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.