Cardiovascular Critical Care I
2011;58:e123-210; J Am Coll Cardiol 2011;58:e44-122; Br J Clin Pharmacol 2011;72:647-57)
Medication
Heparin (UFH)a
Bivalirudin
Eptifibatide
Tirofiban
Cangrelorb
Mechanism of
action
Indirect thrombin
inhibition (binds to
antithrombin III)
Direct thrombin inhibitor
Binds to GP IIb/IIIa platelet
receptor, inhibiting final
common pathway for platelet
aggregation
Binds to GP IIb/
IIIa platelet receptor,
inhibiting final
common pathway for
platelet aggregation
Inhibits ADP-mediated platelet
activation at P2Y12 receptor
Bolus dose
50–100 units/kg
based on target
activated clotting
time (ACT)
0.75 mg/kg
180 mcg/kg x 2, 10 min apart
25 mcg/kg
30 mcg/kg
Continuous
infusion
Not typically given
during PCI
1.75 mg/kg/hr
2 mcg/kg/min
0.15 mcg/kg/min
4 mcg/kg/min
Platelet inhibition
Indirectly inhibits
thrombin-mediated
platelet activation
Indirectly inhibits thrombin-mediated
platelet activation
Restoration of platelet function
within 6–8 hr of discontinuation
Restoration of
platelet function
within 6–8 hr of
discontinuation
Onset of platelet inhibition
within min of administration
Restoration of platelet function
within 1 hr of discontinuation
Elimination
Hepatic and reticulo-
endothelial system
80% plasma proteolysis
20% renal
Renal (50%)
Renal (65%)
Plasma dephosphorylation
Removed by
dialysis
No
Partial
Yes
Yes
N/A
Other notable
adverse effect(s)
or clinical pearls
Target ACT of about
200–300 s during
procedure based on
presence of GP IIb/
IIIa inhibitor and
device used
Requires renal dose adjustment
Useful in patients with suspected or
confirmed HIT
May be preferred in patients with higher
bleeding risk (particularly compared
with UFH with GP IIb/IIIa inhibitor
and among patients who undergo a
transfemoral PCI approach)
Requires renal dose adjustment
Acute, profound
thrombocytopenia
Requires renal dose
adjustment
Acute, profound
thrombocytopenia
Oral prasugrel and clopidogrel
must be given immediately
after discontinuation of
cangrelor infusion to maintain
platelet inhibition. Ticagrelor
should be given as soon as
possible, and administration
may overlap with cangrelor
infusion to maintain platelet
inhibition after cessation of
cangrelor
aEnoxaparin may be used as an alternative to UFH.
bU.S. Food and Drug Administration (FDA) approved as an adjunct to PCI for reducing the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients who have
not been treated with a P2Y12 platelet inhibitor and are not receiving a glycoprotein IIb/IIIa inhibitor.
ACT = activated clotting time; GP = glycoprotein; HIT = heparin-induced thrombocytopenia; N/A = not applicable; UFH = unfractionated heparin.