PMS-FLUTAMIDE TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

FLUTAMIDE

Available from:

PHARMASCIENCE INC

ATC code:

L02BB01

INN (International Name):

FLUTAMIDE

Dosage:

250MG

Pharmaceutical form:

TABLET

Composition:

FLUTAMIDE 250MG

Administration route:

ORAL

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

ANTINEOPLASTIC AGENTS

Product summary:

Active ingredient group (AIG) number: 0116869001; AHFS:

Authorization status:

APPROVED

Authorization date:

1996-11-25

Summary of Product characteristics

_ _
_pms-FLUTAMIDE Product Monograph _
_Page 1 of 31_
PRODUCT MONOGRAPH
PR
PMS-FLUTAMIDE
Flutamide Tablets
250 mg
Non-steroidal antiandrogen
PHARMASCIENCE INC.
6111 Royalmount Ave., Suite 100
Montréal, Québec
H4P 2T4
SUBMISSION CONTROL NO
: 158262
Date of Revision:
December 18, 2012
_ _
_pms-FLUTAMIDE Product Monograph _
_Page 2 of 31_
PRODUCT MONOGRAPH
NAME OF DRUG
pr
pms-FLUTAMIDE
Flutamide Tablets
250 mg
THERAPEUTIC CLASSIFICATION
Non-steroidal antiandrogen
ACTION AND CLINICAL PHARMACOLOGY
Flutamide demonstrates potent antiandrogenic effects by inhibiting
androgen uptake and/or
inhibiting nuclear binding of androgen in target tissues. In adult
male rats, ventral prostate
weights
and
seminal
vesicle
weights
were
markedly
reduced
by
daily
administration
of
flutamide.
PHARMACOKINETICS
Analysis of plasma, urine, and feces following a single oral 200 mg
dose of tritium-labelled
flutamide to human volunteers showed that the drug is rapidly and
completely absorbed. It is
excreted mainly in the urine with 4.2% of the dose excreted in the
faeces over 72 hours. The
composition
of
plasma
radioactivity
showed
that
flutamide
is
rapidly
and
extensively
metabolized, with flutamide comprising only 2.5% of plasma
radioactivity one hour after
administration. At least six metabolites have been identified in
plasma. The major plasma
metabolite is a biologically active alpha-hydroxylated derivative
which accounts for 23% of the
plasma tritium one hour after drug administration.
The major urinary metabolite is
2-amino-5-nitro-4-(trifluoromethyl)phenol.
_ _
_pms-FLUTAMIDE Product Monograph _
_Page 3 of 31_
Following a single 250 mg oral dose to normal adult volunteers, low
plasma levels of varying
amounts of flutamide were detected. The biologically active
alpha-hydroxylated metabolite
reaches maximum plasma levels in about two hours, indicating that it
is rapidly formed from
flutamide. The plasma half-life for this metabolite is about 6 hours.
Following multiple oral dosing of 250 mg three times a day in normal
geriatric voluntee