raltitrexed

CLINICAL USE

Treatment of colorectal cancer when fluorouracil and folinic acid cannot be used

DOSE IN NORMAL RENAL FUNCTION

3 mg/m2 every 3 weeks

PHARMACOKINETICS

Molecular weight :458.5

%Protein binding :93

%Excreted unchanged in urine : 40–50

Volume of distribution (L/kg) :548 litres

half-life – normal/ESRD (hrs) :198/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

55–65 Use 75% of the dose (2.25 mg/m2) every 4 weeks25–54 Use 50% of the dose (1.5 mg/m2) every 4 weeks<25 Avoid. See ‘Other Information’

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unlikely to be dialysed. Dose as in GFR<25 mL/min.

HD :Unlikely to be dialysed. Dose as in GFR<25 mL/min.

HDF/high flux :Unknown dialysability. Dose as in GFR<25 mL/min.

CAV/VVHD :Unlikely to be dialysed. Dose as in GFR<25 mL/min.

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsFolic and folinic acid: impairs cytotoxic action

ADMINISTRATION

Reconstition

4 mL water for injection

Route

IV infusion

Rate of Administration

Over 15 minutes

Comments

Dilute in 50–250 ml sodium chloride 0.9% or glucose 5%Stable for 24 hours at 2–8°C

OTHER INFORMATION

Doses above 3 mg/m 2 have an increased incidence of life-threatening/fatal toxicityIncreased risk of treatment-related toxicity if CrCl<65 mL/minAnecdotal reports of using 30–40% of the dose every 4 weeks in patients with severe renal impairment and closely monitoring haematological parameters. Risk of severe and prolonged side effects – use if risk of not treating the patient outweighs the risk of adverse effectsNot metabolised. 40–50% is excreted unchanged in the urine and 15% of dose is excreted in the faeces over a 10-day period. Active tubular secretion may contribute to the renal excretion.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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