imatinib

CLINICAL USE

Antineoplastic agent

DOSE IN NORMAL RENAL FUNCTION

400–600 mg daily, increasing to a maximum of 400 mg twice daily

PHARMACOKINETICS

Molecular weight :589.7 (as mesilate)

%Protein binding :95

%Excreted unchanged in urine : 5

Volume of distribution (L/kg) :No data

half-life – normal/ESRD (hrs) :18/Unknown

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function. See ‘Other Information’

<10 : Dose as in normal renal function. See ‘Other Information’

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

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

HDF/high flux :Unlikely to be dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antibacterials: concentration reduced by rifampicin – avoid concomitant use

Anticoagulants: enhanced anticoagulant effect of warfarin

Antidepressants: concentration reduced by St Johns wort

Anti-epileptics: concentration reduced by phenytoin – avoid concomitant use; absorption of phenytoin possibly reduced

Antipsychotics: avoid concomitant use with clozapine, (increased risk of agranulocytosis)

Ciclosporin: may increase ciclosporin levels

Tacrolimus: may increase tacrolimus levels

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Associated with oedema and superficial fluid retention in 50–70% cases. Probability is increased in patients receiving higher doses, age >65 years, and those with a prior history of cardiac disease. Severe fluid retention (e.g. pleural effusion, pericardial effusion, pulmonary oedema and ascites) has been reported in up to 16% of patients. Can be managed by diuretic therapy, and dose reduction or interruption of imatinib therapySevere elevation of serum creatinine has been observed in approximately 1% of patientsOral bioavailability is 98% Main circulating metabolite is N-demethylated piperazine derivative, and has similar potency to the parent compound. Catalysed by cytochrome P450 CYP3A4. Mainly hepatically metabolised with 68% excreted in faeces and 13% in urine in 7 days. Half-life is 40 hours in normal renal function.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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