Prasugrel hydrochloride for the treatment of acute coronary syndromes. [Review]
Prasugrel hydrochloride for the treatment of acute coronary syndromes. [Review]
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. 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.
English
1465-6566
*Acute Coronary Syndrome/dt [Drug Therapy]
*Piperazines/tu [Therapeutic Use]
*Platelet Aggregation Inhibitors/tu [Therapeutic Use]
*Purinergic P2Y Receptor Antagonists/tu [Therapeutic Use]
*Thiophenes/tu [Therapeutic Use]
Animals
Aspirin/tu [Therapeutic Use]
Clinical Trials, Phase III as Topic
Drug Therapy, Combination
Humans
Percutaneous Coronary Intervention
Piperazines/pd [Pharmacology]
Piperazines/pk [Pharmacokinetics]
Platelet Aggregation Inhibitors/pd [Pharmacology]
Platelet Aggregation Inhibitors/pk [Pharmacokinetics]
Practice Guidelines as Topic
Purinergic P2Y Receptor Antagonists/pd [Pharmacology]
Purinergic P2Y Receptor Antagonists/pk [Pharmacokinetics]
Randomized Controlled Trials as Topic
Thiophenes/pd [Pharmacology]
Thiophenes/pk [Pharmacokinetics]
Ticlopidine/aa [Analogs & Derivatives]
Ticlopidine/tu [Therapeutic Use]
MedStar Heart & Vascular Institute
Journal Article
Review
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. 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.
English
1465-6566
*Acute Coronary Syndrome/dt [Drug Therapy]
*Piperazines/tu [Therapeutic Use]
*Platelet Aggregation Inhibitors/tu [Therapeutic Use]
*Purinergic P2Y Receptor Antagonists/tu [Therapeutic Use]
*Thiophenes/tu [Therapeutic Use]
Animals
Aspirin/tu [Therapeutic Use]
Clinical Trials, Phase III as Topic
Drug Therapy, Combination
Humans
Percutaneous Coronary Intervention
Piperazines/pd [Pharmacology]
Piperazines/pk [Pharmacokinetics]
Platelet Aggregation Inhibitors/pd [Pharmacology]
Platelet Aggregation Inhibitors/pk [Pharmacokinetics]
Practice Guidelines as Topic
Purinergic P2Y Receptor Antagonists/pd [Pharmacology]
Purinergic P2Y Receptor Antagonists/pk [Pharmacokinetics]
Randomized Controlled Trials as Topic
Thiophenes/pd [Pharmacology]
Thiophenes/pk [Pharmacokinetics]
Ticlopidine/aa [Analogs & Derivatives]
Ticlopidine/tu [Therapeutic Use]
MedStar Heart & Vascular Institute
Journal Article
Review