Pharmacology · Parenteral direct thrombin inhibitors
Bivalirudin !
An intravenous peptide that blocks thrombin directly during coronary angioplasty. Its effect fades about an hour after the infusion stops.
Updated 2026-11-01
The figure shows human thrombin with bivalirudin; bivalirudin is a peptide chain in the crystal, so no small-molecule ligand is marked.
Mechanism of action
Bivalirudin is a synthetic 20-amino-acid peptide. One end fits the active site of thrombin and the other end the anion-binding exosite where fibrinogen docks, so it blocks free and clot-bound thrombin. The block is reversible: thrombin slowly cuts the peptide and recovers its activity.
- Bivalirudin binds thrombin's active site and its fibrinogen exosite
- Free and clot-bound thrombin are blocked without antithrombin
- Thrombin slowly cleaves it, so the block wears off
Pharmacokinetics
- Metabolism
- Broken down by proteolytic cleavage.
- Elimination
- Kidneys and proteolysis; clearance falls in moderate or severe kidney impairment and much more in dialysis patients. It is partly removed by haemodialysis.
- Half-life
- About 25 minutes with normal kidney function; longer in kidney impairment.
- Onset and duration
- Immediate by vein; coagulation times return to baseline about 1 hour after stopping.
Indications
- Anticoagulation during percutaneous coronary intervention, including in patients with heparin-induced thrombocytopenia. Heparin-induced thrombocytopenia →
- PCI in acute myocardial infarction, including STEMI. Myocardial Infarction (Heart Attack) →
Adverse effects
Common
- Bleeding, the most common reaction
Contraindications
- Active major bleeding
- Hypersensitivity to bivalirudin
Key interactions
- Heparin, warfarin, thrombolytics or glycoprotein IIb/IIIa inhibitors
- Increase the risk of major bleeding.
What is monitored
- Activated clotting time (ACT) during the procedure
- Kidney function, which sets the infusion regimen
- Access site, haemoglobin and signs of bleeding after the procedure
Administration and safety
- Intravenous bolus followed by continuous infusion, after reconstitution and dilution of the powder
- The reconstituted solution is clear to slightly opalescent and is not frozen
- The infusion is reduced in kidney impairment; overdoses have happened when this was missed, including in haemodialysis
- No specific antidote; its short half-life is the main safety margin
Nursing care
- Check kidney function and weight before the procedure
- Watch the arterial access site, haemoglobin and blood pressure after PCI
- Report chest pain after a STEMI procedure: possible acute stent thrombosis
- Record the ACT values and infusion changes
Pregnancy and breastfeeding
There are no human data in pregnancy; it is used only when the benefit justifies the risk.
Test yourself
Think of the answer, then tap the question to see it.
Which two sites of thrombin does bivalirudin bind?
The catalytic (active) site and the anion-binding exosite where fibrinogen docks.
How is bivalirudin followed during PCI?
With the activated clotting time (ACT).
Why must the bivalirudin infusion be adjusted in kidney impairment?
It is partly cleared by the kidneys; its clearance falls and its half-life lengthens, and overdoses have occurred when the infusion was not reduced.
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 - BIVALIRUDIN injection, powder, lyophilized, for solution (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); 3VXE: Human alpha-thrombin-Bivalirudin complex at PD5.0 (RCSB Protein Data Bank, 2013).
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Representative model, for educational purposes only.