Amsacrine
Amsacrine
CLINICAL USE
Antineoplastic agent:
Acute leukaemias
DOSE IN NORMAL RENAL FUNCTION
Induction of remission: 90–120 mg/m
2
daily for 5–8 days, repeated at 2–4 week
intervals according to response
Maintenance: 150 mg/m
2 as a single dose
or divided over 3 consecutive days every
3–4 weeks
Or according to local policy
PHARMACOKINETICS
Molecular weight                           :
393.5
%Protein binding                           :
96–98
%Excreted unchanged in urine     :
2–10
Volume of distribution (L/kg)       :
1.67
half-life – normal/ESRD (hrs)      :
5–8/Unchanged
DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50     : 60–75 mg/m2 daily
10 to 20     : 60–75 mg/m2 daily
<10           :
60–75 mg/m2 daily
DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD                :
Unlikely to be dialysed. Dose as in
GFR <10 mL/min
HD                     :
Unlikely to be dialysed. Dose as in
GFR <10 mL/min
HDF/high flux   :
Unlikely to be dialysed. Dose as in
GFR <10 mL/min
CAV/VVHD      :
Unknown dialysability. Dose as in
GFR 10 to 20 mL/min
IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugs
None known
ADMINISTRATION
Reconstition
–
Route
IV
Rate of Administration
60–90 minutes
Comments
Dilute in 500 mL of glucose 5%
Use glass syringes
Incompatible with sodium chloride
OTHER INFORMATION
Increased risk of side effects in renal
impairment
Amsacrine is extensively metabolised in
the liver. The principal metabolites, via
microsomal oxidation, are much more
cytotoxic than the parent drug. Excretion
is via the bile; >50% excreted in faeces
within 2 hours; 35% in urine
See how to identify renal failure stages according to GFR calculation
See how to diagnose irreversible renal disease
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