therapy, Combination
  • Humans
  • Percutaneous Coronary Intervention
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Platelet Aggregation Inhibitors / pharmacokinetics
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Practice Guidelines as Topic
  • Prasugrel Hydrochloride
  • Purinergic P2Y Receptor Antagonists / pharmacokinetics
  • Purinergic P2Y Receptor Antagonists / pharmacology
  • Purinergic P2Y Receptor Antagonists / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Thiophenes / pharmacokinetics
  • Thiophenes / pharmacology
  • Thiophenes / therapeutic use*
  • Ticlopidine / analogs & derivatives
  • Ticlopidine / therapeutic use

Substances

  • Piperazines
  • Platelet Aggregation Inhibitors
  • Purinergic P2Y Receptor Antagonists
  • Thiophenes
  • Clopidogrel
  • Prasugrel Hydrochloride
  • Ticlopidine
  • Aspirin