BIVALIRUDIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BIVALIRUDIN (BIVALIRUDIN).
Bivalirudin is a direct thrombin inhibitor that binds reversibly to the active site of both free and clot-bound thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin and activation of factors V, VIII, and XIII.
| Metabolism | Bivalirudin is metabolized via proteolytic cleavage and undergoes renal excretion; not metabolized by cytochrome P450 enzymes. |
| Excretion | Renal: 20% unchanged; proteolytic cleavage (hepatic and other sites) accounts for the remainder. |
| Half-life | 25 minutes (in patients with normal renal function); prolonged to ~57 minutes in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | ~34% bound to human serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.17 L/kg, predominantly confined to intravascular space. |
| Bioavailability | Intravenous: 100% (only parenteral route available). |
| Onset of Action | Intravenous: Immediate (within minutes) due to direct thrombin inhibition. |
| Duration of Action | Approximately 1 hour after infusion discontinuation; clinical effect correlates with aPTT prolongation. |
Initial intravenous bolus of 0.75 mg/kg, followed by continuous intravenous infusion at 1.75 mg/kg/hour for the duration of the procedure.
| Dosage form | INJECTABLE |
| Renal impairment | In patients with severe renal impairment (CrCl <30 mL/min) or on hemodialysis, reduce infusion rate to 1.0 mg/kg/hour; no adjustment needed for CrCl ≥30 mL/min. |
| Liver impairment | No specific dose adjustment required for hepatic impairment; use with caution in severe hepatic dysfunction. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; monitor renal function as elderly patients may have reduced renal clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BIVALIRUDIN (BIVALIRUDIN).
| Breastfeeding | Unknown if excreted in human breast milk; molecular weight (2.18 kDa) suggests possible minimal excretion. M/P ratio not established. Risk to infant likely low due to poor oral bioavailability. Caution recommended, especially in preterm or ill infants. |
| Teratogenic Risk | Pregnancy category unknown; no adequate human studies. In animal reproduction studies, no evidence of fetal harm was observed at doses up to 16 times the human AUC. However, because bivalirudin does not cross the placenta significantly (molecular weight ~2 kDa, low lipid solubility), the risk of teratogenicity is considered low. Potential for maternal hemorrhage during delivery exists due to anticoagulant effect. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Active major bleeding","Hypersensitivity to bivalirudin or any component of the product"]
| Precautions | ["Bleeding risk: major hemorrhage, intracranial bleeding, retroperitoneal bleeding","Thrombotic events with abrupt discontinuation","Renal impairment: dose adjustment required in severe renal impairment (CrCl < 30 mL/min) and dialysis-dependent patients","Risk of anaphylaxis or allergic reactions","Formation of antibodies to bivalirudin (non-neutralizing)"] |
| Food/Dietary | No specific food interactions with bivalirudin. However, because bivalirudin increases bleeding risk, avoid alcohol and high-dose fish oil supplements (which may also affect clotting) unless discussed with a healthcare provider. |
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| Fetal Monitoring | Monitor activated clotting time (ACT) or activated partial thromboplastin time (aPTT) during infusion. Assess maternal signs of bleeding (e.g., hematuria, ecchymosis). Fetal monitoring for signs of distress or hemorrhage is recommended if used near delivery. Baseline and periodic complete blood count (CBC) including platelets. |
| Fertility Effects | No human data on fertility effects. In animal studies, no adverse effects on fertility or reproductive performance were observed at up to 16 times the human AUC. |
| Clinical Pearls | Bivalirudin is a direct thrombin inhibitor used primarily in percutaneous coronary intervention (PCI) and for heparin-induced thrombocytopenia (HIT). It has a short half-life (25 min) and is renally cleared; dose adjustment is required for severe renal impairment. Monitor ACT (activated clotting time) during PCI to maintain target range. Reversal agent is not available; consider hemodialysis for overdose. Avoid intramuscular injection due to risk of hematoma. |
| Patient Advice | This medication prevents blood clots and is given intravenously during procedures like angioplasty. · You will be monitored closely for signs of bleeding, such as easy bruising, blood in urine or stool, or prolonged bleeding from cuts. · Report any unusual bleeding, especially from surgical sites or injection areas, to your healthcare team immediately. · Avoid taking aspirin, ibuprofen, or other blood thinners unless prescribed by your doctor, as they may increase bleeding risk. · Tell your doctor if you have kidney problems, as the dose may need to be adjusted. |