BLACK BOX WARNING
- contraindicated in prior stroke/TIA — net harm established in TRITON-TIMI 38
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
- TRITON-TIMI 38: prasugrel superior to clopidogrel in ACS-PCI but higher bleeding risk
- AVOID in prior stroke/TIA (net harm), age >=75, or weight <60 kg
- More potent and less susceptible to CYP2C19 polymorphism than clopidogrel
- 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.