Arsenic trioxide

CLINICAL USE

Antineoplastic agent:
Acute promyelocytic leukaemia (APL)

DOSE IN NORMAL RENAL FUNCTION

150 mcg/kg daily until remission occurs
Consolidation: 150 mcg/kg daily for 5 days
per week for 25 doses spread over up to 5
weeks (to start 3–4 weeks after completion of
induction)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
197.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
96% bound to
haemoglobin

%Excreted unchanged in urine &nbsp &nbsp :
1–8

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
4 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
92/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Reduce dose, use with caution

10 to 20 &nbsp &nbsp : Reduce dose, use with caution

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :
Reduce dose, use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
Unknown dialysability. Dose as in
GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/
min

HDF/high flux &nbsp :
Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/
min

CAV/VVHD &nbsp &nbsp &nbsp:
Unknown dialysability. Dose as in
GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs
Use with care in combination with

other drugs known to cause QT interval
prolongation

ADMINISTRATION

Reconstition

–

Route

Rate of Administration

Over 1–4 hours

Comments

Dilute with 100–250 mL glucose 5% or

sodium chloride 0.9%

OTHER INFORMATION

Can cause QT interval prolongation and

hypokalaemia

Arsenic trioxide is under investigation

for other conditions, e.g. multiple
myeloma, acute myeloid leukaemias and
myelodysplastic syndromes

Intensive monitoring is required

Renal excretion is the main route of

elimination; can accumulate in renal
impairment

Arsenic is stored mainly in liver, kidney,

heart, lung, hair and nails. Trivalent forms
of arsenic are methylated in humans and
mostly excreted in urine. In APL patients,
daily administration of 0.15 mg/kg/day of
arsenic trioxide resulted in an approximate
4-fold increase in the urinary excretion of
arsenic after 2 to 4 weeks of continuous
dosing, when compared to baseline values

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