Capecitabine

CLINICAL USE

Antineoplastic agent (antimetabolite):

Colorectal, colon and breast cancer

DOSE IN NORMAL RENAL FUNCTION

1.25 g/m2 twice daily for 14 days, repeated after 7 days

PHARMACOKINETICS

Molecular weight :359.4

%Protein binding :54

%Excreted unchanged in urine : 3

Volume of distribution (L/kg) :No data

half-life – normal/ESRD (hrs) :0.85/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

30–50 75% of dose (950 mg/m2 twice daily) use with care10–30 Avoid

<10 : Avoid

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in GFR <10 mL/min

HD :Unlikely to be dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD :Unknown dialysability. Dose as in GFR=10–30 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Allopurinol: avoid concomitant use

Anticoagulants: possibly enhances effect of coumarins

Anti-epileptics: reported toxicity with phenytoin, due to increased phenytoin levels

Antipsychotics: avoid concomitant use with clozapine – increased risk of agranulocytosis

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

–

Comments

Give after food

OTHER INFORMATION

Capecitabine is a prodrug that is metabolised to fluorouracil

Contraindicated in severe renal impairment due to increased incidence of grade 3 or 4 adverse reactions in patients with GFR of 30–50 mL/min

Extensive absorption (~70%) after food intake.

First metabolised in the liver and then in the tumour. Up to 96% dose is recovered in the urine. Terminal T½ = 0.85 hours

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