Alteplase
Alteplase
CLINICAL USE
Fibrinolytic drug:
Acute myocardial infarction
Pulmonary embolism
Acute ischaemic stroke
To unblock dialysis lines (unlicensed
indication)
DOSE IN NORMAL RENAL FUNCTION
Myocardial infarction: accelerated
regimen (initiated within 6 hours) 15 mg
IV bolus, 50 mg over 30 minutes, then
35 mg over 1 hour (total dose 100 mg); or
(if initiated within 6–12 hours) 10 mg over
1–2 minutes followed by IV infusion of
50 mg over 1 hour, then 4 infusions each
of 10 mg over 30 minutes (total dose –
100 mg over 3 hours)
Pulmonary embolism: 10 mg by IV
injection over 1–2 minutes, followed by an
infusion of 90 mg over 2 hours. Total dose
should not exceed 1.5 mg/kg in patients
who weigh <65 kg
Acute ischaemic stroke: 0.9 mg/kg over
60 minutes, 10% of dose as initial bolus;
maximum 90 mg. Start within 3 hours of
symptoms
PHARMACOKINETICS
Molecular weight :
65 000 (non-
glycosylated protein)
%Protein binding :
No data
%Excreted unchanged in urine :
Minimal
Volume of distribution (L/kg) :
0.1
half-life – normal/ESRD (hrs) :
α: 4–5 minutes; β:
40 minutes
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 :
Not dialysed. Dose as in normal renal function
HD :
Not dialysed. Dose as in normal renal function
HDF/high flux :
Unknown dialysability. Dose as in
normal renal function
CAV/VVHD :
Not dialysed. Dose as in normal renal function
IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugs
Risk of haemorrhage can be increased by
the use of coumarin derivatives, platelet
aggregation inhibitors, heparin, and other
agents influencing coagulation
ADMINISTRATION
Reconstition
50 mg vial: dissolve in 50 mL water for
injection
20 mg vial: dissolve in 20 mL water for
injection.
The reconstituted solutions can be further
diluted (minimum concentration 0.2 mg/
mL) with sterile sodium chloride 0.9%
Route
IV
Rate of Administration
See under dose
Comments
Water or glucose solution must NOT be
used for dilution
50 mg vial = 29 mega units/vial
20 mg vial = 11.6 mega units/vial
OTHER INFORMATION
Patients weighing less than 65 kg should
receive a total dose of 1.5 mg/kg according
to dose schedule
Allergic reactions are less likely with
alteplase than streptokinase and repeated
administration is possible
1.7 g arginine in the 50 mg vial, 0.7 g
arginine in 20 mg vial – may lead to
hyperkalaemia in renal failure
Pay attention to potential bleeding sites
during treatment
To unblock dialysis lines, use 2 mg in 2 mL
down each lumen and leave in situ for at
least 60 minutes or until the next dialysis
session
Alternative regimens for unblocking
dialysis lines: an infusion of 20 mg over
20 hours, or 50 mg over 12 hours
See how to identify renal failure stages according to GFR calculation
See how to diagnose irreversible renal disease
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