BLACK BOX WARNING
- serious bleeding risk
tirofiban
Brand: Aggrastat
⚠ BBW ISMP High Alert Prototype: abciximab
Drug Class: glycoprotein IIb/IIIa inhibitor
Drug Family: antiplatelet
Subclass: non-peptide tyrosine derivative GP IIb/IIIa inhibitor
Organ Systems: cardiovascularhematology-oncology
Mechanism of Action
Small molecule non-peptide mimetic of the RGD sequence in fibrinogen; competitively and reversibly inhibits fibrinogen binding to GP IIb/IIIa receptors, blocking the final common pathway of platelet aggregation; highest selectivity for GP IIb/IIIa among the three agents in this class.
glycoprotein IIb/IIIa receptor (integrin alphaIIb-beta3)
Indications
- acute coronary syndromes (NSTEMI/unstable angina) in patients undergoing PCI or managed medically
Contraindications
- active internal bleeding or history of bleeding diathesis within 30 days
- stroke within 30 days or history of hemorrhagic stroke
- major surgery or severe physical trauma within the preceding month
- severe hypertension (SBP >180 mmHg or DBP >110 mmHg)
- thrombocytopenia <100,000 cells/mcL
Adverse Effects
Common
- bleeding (femoral access site, GI)
- thrombocytopenia
- nausea
Serious
- major hemorrhage
- intracranial hemorrhage
- severe thrombocytopenia (<50,000 cells/mcL)
Pharmacokinetics (ADME)
| Absorption | IV administration only |
| Distribution | Vd approximately 22-42 L; 65% plasma protein bound |
| Metabolism | minimal hepatic metabolism; primarily excreted unchanged |
| Excretion | renal (~65%) and fecal (~25%) as unchanged drug; half the normal infusion rate if CrCl <60 mL/min |
| Half-life | approximately 2 hours |
| Onset | within minutes of bolus |
| Peak | end of initial bolus |
| Duration | platelet function recovers within 4-8 hours of stopping infusion |
| Protein Binding | 65% |
| Vd | 22-42 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| anticoagulants (heparin, DOACs) | additive bleeding risk; heparin used concurrently in ACS/PCI protocols with careful aPTT monitoring | major |
| other GP IIb/IIIa inhibitors | concurrent use not recommended; additive receptor blockade | major |
| NSAIDs and antiplatelet agents | increased bleeding risk | moderate |
Nursing Considerations
- Administer high-dose bolus regimen (25 mcg/kg over 3 minutes, then 0.15 mcg/kg/min) or standard regimen per protocol; reduce maintenance infusion by 50% when CrCl falls below 60 mL/min.
- Monitor platelet count at baseline, 6 hours after initiation, and at 24 hours; severe thrombocytopenia (< 50,000) requires immediate discontinuation and physician notification.
- Prepare heparin per weight-based ACS/PCI protocol when co-administered; monitor aPTT every 4-6 hours; maintain target aPTT 60-100 seconds per institutional protocol.
- Monitor femoral or radial access sites continuously; instruct patient to report new back pain, neurological changes, or signs of retroperitoneal bleeding (hypotension, decreased hematocrit without visible source).
Clinical Pearls
- Tirofiban, eptifibatide, and abciximab all inhibit GP IIb/IIIa but differ critically in reversibility, half-life, and antigenicity; tirofiban's small-molecule structure eliminates the risk of human anti-drug antibodies seen with abciximab.
- The high-dose bolus regimen of tirofiban achieves greater than 90% platelet inhibition immediately and has largely replaced older low-dose regimens in contemporary PCI practice based on ADVANCE trial evidence.
Safety Profile
Pregnancy generally-safe
Lactation insufficient-data
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
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