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

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :
    Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Not dialysed. Dose as in normal renal function

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

    IMPORTANT DRUG INTERACTIONS

  • Potentially hazardous interactions with other drugs
  • Avoid concurrent administration with

    pimozide or St John’s wort

  • Oestrogens and progestogens: may cause

    contraceptive failure

    ADMINISTRATION


    Reconstition



    Route


    Oral

    Rate of Administration



    Comments



    OTHER INFORMATION


    Less than 0.2% of a dose is recovered in

    dialysate after haemodialysis