Intravenous GPIIb-IIIa Antagonists
. | Abciximab . | Eptifibatide . | Tirofiban . | Lamifiban . |
|---|---|---|---|---|
| Brand name | ReoPro | Integrilin | Aggrastat | — |
| Structure | Chimeric antibody | Cyclic heptapeptide | Nonpeptide | Nonpeptide |
| Fab fragment | ||||
| Molecular weight (Daltons) | 47,600 | 832 | 495 | 468 |
| KD (nM) | 5 | 120 | 15 | 9 |
| Plasma half-life | 10-30 min | ∼2.5 h | ∼2 h | ∼2 h |
| Excretion | Unknown | ∼50% renal | 39-69% renal | 90% renal |
| Approved indications* | PCI. Refractory unstable angina when PCI is planned within 24 h. | ACS (unstable. angina and non-Q wave MI) PCI. | ACS (unstable angina and non-Q wave MI). | Not approved — undergoing trials. |
| Approved dose* | For PCI: 0.25 mg/kg bolus, 0.125 μg/kg/min (max 10 μg/min) infusion × 12 h. | For ACS: 180 μg/kg bolus, 2.0 μg/kg/min infusion × 72-96 h (PURSUIT dose). | For ACS: 0.4 μg/kg/min × 30 min, then 0.1 μg/kg/min × 48-108 h. | Not approved — undergoing trials. |
| †For unstable angina: 0.25 mg/kg bolus, 10 μg/min infusion × 18-24 h before PCI, continued 1 h after PCI. | †For PCI: 135 μg/kg bolus, 0.5 μg/kg/min infusion for 20-24 h (IMPACT II dose). | |||
| Abbreviations: ACS, acute coronary syndromes; IMPACT II, Integrilin to Minimize Platelet Aggregation and Coronary Thrombosis-II; KD, dissociation constant; MI, myocardial infarction; PCI, percutaneous coronary intervention; PURSUIT, Platelet IIb/IIIa in Unstable angina: Receptor Suppression Using Integrilin Therapy. | ||||
. | Abciximab . | Eptifibatide . | Tirofiban . | Lamifiban . |
|---|---|---|---|---|
| Brand name | ReoPro | Integrilin | Aggrastat | — |
| Structure | Chimeric antibody | Cyclic heptapeptide | Nonpeptide | Nonpeptide |
| Fab fragment | ||||
| Molecular weight (Daltons) | 47,600 | 832 | 495 | 468 |
| KD (nM) | 5 | 120 | 15 | 9 |
| Plasma half-life | 10-30 min | ∼2.5 h | ∼2 h | ∼2 h |
| Excretion | Unknown | ∼50% renal | 39-69% renal | 90% renal |
| Approved indications* | PCI. Refractory unstable angina when PCI is planned within 24 h. | ACS (unstable. angina and non-Q wave MI) PCI. | ACS (unstable angina and non-Q wave MI). | Not approved — undergoing trials. |
| Approved dose* | For PCI: 0.25 mg/kg bolus, 0.125 μg/kg/min (max 10 μg/min) infusion × 12 h. | For ACS: 180 μg/kg bolus, 2.0 μg/kg/min infusion × 72-96 h (PURSUIT dose). | For ACS: 0.4 μg/kg/min × 30 min, then 0.1 μg/kg/min × 48-108 h. | Not approved — undergoing trials. |
| †For unstable angina: 0.25 mg/kg bolus, 10 μg/min infusion × 18-24 h before PCI, continued 1 h after PCI. | †For PCI: 135 μg/kg bolus, 0.5 μg/kg/min infusion for 20-24 h (IMPACT II dose). | |||
| Abbreviations: ACS, acute coronary syndromes; IMPACT II, Integrilin to Minimize Platelet Aggregation and Coronary Thrombosis-II; KD, dissociation constant; MI, myocardial infarction; PCI, percutaneous coronary intervention; PURSUIT, Platelet IIb/IIIa in Unstable angina: Receptor Suppression Using Integrilin Therapy. | ||||
Approved indications and approved dose according to label of United States Food and Drug Administration (FDA); †FDA approved dose for indication, but may not be optimal (see text). For abciximab in unstable angina, an infusion of 12 h after PCI is recommended. For eptifibatide during PCI, the PURSUIT dose of 180 μg/kg bolus and 2.0 μg/kg/min infusion is recommended. Modified from Lincoff et al. JACC 35, 1103, 2000.