Rx Update: December 2002

Argatroban and Bivalirudin

Mary Ross, R.Ph., M.B.A., Joan Murhammer, R.Ph., Kevin Bebout, R. Ph.
First Published: December 2002
Peer Review Status: Internally Reviewed


Argatroban

Argatroban (GlaxoSmithKline) is an anticoagulant indicated for the prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). Argatroban is a synthetic, reversible direct inhibitor of thrombin.

The primary adverse effect of argatroban therapy is hemorrhage. Other adverse effects that have been reported include allergic reactions, dyspnea, hypotension, fever, diarrhea, sepsis, cardiac arrest, and nausea. All other parenteral anticoagulants should be discontinued before argatroban is initiated; the drug is contraindicated in patients with overt major bleeding.

Argatroban is administered as a continuous intravenous infusion. The recommended initial adult dose is 2 mcg/Kg/minute. The dosage can be titrated as clinically indicated to a target aPTT of 1.5 to 3 times the initial baseline value (not to exceed 100 seconds). The recommended maximum infusion rate of argatroban is 10 mcg/Kg/minute. The initial dose needs to be reduced to 0.5 mcg/Kg/minute in patients with moderate liver impairment. The dose does not need to be adjusted in patents with renal impairment.

Argatroban injection is available as a 100 mg/ml, 2.5 ml vial. The vial is further diluted to 1 mg/ml with a compatible diluent (NS, D5W, LR) prior to administration.

At UIHC, argatroban is restricted to prescribing by Cardiac Catheterization Laboratory and Adult and Pediatric Hematology/Oncology staff physicians.

Bivalirudin

Bivalirudin (Angiomax® - The Medicines Company) is a specific and reversible direct thrombin inhibitor indicated for use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA) as an alternative to heparin therapy. It is indicated for use with aspirin.

Bivalirudin is contraindicated in patients with active major bleeding. The most common adverse effects reported in patients treated with bivalirudin therapy include back pain, nausea, pain, headache, injection site pain, insomnia, and hypotension. Major bleeding occurs in 3.7% of patients.

The recommended dose of bivalirudin is an initial bolus dose of 1 mg/Kg intravenous followed by a 4-hour intravenous infusion at a rate of 2.5 mg/Kg/hour. Bivalirudin may be continued for an additional 20 hours at a rate of 0.2 mg/Kg/hour, if needed. Bivalirudin should be initiated just prior to PTCA with concurrent aspirin (300 to 325 mg daily). Dose reductions may be required in patients with renal impairment. Anticoagulation status of the patient should be closely monitored.

Bivalirudin injection is available as a 250 mg vial of powder for reconstitution. Once reconstituted with sterile water, the injection is further diluted to 5 mg/ml with D5W or NS for the initial bolus and 4-hour infusion; for the subsequent low-rate infusion, a lower concentration of 0.5 mg/ml should be used.

At UIHC, bivalirudin is restricted to prescribing by Cardiac Catheterization Laboratory and Adult and Pediatric Hematology/Oncology staff physicians.

 

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