Amsacrine
Amsacrine.JPG

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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