Busulfan

CLINICAL USE

  • Chronic myeloid leukaemia Remission of polycythaemia vera
  • Essential thrombocythaemia and myelofibrosis
  • Conditioning before bone marrow transplantation

    DOSE IN NORMAL RENAL FUNCTION

    Oral:

  • Chronic myeloid leukaemia: 60 mcg/kg daily (maximum 4 mg daily); maintenance: 0.5–2 mg daily
  • Polycythaemia vera: 4–6 mg daily; maintenance: 2–3 mg daily
  • Myelofibrosis: 2–4 mg daily

    IV infusion

    Conditioning before bone marrow transplantation: 0.8 mg/kg every 6 hours over 4 days for 16 doses

    PHARMACOKINETICS

  • Molecular weight                           :246.3
  • %Protein binding                           :7–32
  • %Excreted unchanged in urine     : 1–2
  • Volume of distribution (L/kg)       :0.62–0.85
  • half-life – normal/ESRD (hrs)      :3/–

    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                :Unknown dialysability. Dose as in normal renal function
  • HD                     :Dialysed. Dose as in normal renal function
  • HDF/high flux   :Dialysed. Dose as in normal renal function
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: concentration increased by metronidazole
  • Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosis
  • Antifungals: metabolism inhibited by itraconazole, monitor for signs of busulfan toxicity

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral,

    IV infusion

    Rate of Administration

    Over 2 hours

    Comments

    Dilute the solution to 500 mcg/mL with sodium chloride or glucose 5%Give via a central venous catheter

    OTHER INFORMATION

  • Can cause haemorrhagic cystitis
  • Can cause an increase in creatinine and haematuria.
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