Gb IIb/IIIa Inhibitors (STEMI/NSTEMI/UA) Flashcards
GP IIb/IIIa Inhibitors
Indications
Conformational changes in receptor allow binding with
- Fibrin
- Thrombin
- VWF
Binding triggers:
- Adhesion
- Activation
- Aggregation of platelets
Efficacy order!
- anti platelet
- UA/NSTEMI
Receptor blocking determines antiplatelet efficacy (abciximab>eptifibatide>tirofiban),
Clinical efficacy (UA/NSTEMI): (eptifibatide = tirofiban > abciximab),
and bleeding
GP IIb/IIIa Inhibitors
CI
CI: active or recent bleed 4-6weeks Hemorrhagicaccident CVA in 30 days- 2 ys Severe HTN >180/110 Major surgery/trauma in past 4-6 weeks Thrombocytopenia Bleeding diathesis/warfarin with elevated INR Renal insufficiency/failure
Eptifibatide MOA
Cyclic, small molecule
GP IIb/IIIa receptor antagonist
Selective
Reversible
Competitive inhibition
Temporarily blocks fibrin cross linking btwn active Gp Receptors
Eptifibatide Indications
Medical therapy in NSTEMI ACS with herparin, ASA +/- PCI and stenting
Eptifibatide Metabolism
Half life 1.1-2.5 hrs
(2 half lives at 5 hrs is 75% gone.. 90% gone is 3.3 half lives)
RENAL elimination
Platelet function returns within 4-12 hrs of D/C
Eptifibatide DI/CI/ Caution
Caution: aPTT>/= 45 seconds
CrCl less than 50
Eptifibatide SE
Bleeding (10%)
Eptifibatide considerations
Reduce MI/death by 20% after PCI for ACS when used with ASA
Tirofiban MOA
Nonpeptide, small molecule GP IIb/IIIa receptor antagonist Selective Reversible Competitive inhibition
Temporarily blocks fibrin cross linking btwn active Gp Receptors
Tirofiban Indications
Medical therapy in NSTEMI ACS with herparin, ASA +/- PCI and stenting
Tirofiban Metabolism
Infusion runs for up to 24 hours after PCI
Half life is 2 hrs
RENAL elimination
Platelet function returns within 4-12 hours of D/C
Tirofiban DI/CI/ Caution
Caution:
Platelets /= 45 secs
CrCl less than 30
Tiro Thirty- TT
Tirofiban considerations
Reduce MI/death by 20% after PCI for ACS when used with ASA