CLINICAL USE

Anti-emetic: Cancer chemotherapy Postoperative nausea and vomiting (PONV)

DOSE IN NORMAL RENAL FUNCTION

Chemotherapy: IV bolus or infusion of 5 mg before chemotherapy, then 5 mg every morning orally for 5 days PONV: IV bolus or infusion of 2 mg before induction of anaesthesia, then 2 mg within 2 hours of the end of surgery

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 284.4 (320.8 as hydrochloride)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 71
  • %Excreted unchanged in urine &nbsp &nbsp : 8 (70% as metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 400–600 litres
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 8–45 (depends on metaboliser status)/ Increased

    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: Unlikely to be dialysed. Dose as in normal renal function

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Unlikely to be dialysed. Dose as in normal renal function
  • HDF/high flux &nbsp : Unknown dialysability. Dose as in normal renal function
  • CAV/VVHD &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Anti-arrhythmics: increased risk of ventricular arrhythmias – use with caution; avoid with amiodarone, disopyramide, flecainide, lidocaine, mexiletine, procainamide or propafenone
  • Beta-blockers: increased risk of ventricular arrhythmias – use with caution; avoid with sotalol

    ADMINISTRATION

    Reconstition

    Route

    Oral, IV bolus,

    IV infusion

    Rate of Administration

    Bolus: over at least 1 minute Infusion: over 15 minutes

    Comments

    Can be added to 100 mL sodium chloride 0.9%, glucose 5% or Ringer’s solution Give oral preparation at least an hour before food

    OTHER INFORMATION

    In impaired kidney function, plasma concentrations of tropisetron may be increased by up to 50%, but no problem with short courses .