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argatroban (Novastan)

Indications: 1) heparin-induced thrombocytopenia (FDA approved 2000) 2) anticoagulant for prevention of thrombosis in patients with or at risk for heparin-induced thrombocytopenia undergoing percutaneous coronary intervention (PCI) (FDA approved 2002) 3) treatment of deep vein thrombosis in patients with heparin-induced thrombocytopenia [1] Dosage: (administration) 1) given intravenously as continuous infusion 2) heparin-induced thrombocytopenia: - adult patients without hepatic impairment is 2 ug/kg/min 3) PCI in HIT/HITTS patients a) bolus of 350 mcg/kg over 3-5 minutes via large bore IV b) then 25 ug/kg/min infusion ,Available in 250-mg (in 2.5-mL) single-use amber vials. Inert ingredients: 750 mg D-sorbitol, 1,000 mg dehydrated alcohol. Dilute contents 100-fold, i.e. each 2.5-mL vial should be diluted by mixing with 250 mL of diluent, pH of intravenous solution prepared as recommended is 3.2 to 7.5 Store the vials in original cartons at room temperature Pharmacokinetics: - metabolized in the liver - protein-binding 54% - 1/2 life of about 50 minutes Laboratory: 1) heparin-induced thrombocytopenia: - monitor aPTT - steady-state levels within 1-3 hours following initiation of argatroban 2) PCI in HIT/HITTS patients a) activated clotting time (ACT), 300-450 sec is therapeutic b) should be checked 5-10 minutes after the bolus dose c) procedure may proceed if the ACT is > 300 seconds d) if the ACT is < 300 seconds, an additional IV bolus dose of 150 ug/kg should be administered, the infusion dose increased to 30 ug/kg/min, & the ACT checked 5-10 minutes later (see Table 9) e) if the ACT is > 450 seconds, the infusion rate should be decreased to 15 ug/kg/min, & the ACT checked 5-10 minutes later f) maintain infusion rate throughout procedure if ACT is therapeutic 3) argatroban in plasma Mechanism of action: - direct thrombin antagonist Notes: Manufactured by GlaxoSmithKline

Interactions

drug interactions drug adverse effects of antithrombotic agent(s)

Related

heparin-induced thrombocytopenia; heparin-associated antibody syndrome (HIT)

General

thrombin inhibitor

Properties

INHIBITS: carbonic anhydrase (dehydratase)

Database Correlations

PUBCHEM correlations

References

  1. Medical Knowledge Self Assessment Program (MKSAP) 11, 17. American College of Physicians, Philadelphia 1998, 2015
  2. Prescriber's Letter 8(2):supplement 2001
  3. Di Nisio M et al Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40 PMID: 16148288