prasugrel

Brand: Effient

⚠ BBW Prototype: clopidogrel
Drug Class: antiplatelet
Drug Family: antiplatelet
Subclass: P2Y12 ADP receptor antagonist (thienopyridine prodrug)
Organ Systems: cardiovascular

Mechanism of Action

Prodrug more efficiently activated than clopidogrel; irreversible P2Y12 blockade; more potent and consistent than clopidogrel; less susceptible to CYP2C19 polymorphism.

P2Y12 ADP receptor

Indications

  • ACS with planned PCI (TRITON-TIMI 38)

Contraindications

  • active pathological bleeding
  • prior stroke/TIA (NET HARM)
  • age >=75 (relative — higher bleeding risk)
  • weight <60 kg (relative)
  • severe hepatic impairment

Adverse Effects

Common

  • bleeding
  • rash

Serious

  • major hemorrhage (greater than clopidogrel)

Pharmacokinetics (ADME)

Absorption 79% absorbed; rapid hydrolysis and CYP3A4/CYP2C19 activation
Distribution irreversible
Metabolism hepatic (less CYP2C19 dependent than clopidogrel)
Excretion renal 68%, fecal 27%
Half-life 7-10 days (platelet lifespan)
Onset 1 hour
Peak peak 2h
Duration 7-10 days
Protein Binding 98%
Vd variable

Drug Interactions

Drug / Agent Mechanism Severity
warfarin additive bleeding risk major
NSAIDs additive bleeding risk major

Nursing Considerations

  1. TRITON-TIMI 38: prasugrel superior to clopidogrel in ACS-PCI but higher bleeding risk
  2. AVOID in prior stroke/TIA (net harm), age >=75, or weight <60 kg
  3. More potent and less susceptible to CYP2C19 polymorphism than clopidogrel
  4. Hold 7 days before surgery

Clinical Pearls

  • More potent antiplatelet effect than clopidogrel: less CYP2C19 dependency
  • TRITON-TIMI 38: reduced stent thrombosis and CV events but increased fatal bleeding, including intracranial hemorrhage in prior TIA/stroke patients

Safety Profile

Pregnancy avoid
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.