Prasugrel.
Prasugrel is a third-generation thienopyridine which selectively inhibits the platelet P2Y(12) receptor more rapidly, more potently, and with less interindividual response variability compared with the second-generation thienopyridine clopidogrel. Large-scale phase III clinical testing showed that in high-to moderate-risk acute coronary syndrome patients undergoing percutaneous coronary intervention, prasugrel translates into a greater reduction in ischemic events, including stent thrombosis, in the short and long term compared to clopidogrel. Prasugrel, however, is associated with an increased risk of major bleeding, which is more pronounced in certain patient subgroups. The ideal patient population for prasugrel use are those patients without prior transient ischemic attack/stroke, <75 years of age and >60 kg in whom the greatest ischemic benefit is achieved without a significant increase in major bleeding risk. Dose modifications in specific populations or at given time-points may represent an avenue to minimize bleeding risk and therefore maximize the clinical benefit of prasugrel. Ongoing clinical studies with prasugrel will better define the safety and efficacy profiles of this agent and potentially set the basis for new indications for use.
University of Florida College of Medicine-Jacksonville, Jacksonville, FL, USA. dominick.angiolillo@jax.ufl.edu
Antonio
A
Tello-Montoliu
Salvatore D
SD
Tomasello
Dominick J
DJ
Angiolillo
D054058:Acute Coronary Syndrome / Q000188:drug therapy*; D015906:Angioplasty, Balloon, Coronary; D001189:Aryl Hydrocarbon Hydroxylases / Q000502:physiology; D002986:Clinical Trials as Topic; D003362:Cost-Benefit Analysis; D065731:Cytochrome P-450 CYP2C19; D003925:Diabetic Angiopathies / Q000188:drug therapy; D004347:Drug Interactions; D006801:Humans; D018579:Patient Selection; D010879:Piperazines / Q000008:administration & dosage / Q000009:adverse effects / Q000191:economics / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010974:Platelet Aggregation / Q000187:drug effects; D000068799:Prasugrel Hydrochloride; D058921:Purinergic P2Y Receptor Antagonists / Q000009:adverse effects / Q000191:economics / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D012008:Recurrence; D013876:Thiophenes / Q000008:administration & dosage / Q000009:adverse effects / Q000191:economics / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*
D010879:Piperazines; D058921:Purinergic P2Y Receptor Antagonists; D013876:Thiophenes; D001189:Aryl Hydrocarbon Hydroxylases; C045793:CYP2C19 protein, human; D065731:Cytochrome P-450 CYP2C19; D000068799:Prasugrel Hydrochloride