Pharmacology · Antiplatelet drugs
Tirofiban !
An intravenous non-peptide blocker of the platelet glycoprotein IIb/IIIa receptor, used in acute coronary syndromes without ST elevation.
Updated 2026-11-01
The figure shows the head of human integrin αIIbβ3 with tirofiban in the fibrinogen-binding site (the crystal also holds an antibody fragment used to crystallise it).
Mechanism of action
Tirofiban is a small non-peptide molecule that reversibly blocks fibrinogen binding to glycoprotein IIb/IIIa, the main platelet receptor for aggregation. With the receptor occupied, activated platelets can no longer link together, whatever the trigger. Platelet function returns within hours after the infusion stops.
- Tirofiban blocks the fibrinogen site of glycoprotein IIb/IIIa
- Activated platelets can no longer link through fibrinogen
- The block is reversible and fades within hours
Pharmacokinetics
- Elimination
- Mostly unchanged, about two-thirds in the urine and a quarter in the faeces; clearance falls in moderate to severe kidney impairment.
- Half-life
- About 2 hours.
- Onset and duration
- Rapid by vein; platelet aggregation returns near baseline 4 to 8 hours after stopping in most patients.
Indications
- Non-ST-elevation acute coronary syndrome, to reduce death, myocardial infarction and refractory ischaemia, usually with aspirin and heparin. Myocardial Infarction (Heart Attack) →
Adverse effects
Common
- Bleeding, the most common reaction
- Bleeding at the catheter access site
Contraindications
- Thrombocytopenia after previous tirofiban
- Active internal bleeding, bleeding tendency, major surgery or severe trauma within the previous month
- Hypersensitivity to tirofiban
Key interactions
- Heparin, aspirin, other antiplatelets, anticoagulants and thrombolytics
- Add to the risk of bleeding.
What is monitored
- Platelet count (pseudothrombocytopenia is ruled out when it falls)
- Haemoglobin and kidney function
- Access site and signs of bleeding
Administration and safety
- Intravenous loading infusion followed by continuous infusion with a pump
- The regimen is reduced in severe kidney impairment
- Stopped, together with heparin, if thrombocytopenia is confirmed or bleeding cannot be controlled
Nursing care
- Ask about earlier glycoprotein IIb/IIIa blockers, which raise the risk of thrombocytopenia
- Check platelets, haemoglobin and kidney function at baseline and during the infusion
- Watch the access site, urine, stools and neurological status for bleeding
- Keep punctures and invasive procedures to a minimum
Pregnancy and breastfeeding
Human data are limited; it is used only when clearly needed.
Test yourself
Think of the answer, then tap the question to see it.
How do tirofiban and eptifibatide differ chemically?
Tirofiban is a small non-peptide molecule; eptifibatide is a cyclic peptide. Both reversibly block glycoprotein IIb/IIIa.
What should be checked if the platelet count falls on tirofiban?
Whether it is real or pseudothrombocytopenia; if real thrombocytopenia is confirmed, tirofiban and heparin are stopped.
How quickly does platelet function recover after a tirofiban infusion?
Within hours: aggregation returns near baseline 4 to 8 hours after stopping in most patients.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - TIROFIBAN HYDROCHLORIDE injection, solution (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); 2VDM: Re-refinement of Integrin AlphaIIbBeta3 Headpiece Bound to Antagonist Tirofiban (RCSB Protein Data Bank, 2008).
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Representative model, for educational purposes only.