Argatroban
Argatroban
CLINICAL USE
Anticoagulant:
Prophylaxis or treatment of thrombosis
in patients with heparin-induced
thrombocytopenia (HIT)
Adjunct in patients at risk of HIT
undergoing percutaneous coronary
intervention
DOSE IN NORMAL RENAL FUNCTION
Anticoagulant for prophylaxis or
treatment of thrombosis: infusion of
2 mcg/kg/min; adjust according to
response (APTT); maximum
10 mcg/kg/min
Anticoagulant for patients undergoing
percutaneous coronary intervention:
initially a bolus of 350 mcg/kg
administered via a large bore IV line over
3–5 minutes, followed by an infusion of
25 mcg/kg/min. Additional IV bolus doses
of 150 mcg/kg may be given if required and
the infusion rate changed to
15–40 mcg/kg/min
PHARMACOKINETICS
Molecular weight :
508.6
%Protein binding :
54
%Excreted unchanged in urine :
16
Volume of distribution (L/kg) :
0.17
half-life – normal/ESRD (hrs) :
39–51 minutes/
Unchanged
DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50 : Dose as in normal renal function
10 to 20 : Dose as in normal renal function
<10 :
Dose as in normal renal function
DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD :
Unlikely to be dialysed. Dose as in
normal renal function
HD :
Not dialysed. Dose as in normal renal function
HDF/high flux :
Not dialysed. Dose as in normal renal function
CAV/VVHD :
Unlikely to be dialysed. Dose as in
normal renal function
IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugs
Heparin: avoid concomitant
administration
Urokinase: may increase the risk of
bleeding
Thrombolytics: may increase risk of
bleeding complications; enhance effect of
argatroban
Antiplatelets and anticoagulants: increased
risk of bleeding complications
ADMINISTRATION
Reconstition
–
Route
IV
Rate of Administration
Bolus: over 3–5 minutes
Infusion: 2–25 mcg/kg/min
Comments
Physically and chemically stable for up to
96 hours if refrigerated or at controlled
room temperature and protected from
light
Dilute to 1 mg/mL with sodium chloride
0.9%, glucose 5% or Lactated Ringer’s
solution, i.e. 250 mg (2.5 mL) into 250 mL
of diluent. The solution must be mixed by
inversion for 1 minute
OTHER INFORMATION
Can also be used for haemodialysis
anticoagulation: 0.1 mg/kg bolus, followed
by a continuous infusion of 0.1-0.2 mg/kg/
hour, dosing being adjusted to maintain an
APTT 1.5–3 times normal.
For CVVHD a dose of 0.5–1 mcg/kg/min
was suggested, dosing being adjusted to
maintain an APTT 1.5–2 times normal.
20% of argatroban is removed during a
4 hour dialysis session
There is no specific antidote
Contraindicated in patients with overt
major bleeding
See how to identify renal failure stages according to GFR calculation
See how to diagnose irreversible renal disease
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