ANGIOMAX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANGIOMAX (ANGIOMAX).
Direct thrombin inhibitor that reversibly binds to the active site of thrombin, blocking its interaction with substrates, thereby inhibiting fibrin formation and activation of coagulation factors V, VIII, and XIII.
| Metabolism | Primarily degraded by hydrolysis and proteolytic cleavage; not metabolized by cytochrome P450 enzymes; some proteolytic cleavage by thrombin; elimination half-life ~25 minutes. |
| Excretion | Renal: ~90% unchanged; biliary/fecal: negligible (<1%) |
| Half-life | Terminal elimination half-life: 25-30 minutes in patients with normal renal function; increased to 2-3 hours in dialysis-dependent patients |
| Protein binding | ~20% bound to α2-macroglobulin and other plasma proteins |
| Volume of Distribution | 0.2 L/kg (primarily intravascular, minimal tissue distribution) |
| Bioavailability | Intravenous: 100% (not administered via other routes) |
| Onset of Action | Intravenous: Immediate (anticoagulant effect within 5 minutes) |
| Duration of Action | Intravenous: 2-4 hours after infusion cessation; anticoagulant effect monitored via ACT |
1 mg/kg intravenous bolus followed by 0.1 mg/kg/hour continuous intravenous infusion for duration of procedure; alternatively, 0.75 mg/kg intravenous bolus followed by 1.75 mg/kg/hour continuous intravenous infusion for up to 4 hours during percutaneous coronary intervention.
| Dosage form | INJECTABLE |
| Renal impairment | For patients with severe renal impairment (CrCl <30 mL/min), reduce infusion dose to 0.1 mg/kg/hour. For patients on hemodialysis, reduce infusion dose to 0.1 mg/kg/hour with no bolus dose. No specific recommendation for moderate impairment (CrCl 30-59 mL/min); use with caution. |
| Liver impairment | No dose adjustment required for mild hepatic impairment (Child-Pugh Class A). For moderate (Child-Pugh Class B) or severe (Child-Pugh Class C) impairment, no specific studies; use with caution. |
| Pediatric use | Safety and effectiveness in pediatric patients (<18 years) have not been established; no specific dosing guidelines available. |
| Geriatric use | Elderly patients may have increased bleeding risk due to age-related changes in renal function; monitor renal function and adjust dose accordingly. No specific geriatric dose adjustment aside from renal adjustment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANGIOMAX (ANGIOMAX).
| Breastfeeding | It is unknown whether bivalirudin is excreted in human milk. No M/P ratio is available. Because many drugs are excreted in human milk and because of the potential for adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Teratogenic Risk | ANGIOMAX (bivalirudin) is a direct thrombin inhibitor. There are no adequate and well-controlled studies in pregnant women. In animal studies, bivalirudin did not demonstrate teratogenicity in rats or rabbits at doses up to 10.8 mg/kg/day (approximately 1.5 times the human dose of 0.75 mg/kg based on body surface area). However, bleeding risk exists for both mother and fetus. Use during pregnancy only if clearly needed and potential benefit justifies risk to fetus. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Active major bleeding","Hypersensitivity to bivalirudin or any component of the formulation","Patients with heparin-induced thrombocytopenia (HIT) or heparin-induced thrombocytopenia with thrombosis syndrome (HITTS) when used for PCI (relative contraindication depending on context)"]
| Precautions | ["Hemorrhage risk: major bleeding events, including intracranial and retroperitoneal bleeding","Hepatic impairment: dose adjustment required in moderate to severe hepatic impairment","Renal impairment: clearance reduced in severe renal impairment","Hypersensitivity reactions (rare)","No reversal agent available"] |
| Food/Dietary | No known food interactions with bivalirudin. However, patients should avoid alcohol due to increased bleeding risk. Maintain a balanced diet; no specific dietary restrictions required. |
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| Fetal Monitoring | Monitor activated clotting time (ACT) during infusion to maintain therapeutic anticoagulation. Monitor for signs of bleeding in both mother and fetus. For pregnant patients, consider fetal heart rate monitoring as clinically indicated. Assess hemoglobin/hematocrit for occult bleeding. |
| Fertility Effects | No specific studies on fertility in humans. In animal studies, no impairment of fertility was observed in rats at doses up to 10.8 mg/kg/day (approximately 1.5 times the human dose). Effects on human fertility are unknown. |
| Clinical Pearls | ANGIOMAX (bivalirudin) is a direct thrombin inhibitor used in patients undergoing percutaneous coronary intervention (PCI) and for heparin-induced thrombocytopenia (HIT). Monitor activated clotting time (ACT) to guide dosing; target ACT >300 seconds during PCI. No reversal agent exists; if bleeding occurs, consider hemodialysis or recombinant factor VIIa. Use with caution in renal impairment (CrCl <30 mL/min) as 80% of drug is cleared renally. Do not administer intramuscularly. Infusion rate adjustments may be needed in renal dysfunction. |
| Patient Advice | This medication prevents blood clots during heart procedures. It increases bleeding risk; watch for unusual bruising, blood in urine or stool, or bleeding that won't stop. · Avoid aspirin, NSAIDs (ibuprofen, naproxen), and other blood thinners unless prescribed by your doctor, as they increase bleeding risk. · Inform all healthcare providers you are taking this medication before any surgery or dental procedure. · Report any signs of severe allergic reaction: rash, hives, difficulty breathing, or swelling of face/mouth. · This drug has no reversal agent; seek immediate medical attention for any head injury or fall. |