Anastrozole

CLINICAL USE

Treatment of breast cancer in post-
menopausal women

DOSE IN NORMAL RENAL FUNCTION

1 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
293.4

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
40

%Excreted unchanged in urine &nbsp &nbsp :

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
No data

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
40–50/Probably
unchanged

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:
Dialysed. Dose as in normal renal
function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
Dialysed. Dose as in normal renal
function

HDF/high flux &nbsp :
Dialysed. Dose as in normal renal
function

CAV/VVHD &nbsp &nbsp &nbsp:
Dialysed. Dose as in normal renal
function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Oestrogen-containing therapies: avoid

concomitant administration as would
negate pharmacological action

amoxifen: avoid concomitant

administration

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Anastrozole is extensively metabolised in

the liver; only 10% of unchanged drug and
60% of metabolites (largely inactive) are
excreted in the urine

Although renal clearance of anastrozole

decreases proportionally with creatinine
clearance, the reduction in renal clearance
does not affect total body clearance of
anastrozole. According to the American
SPC a dose reduction is not required in
renal impairment

In the UK, the SPC recommends avoiding

the use of anastrozole in patients with
GFR<20 mL/min

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