RATIO-BICALUTAMIDE TABLET

Država: Kanada

Jezik: angleščina

Source: Health Canada

Aktivna sestavina:

BICALUTAMIDE

Dostopno od:

RATIOPHARM INC DIVISION OF TEVA CANADA LIMITED

Koda artikla:

L02BB03

INN (mednarodno ime):

BICALUTAMIDE

Odmerek:

50MG

Farmacevtska oblika:

TABLET

Sestava:

BICALUTAMIDE 50MG

Pot uporabe:

ORAL

Enote v paketu:

30

Tip zastaranja:

Prescription

Terapevtsko območje:

ANTINEOPLASTIC AGENTS

Povzetek izdelek:

Active ingredient group (AIG) number: 0127996001; AHFS:

Status dovoljenje:

CANCELLED POST MARKET

Datum dovoljenje:

2014-09-19

Lastnosti izdelka

PRODUCT MONOGRAPH
Pr
ratio-BICALUTAMIDE
(Bicalutamide Tablets)
50 mg
Non-Steroidal Antiandrogen
ratiopharm inc.
Date of Preparation:
17,800 rue Lapointe
March 1, 2006
Mirabel, PQ
J7J 1P3
Control #: 104203
-2-
Product Monograph
Pr
ratio-BICALUTAMIDE
(Bicalutamide Tablets)
50 mg
Non-Steroidal Antiandrogen
ACTION
AND
CLINICAL
PHARMACOLOGY
Bicalutamide is a non-steroidal antiandrogen, devoid of other
endocrine activity. Bicalutamide
competitively inhibits the action of androgens by binding to cytosol
androgen receptors in target
tissue. This inhibition results in regression of prostatic tumours.
Bicalutamide is a racemate and
the (R)-enantiomer is primarily responsible for the antiandrogenic
activity of bicalutamide.
Pharmacokinetics and Metabolism
The absorption, distribution, metabolism and excretion of bicalutamide
has been investigated
after administration of a single 50 mg oral dose to volunteers. The
results indicated that the dose
was extensively absorbed and was excreted almost equally in urine
(36%) and faeces (43%) over
a 9 day collection period. There is no evidence of any clinically
significant effect of food on
bioavailability. Steady state plasma concentrations of the
(R)-enantiomer of approximately 9
µg/ml are observed during daily administration of 50 mg doses of
bicalutamide. At steady state,
the
active
(R)-enantiomer
accounts
for
99%
of
the
circulating
plasma
bicalutamide
concentration. Bicalutamide is highly protein bound (racemate 96%,
R-enantiomer 99.6%). On
daily administration, the (R)-enantiomer accumulates about 10-fold in
plasma, consistent with an
elimination half-life of approximately one week. The (S)-enantiomer is
very rapidly cleared
relative to the (R)-enantiomer. The pharmacokinetics of the
(R)-enantiomer are unaffected by
age, renal impairment or mild to moderate hepatic impairment. Patients
with severe hepatic
impairment eliminate the (R)-enantiomer from plasma more slowly.
Bicalutamide is extensively
metabolized via both oxidation and glucuronidation with approximately
equal renal