GPIIb/IIIa Receptor Antagonist (Non-Peptide Mimetic) Pregnancy: Contraindicated — insufficient data.

Tirofiban (GPIIb/IIIa Inhibitor — ACS/PCI)

Brand names: Aggrastat

Adult dose

Dose: High-dose bolus (HDB) regimen (current standard): 25 mcg/kg IV over 3 minutes, then 0.15 mcg/kg/min for 18–24 hours. Standard regimen (historical): 0.4 mcg/kg/min over 30 min, then 0.1 mcg/kg/min

Route: IV bolus then infusion

Frequency: Continuous infusion after loading

Max: Infusion: 0.15 mcg/kg/min

Non-peptide GPIIb/IIIa antagonist. High-dose bolus regimen achieves faster and more complete platelet inhibition than original dosing — improves outcomes in high-risk ACS with PCI. Platelet function recovers within 4–8 hours of stopping. Used in high-risk NSTEMI and as bailout in PCI.

Paediatric dose

Route:

Not licensed in paediatrics.

Dose adjustments

Renal

eGFR <30 mL/min: reduce infusion rate by 50% (0.075 mcg/kg/min after HDB bolus).

Hepatic

No dose adjustment for mild-moderate hepatic impairment.

Clinical pearls

PRISM-PLUS trial (NEJM 1998): tirofiban + heparin vs heparin alone in NSTEMI — 32% relative risk reduction in composite endpoint at 7 days. The tirofiban-only arm (without heparin) was stopped early for excess mortality — emphasises importance of combination with anticoagulation
High-dose bolus (HDB) regimen development: original tirofiban dosing provided insufficient early platelet inhibition at time of PCI. STRATEGY and On-TIME 2 trials demonstrated HDB (25 mcg/kg) achieves >90% platelet aggregation inhibition within minutes — now the recommended regimen in ESC guidelines
Acute profound thrombocytopenia: tirofiban (and other GPIIb/IIIa inhibitors) can cause acute profound thrombocytopenia within 2–6 hours of first dose — immediate platelet count mandatory at 4–6 hours; stop drug and give platelet transfusion if platelet count <20 × 10⁹/L with bleeding

Contraindications

Active major bleeding
Recent stroke (within 30 days) or history of haemorrhagic stroke
Severe hypertension (SBP >180, DBP >110)
Platelet count <100 × 10⁹/L
Major surgery within 6 weeks

Side effects

Bleeding (most common serious adverse event — major bleeding 1–5%)
Thrombocytopenia (acute profound: <50 × 10⁹/L in 0.2% — within hours of initiation; stop drug immediately)
Nausea
Fever

Interactions

Anticoagulants and antiplatelets (additive major bleeding risk — requires careful dose management of heparin in ACS protocols)
Thrombolytics (avoid concurrent systemic use)

Monitoring

Platelet count at baseline and 4–6 hours after starting (acute thrombocytopenia detection)
aPTT (heparin co-therapy — target 50–70 seconds)
Access site haemostasis
Renal function (dose adjustment criterion)
ECG and haemodynamics

Reference: BNFc; BNF 90; PRISM-PLUS Trial (NEJM 1998); On-TIME 2 Trial (NEJM 2008); ESC ACS NSTEMI Guidelines 2023; MHRA SPC Aggrastat. Verify against your local formulary and the latest BNF before prescribing.

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways