Quick summary
Bivalirudin (Angiomax) is an FDA-approved 20-amino acid direct thrombin inhibitor derived from leech hirudin, used during PCI and in heparin-induced thrombocytopenia. Its reversible binding and 25-minute half-life provide predictable, controllable anticoagulation.
Overview
Bivalirudin is a 20-amino acid synthetic direct thrombin inhibitor (DTI) derived from hirudin, the natural anticoagulant found in medicinal leech saliva. FDA-approved under the brand name Angiomax, it is used as an anticoagulant during percutaneous coronary intervention (PCI) and in patients with or at risk for heparin-induced thrombocytopenia (HIT). Its reversible binding mechanism and short half-life allow predictable anticoagulation with rapid offset after cessation.
Mechanism of action
Bivalirudin specifically inhibits both circulating and clot-bound thrombin by bivalently binding to two distinct sites on the thrombin molecule: the catalytic active site and the anion-binding exosite 1 (fibrinogen recognition site). This dual binding differentiates bivalirudin from univalent inhibitors. Importantly, thrombin slowly cleaves bivalirudin at the Arg3-Pro4 bond, resulting in gradual recovery of thrombin activity — providing reversible inhibition proportional to drug concentration. Bivalirudin directly inhibits thrombin-catalyzed or induced reactions, including fibrin formation, coagulation factor V, VIII, and XIII activation, and platelet aggregation triggered by thrombin. The result is dose-dependent prolongation of activated clotting time (ACT), aPTT, and thrombin time.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| Percutaneous coronary intervention (PCI) | intravenous | 0.75–0.75 mg/kg | IV bolus, then infusion for duration of procedure | Bolus: 0.75 mg/kg IV. Infusion: 1.75 mg/kg/h during PCI. Post-procedure optional: 0.2 mg/kg/h for up to 20 hours. Dose adjustment required for renal impairment (GFR <30 mL/min: reduce infusion to 1 mg/kg/h). |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
The REPLACE-2 trial (n=6,010) demonstrated bivalirudin non-inferior to heparin plus GP IIb/IIIa inhibitor for composite ischemic endpoints during PCI, with significantly lower bleeding rates. The HORIZONS-AMI trial in ST-elevation MI patients showed bivalirudin reduced 30-day major bleeding by 40% versus heparin with GP IIb/IIIa inhibitors, and reduced cardiac mortality at 3 years. The EUROMAX and HEAT-PPCI trials provided additional evidence in primary PCI settings, though results varied on net clinical benefit. Meta-analyses confirm bivalirudin's consistent reduction in major bleeding with comparable ischemic outcomes versus heparin-based anticoagulation in interventional cardiology.[1][2][3][4][5]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with Bivalirudin for synergistic effects.
Legal status
FDA-approved (NDA 020873) for anticoagulation in patients undergoing PCI and in patients with or at risk of HIT/HITTS undergoing PCI. Prescription-only; administered by healthcare professionals in catheterization laboratory settings. IV infusion only.
Sourcing & access
Prescription required
Bivalirudin is an FDA-approved prescription medication available through licensed healthcare providers, telehealth platforms, and 503A/503B compounding pharmacies.
Frequently asked questions
Bivalirudin (Angiomax) is used as an anticoagulant during percutaneous coronary intervention (PCI) and for patients with or at risk of heparin-induced thrombocytopenia (HIT). It is administered intravenously in catheterization laboratory settings.
Bivalirudin directly inhibits both circulating and clot-bound thrombin by binding to two distinct sites: the catalytic active site and the anion-binding exosite 1. Thrombin slowly cleaves bivalirudin, providing reversible inhibition that wears off predictably when the infusion stops.
The HORIZONS-AMI trial showed bivalirudin reduced 30-day major bleeding by 40 percent versus heparin with GP IIb/IIIa inhibitors, with comparable ischemic outcomes. Its short half-life and predictable offset are advantages in procedural settings.
Bivalirudin has a half-life of approximately 25 minutes with normal renal function, extending to about 57 minutes in severe renal impairment. Dose adjustment is required for patients with GFR below 30 mL/min.
Research references
- Bivalirudin versus heparin with or without tirofiban in patients with acute coronary syndromes undergoing percutaneous coronary intervention (REPLACE-2 trial)PubMed
- Bivalirudin: a direct thrombin inhibitorPubMed
- Bivalirudin: pharmacology and clinical applicationsPubMed
- Safety and efficacy of bivalirudin with and without glycoprotein IIb/IIIa inhibitors in patients with acute coronary syndromes undergoing percutaneous coronary intervention (ACUITY trial)PubMed
- Bivalirudin reduces platelet and monocyte activation after elective percutaneous coronary interventionPubMed