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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    393.5
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    96–98
  • %Excreted unchanged in urine &nbsp &nbsp :
    2–10
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    1.67
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    5–8/Unchanged

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


  • 20 to 50 &nbsp &nbsp : 60–75 mg/m2 daily
  • 10 to 20 &nbsp &nbsp : 60–75 mg/m2 daily
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 60–75 mg/m2 daily

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Unlikely to be dialysed. Dose as in
    GFR <10 mL/min
  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    Unlikely to be dialysed. Dose as in
    GFR <10 mL/min
  • HDF/high flux &nbsp :
    Unlikely to be dialysed. Dose as in
    GFR <10 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
    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

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