TEVA-FLUTAMIDE TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

FLUTAMIDE

Available from:

TEVA CANADA LIMITED

ATC code:

L02BB01

INN (International Name):

FLUTAMIDE

Dosage:

250MG

Pharmaceutical form:

TABLET

Composition:

FLUTAMIDE 250MG

Administration route:

ORAL

Units in package:

100/250/500/1000

Prescription type:

Prescription

Therapeutic area:

ANTINEOPLASTIC AGENTS

Product summary:

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

Authorization status:

CANCELLED POST MARKET

Authorization date:

2018-04-30

Summary of Product characteristics

PRODUCT MONOGRAPH
Pr
TEVA–FLUTAMIDE
(flutamide tablets)
250 mg
Non-Steroidal Antiandrogen
Teva Canada Limited
Date of Revision: December 02, 2014
30 Novopharm Court
Toronto, Canada
M1B 2K9
Control Number: 174585
2
Pr
TEVA–FLUTAMIDE
(flutamide tablets)
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 prostrate
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 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.
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 volunteers,
flutamide and its active metabolite approached steady-state plasma
levels (based on
pharmacokinetic simulations) after the fourth flutamide dose. The
half-life of the active
metabolite in geriatric volunteers