Version October 2024
| Clopidogrel | Prasugrel | Ticagrelor | Cangrelor | |
| Mechanism of action | Pro-drug, irreversible | Pro-drug, irreversible | Direct-acting, reversible | Direct-acting, reversible |
| Formulation | Oral | Oral | Oral | IV |
| Onset | ≈6 hours with 600 mg LD | ≈60 minutes with 60 mg LD | ≈30 minutes with 180 mg LD | ≈2 minutes |
| Extent of platelet inhibition* | ≈56% | >75% | ≈93% | >90% |
| Metabolic activation enzymes | 1A2, 2C19 (primarily), 2B6, 2C9, 3A4, 3A5 | Intestinal hydrolysis 2C19, 2B6, 2C9, 3A4 | None¶ | None |
| Pharmacokinetic drug interactionsΔ | Many, including PPIs | No major | Several including CYP3A4 inhibitors and inducers | None |
| Time to normalization of platelet function | ≈7 days | ≈7 days | <5 days | ≈60 minutes |
| Stop time before cardiac surgery | 5 to 7 days◊ | 7 to 10 days◊ | 5 to 7 days◊ | Discontinue infusion 1 hour before surgery |
IV: intravenous; LD: loading dose; PPI: proton pump inhibitor.
* At steady state on maintenance dose.
¶ Ticagrelor is metabolized to an active metabolite via CYP3A4; exposure to the active metabolite is about 30 to 40% of the exposure to ticagrelor.
Δ Specific interactions may be determined by use of the drug interaction program included within UpToDate.
◊ Check ADP-based platelet function test to confirm offset of drug effect, if available and clinically indicated.Do you want to add Medilib to your home screen?
