Gracial ProdMonograph_cover - epgonline.org

Contents
Page
1. INTRODUCTION 1
1.1 Rationale for Gracial 4
2. PHARMACOKINETICS 6
2.1 Desogestrel 6
Absorption 6
Metabolism 6
Distribution 7
Elimination 7
2.2 Ethinylestradiol 8
3. PHARMACODYNAMICS 10
3.1 Receptor affinity 10
3.2 Selectivity index 11
3.3 Effects on the pituitary ovarian axis 12
3.4 Effects on cervical mucus 15
4. CONTRACEPTIVE EFFICACY 16
5. ACCEPTABILITY 17
5.1 Cycle control 17
Irregular bleeding 18
Withdrawal bleeding 18
5.2 Side effects 20
5.3 Body weight 21
5.4 Continuation rate 21
6. GRACIAL AND MILD TO
MODERATE ACNE 22
6.1 Effect on SHBG and testosterone 22
6.2 Clinical effects 23
7. SAFETY ASPECTS 27
7.1 Venous thromboembolism 28
Hemostasis 28
Epidemiological data 29
7.2 Arterial disease 33
Lipid metabolism 33
Carbohydrate metabolism 35
Blood pressure 35
Epidemiological data 35
7.3 Gynecological cancer 38
Breast cancer 39
Cervical, ovarian and endometrial cancer 40