Tropisetron.txt

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

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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 .

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