Aprepitant

CLINICAL USE

  • Prevention of acute and delayed nausea
    and vomiting associated with moderate and
    highly emetogenic cancer chemotherapy

    DOSE IN NORMAL RENAL FUNCTION

    125 mg once daily on day 1 followed by 80 mg
    once daily on days 2 and 3

    PHARMACOKINETICS

  • Molecular weight                           :
    534.4
  • %Protein binding                           :
    >95
  • %Excreted unchanged in urine     :
    0
  • Volume of distribution (L/kg)       :
    66 litres
  • half-life – normal/ESRD (hrs)      :
    9–13/Unchanged

    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                :
    Not dialysed. Dose as in normal renal function
  • HD                     :
    Not dialysed. Dose as in normal renal function
  • HDF/high flux   :
    Unlikely to be dialysed. Dose as in
    normal renal function
  • CAV/VVHD      :
    Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

  • Potentially hazardous interactions with other drugs
  • Avoid concurrent administration withpimozide or St John’s wort
  • Oestrogens and progestogens: may causecontraceptive failure

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Less than 0.2% of a dose is recovered in

    dialysate after haemodialysis

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