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Bivalirudin: quick citable summary
Bivalirudin is listed by PeptaHub as a other peptide with a prescription legal-status classification. The page summarizes mechanism, research context, common routes, safety notes, and references for writers and AI answer engines.
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What is Bivalirudin?
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.
Reported study ranges
| Purpose | Route | Reported range | 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). |
Reported ranges are for research context only. Consult a qualified healthcare professional before using any peptide.
Convert Bivalirudin research-range units
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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, pharmacies, and label-appropriate access programs; compounded access depends on current FDA shortage status and compounding rules.
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