NORMENS 5MG TABLET

Country: Malaysia

Language: English

Source: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)

Active ingredient:

NORETHISTERONE ACETATE

Available from:

Vitamode Sdn.bhd

INN (International Name):

NORETHISTERONE ACETATE

Units in package:

5x10tablet Tablets; 3x10tablet Tablets

Manufactured by:

RENATA LIMITED

Summary of Product characteristics

NORMENS
®
5MG TABLET
(Norethisterone acetate)
PRESENTATION:
Each
white,
uncoated
tablet
contains
Norethisterone
acetate
BP
equivalent
to
5mg
norethisterone.
PRODUCT DESCRIPTION:
6.0 mm, White, Round Flat Bevel Edge tablet, one side having logo
“N” and other side
contains breakline.
PHARMACOKINETICS
• Absorption
Peak serum concentrations after administration of 5mg
NORMENS
®
were 16±5 ng/mL; t
max
was 1.5 ±0.6 hours. Tthe bioavailability of a single dose of 1mg
norethisterone compared to
an equivalent intravenous dose ranged from 47% to 73%, suggesting a
significant first pass
effect. This study showed that the disposition of norethisterone
follows a biexponential
pattern with half lives of 0.4-2.6 and 5-13 hours respectively. The
apparent volume of
disposition was 4.28±0.56L/kg.
• Distribution
Norethisterone is bound to serum albumin and to sex hormone binding
globulin (SHBG).
Only about 3-4 % of the total serum drug concentrations are present as
free steroid, about 35
% and 61 % are bound to SHBG and albumin, respectively. The apparent
volume of
distribution of norethisterone is 4.4 ± 1.3 L/kg. Following oral
administration, the drug serum
level time course follows a biphasic pattern. Both phases are
characterized by half-lives of 1-
2 and about 5-13 hours, respectively. Norethisterone is transferred
into milk and the drug
levels in breast milk were found to be about 10% of those found in
maternal plasma.
• Metabolism
Norethisterone is mainly metabolized by saturation of the double bond
in ring A and the
reduction
of
the
3-keto
group
to
a
hydroxyl
group
followed
by
conjugation
to
the
corresponding sulfates and glucuronides. Some of these metabolites are
eliminated slowly
from plasma, building approximately to a peak at the midpoint of the
treatment cycle and
rapidly dropping to near baseline levels when treatment is stopped.
Norethisterone is partly
metabolized to ethinylestradiol. Per one milligram of orally
administered norethisterone,
ethinylestradiol is formed equivalent to an oral dose of ap