Prasugrel (Effient)
Thienopyridine prodrug rapidly hydrolyzed in intestine/plasma to thiolactone intermediate (R-95913) by carboxylesterase-2, then oxidatively converted to active R-138727 by hepatic CYP3A4/3A5. Active metabolite irreversibly binds P2Y12 ADP receptors. Faster bioactivation than clopidogrel (~70% of dose converts to active form); active metabolite detectable within 15 min, peaks ~30 min post-dose. More potent antiplatelet effect vs. clopidogrel. Approved for acute coronary syndromes at 60 mg loading dose (5 mg maintenance for low body weight <60 kg), or 5-10 mg once daily. Higher bleeding risk than clopidogrel, particularly in elderly (>75 yr). Weight-based dosing considerations.
Projected serum levels — 10 mg, once daily
Maintenance schedule: 10 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 0.11 mg, trough ≈ 0.000 mg body load. Population-based estimate over 15 days for a 10 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Antiplatelet
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 7.4 h
- Common dose
- 10 mg
- Suggested maximum
- 60 mg/day
- Reference dose range
- 5–60 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 60 mg oral — Cmax 0.66 mg/L at 0.50 h
Documented interactions
-
danger
Carbamazepine (Tegretol) + Prasugrel (Effient)
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Prasugrel (Effient) AUC by ~0.50x
-
danger
Efavirenz (Sustiva) + Prasugrel (Effient)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Prasugrel (Effient) AUC by ~0.36x
-
danger
Levothyroxine (Synthroid) + Prasugrel (Effient)
Prasugrel (Effient) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free concentration…
-
danger
Rifampin + Prasugrel (Effient)
Rifampin inducer of CYP3A4 predicted to change Prasugrel (Effient) AUC by ~0.36x
-
danger
Tacrolimus (Prograf) + Prasugrel (Effient)
Prasugrel (Effient) may displace Tacrolimus (Prograf) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free concentration…
-
danger
Warfarin (Coumadin) + Prasugrel (Effient)
Prasugrel (Effient) may displace Warfarin (Coumadin) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free concentration…
Serum checks 199 modeled interaction pairings for prasugrel (effient) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
-
Pharmacokinetics and Pharmacodynamics of Prasugrel, a Thienopyridine P2Y12 Inhibitor
Comprehensive review of prasugrel prodrug bioactivation via CES2 and CYP3A4, active metabolite R-138727 formation (~70% of dose), faster P2Y12 inhibition onset vs. clopidogrel.
-
Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor
Pharmacodynamic study demonstrating R-138727 irreversibly binds P2Y12, with cysteine cross-links at position 97 and 175 of the receptor for sustained platelet inhibition.
-
Prasugrel achieves greater and faster P2Y 12 receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite
Comparative PK/PD study showing prasugrel active metabolite formation faster (~30 min) and more efficient than clopidogrel, resulting in superior antiplatelet effect.
3 published studies referenced in the app, each with a plain-language summary.