Gracial ProdMonograph_cover - epgonline.org
Gracial ProdMonograph_cover - epgonline.org
Gracial ProdMonograph_cover - epgonline.org
You also want an ePaper? Increase the reach of your titles
YUMPU automatically turns print PDFs into web optimized ePapers that Google loves.
3. Pharmacodynamics<br />
•Etonogestrel has a high selectivity index<br />
• The 22-day regimen of <strong>Gracial</strong> permits a very low<br />
progestogen dose in the first seven days of the cycle,<br />
without compromising contraceptive reliability<br />
•<strong>Gracial</strong> inhibits follicle development and ovulation<br />
3.1 Receptor affinity<br />
Different progestogens have different hormonal profiles: in<br />
addition to the progestogenic activity required for the<br />
inhibition of ovulation, progestogens may also possess some<br />
degree of androgenic activity. This is neither required nor<br />
desirable in OCs because of adverse effects such as<br />
androgenic skin disorders.<br />
Desogestrel is derived, like levon<strong>org</strong>estrel, gestodene and<br />
n<strong>org</strong>estimate, from 19-nortestosterone. Desogestrel is,<br />
however, differentiated from levon<strong>org</strong>estrel and other<br />
progestogens by a methylene group at position 11, which<br />
interferes with the binding of desogestrel to androgen<br />
receptors.<br />
CH 3<br />
H 2<br />
C<br />
11<br />
12<br />
CH 2<br />
13<br />
17<br />
OH<br />
C<br />
CH<br />
2<br />
1<br />
9<br />
10 8<br />
14<br />
15<br />
16<br />
3 5<br />
4<br />
6<br />
7<br />
Fig. 6: Structure of desogestrel<br />
10
Change language