Anticoagulant · Direct thrombin inhibitor
Bivalirudin (Angiomax)
Also called Angiomax
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Heparin vs Warfarin: aPTT vs INR, HIT, Bridging, Antidotes and DOAC Reversal
Indications
- Anticoagulation during PCI, including primary PCI for STEMI
- PCI in patients with HIT or HIT with thrombosis
- HIT in the ICU, especially with liver dysfunction (off-label)
- ECMO and ventricular assist device anticoagulation, often for HIT or heparin resistance (off-label)
- Cardiac surgery on bypass in acute HIT when surgery cannot wait (off-label)
Dosing
Bivalirudin drip card and mL/h converterStart: HIT: 0.15 mg/kg/h, lower in kidney failure (no bolus). PCI: 0.75 mg/kg bolus, then 1.75 mg/kg/h
| Where | Dose |
|---|---|
| Other ICU drugs | Bivalirudin: Reduce; argatroban needs no kidney adjustment |
Mechanism of action
Bivalirudin is a synthetic 20-amino-acid analog of hirudin, the 65-amino-acid anticoagulant of the medicinal leech. It binds thrombin at two sites: its D-Phe-Pro-Arg-Pro head occupies the catalytic site and its hirudin-derived tail grips exosite 1, the fibrinogen-binding site, so it blocks free and clot-bound thrombin without antithrombin. Thrombin slowly cuts the Arg3–Pro4 bond, which frees the enzyme and makes the inhibition transient. It does not bind PF4, so HIT antibodies do not recognize it.
Pharmacology
- Hematologic: dose-dependent rise in ACT, aPTT, PT/INR and thrombin time, back to baseline about 1 h after stopping
- Hematologic: blocks thrombin-induced platelet activation; its modest INR rise can mislead during warfarin overlap (label)
- Hematologic: in stagnant blood (venous reservoirs, pericardial blood, cell savers, low-flow parts of a circuit) thrombin breaks the drug down and clot can form
- Renal: about 20% renal clearance, so infusions (not boluses) are reduced in kidney failure
Pharmacokinetics
| Onset | Immediate IV |
|---|---|
| Duration | Coagulation times normalize about 1 h after stopping; longer in kidney failure |
| Half-life | 25 min with normal kidneys; 34–57 min in moderate to severe impairment; 3.5 h on dialysis |
| Distribution | Vd about 0.2 L/kg (extracellular fluid) |
| Protein binding | None apart from thrombin; does not bind red cells |
| Metabolism | Proteolysis, partly by thrombin itself |
| Clearance | 3.4 mL/kg/min; 21% lower in moderate to severe kidney impairment, 70% lower on dialysis |
| Elimination | About 20% by the kidneys (filtration with tubular handling); the rest broken down to amino acids |
| Dialysis | About 25% removed by hemodialysis |
Chemistry
- Hirulog: D-Phe-Pro-Arg-Pro, four glycines, then a 12-residue segment copied from hirudin's C-terminus (residues 53–64); MW 2,180 Da
- Made by chemical synthesis; residue 1 is D-phenylalanine, a non-natural isomer, and all other chiral residues are L
- Supplied as the trifluoroacetate salt: 250 mg lyophilized with 125 mg mannitol and sodium hydroxide, pH 5–6 after reconstitution with 5 mL water; diluted to 5 mg/mL in D5W or NS, stable 24 h at room temperature
- Ready-to-use 5 mg/mL vials (polyethylene glycol, acetate) are refrigerated. A polar peptide, it is not absorbed orally and stays extracellular
Adverse effects and cautions
In the one-pagers
- Bleeding, Reversal, HIT and DICHeparin-induced thrombocytopenia (HIT): Start a non-heparin anticoagulant at once: argatroban (liver-cleared; good in kidney failure) or bivalirudin; fondaparinux or a DOAC when stable
- ACS and STEMIInitial medications: Heparin (UFH): PCI: 70-100 units/kg to ACT; lytic: 60 units/kg (max 4,000): Or bivalirudin, enoxaparin
- ECMO EssentialsMonitoring and anticoagulation: UFH is usual; bivalirudin or argatroban if HIT. High free Hb, bilirubin or lipids falsely lower anti-Xa. Follow your institution's protocols.
- LVAD BasicsComplications: Pump thrombosis: Rising power, high LDH and free Hgb, dark urine: IV heparin or bivalirudin; pump exchange if refractory
- Impella Heart PumpPurge system: HIT: stop all heparin, purge included. Use a bicarbonate-dextrose purge and IV argatroban or bivalirudin, per your institution's or agency's protocols.
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Sources
- FDA label: Bivalirudin, Sandoz (2019)
- FDA label: Bivalirudin ready-to-use, MAIA (2024)
- Garcia, ACCP Parenteral Anticoagulants (Chest 2012)
For education and exam preparation only. Follow your institution’s protocols. Typical adult values for study. Follow the order, the label and your institution's protocols.