BOXED WARNING Diminished antiplatelet effect in CYP2C19 poor metabolizers; consider an alternative P2Y12 inhibitor.
FDA dosing
Population
Start
Target
Max
Acute coronary syndrome
Adult
300 mg loading dose once, then 75 mg QD
75 mg QD
Recent MI, recent stroke, or established peripheral arterial disease
Adult
75 mg QD (no loading dose)
75 mg QD
Renal Limited experience in moderate-to-severe renal impairment
Hepatic No adjustment needed
Instructions
Initiating without a loading dose (ACS) delays antiplatelet effect by several days
Interrupt therapy 5 days before elective surgery with major bleeding risk; resume as soon as hemostasis achieved
Contraindications
Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage)
Cautions
Increased risk of bleeding
Premature discontinuation increases risk of cardiovascular events
Thrombotic thrombocytopenic purpura (may be fatal, even after <2 weeks)
Cross-reactivity among thienopyridines
Reduced effectiveness in CYP2C19 poor metabolizers
Adverse reactions
Bleeding (including life-threatening and fatal)
Epistaxis
Hematuria/hematoma/bruise
Pruritus
Thrombotic thrombocytopenic purpura
Pregnancy No drug-associated risk identified; discontinue 5-7 days before labor/delivery or neuraxial blockade (maternal bleeding/spinal hematoma risk)
Lactation No human data; present in rat milk
⚠ BOXED WARNING
Diminished effectiveness in CYP2C19 poor metabolizers