Anticoagulant · Direct thrombin inhibitor

Bivalirudin (Angiomax)

Also called Angiomax

Reviewed by Alex G, BSN, RN, CEN, CCRN, CMC, NREMT-P · From the Reference tab of the app

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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

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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 your local protocols and medical direction.