Gracial ProdMonograph_cover - epgonline.org

Summary of product characteristics
ELIMINATION
Ethinylestradiol serum levels decrease in two
phases, the terminal disposition phase is
characterized by a half-life of approximately
24 hours. Unchanged drug is not excreted,
ethinylestradiol metabolites are excreted at a
urinary to biliary ratio of 4:6. The half-life of
metabolite excretion is about 1 day.
STEADY-STATE CONDITIONS
Steady-state concentrations are reached after
3–4 days when serum drug levels are higher by
30–40% as compared to single dose.
5.3 Preclinical safety data
Animal toxicity studies for human risk estimation
were performed for both components of the
preparation, ethinylestradiol and desogestrel, and
the combination.
No effects which might indicate an unexpected risk
to humans were observed during systemic
tolerance studies after repeated administration.
Long-term repeated dose toxicity studies did not
indicate a tumorigenic potential. However, it must
be borne in mind that sex steroids can promote
the growth of certain hormone-dependent tissues
and tumors.
Studies on embryotoxicity and teratogenicity and
the evaluation of the effects of both components
on the fertility of parent animals, fetal
development, lactation and reproductive
performance of the offspring gave no indication of
a risk of adverse effects in humans after
recommended use of the preparation.
In vitro and in vivo studies gave no indication of a
mutagenic potential.
6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Blue tablets:
Colloidal silicon dioxide; lactose; potato starch;
povidone; stearic acid; dl-alpha-tocopherol;
indigotin (E132).
White tablets:
Colloidal silicon dioxide; lactose; potato starch;
povidone; stearic acid; dl-alpha-tocopherol.
The daily amount of lactose (< 100 mg) is such
that women with an intolerance to lactose are
highly unlikely to experience a problem.
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
Shelf life of the tablets is as indicated on the box,
if stored according to the directions in Section 6.4.
6.4 Special precautions for storage
Store at 2°C to 30°C.
6.5 Nature and contents of container
Push-through packs with 7 blue and 15 white
tablets. Tablets are round, flat and 6 mm in
diameter. Tablets are coded on one side with
Organon* and on the reverse side with TR8 (white
tablets) or TR9 (blue tablets).
The pack is a PVC/Al blister consisting of
aluminium foil with a heat-seal coating and a PVC
film. Each blister is packed in a printed aluminium
pouch. The pouch is packed in a printed
cardboard box together with the package leaflet.
6.6 Instructions for use/handling and
disposal (if appropriate)
Store all drugs properly and keep them out of
reach of children.
7. MARKETING AUTHORIZATION
HOLDER
N.V. Organon
P.O. Box 20
5340 BH Oss
The Netherlands
8. NUMBERS IN THE COMMUNITY
REGISTER OF MEDICINAL
PRODUCTS
9. DATE OF FIRST AUTHORIZATION
[Market-specific information must be included in
this section where applicable].
10. DATE OF REVISION OF TEXT
February 1998.
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