Lomustine

CLINICAL USE


Treatment of Hodgkin’s disease and certain solid tumours

DOSE IN NORMAL RENAL FUNCTION

120–130 mg/m2 every 6–8 weeks if used alone; lower dose is used in combination treatment and compromised bone marrow function

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :233.7
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :60
  • %Excreted unchanged in urine &nbsp &nbsp : 50 (as metabolites)

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :No data

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :16–48 (metabolites)

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    45–60 75% of dose30–45 50–70% of dose<30 Not recommended.

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Avoid

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Avoid.
  • HDF/high flux &nbsp :Unknown dialysability. Avoid. See ‘Other Information’
  • CAV/VVHD &nbsp &nbsp &nbsp:Unlikely to be dialysed. Avoid. See ‘Other Information’

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • None known

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Bone marrow toxicity is delayed Relatively rapid and complete oral absorption, followed by first pass metabolism. Part of lomustine metabolism is mediated through hepatic microsomal enzymes. Metabolites predominantly excreted by kidneys; 10% excreted as CO2 and < 5% in faeces
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