title: Clinical performance and endocrine profiles of contraceptive vaginal rings releasing 3-keto-desogestrel and ethinylestradiol.
abstract: The clinical performance and endocrine profiles of contraceptive vaginal rings (CVR) with an in vitro daily release rate of 15 micrograms of ethinylestradiol combined with 75, 100 or 150 micrograms 3-keto-desogestrel were evaluated. Two studies were performed; one with 11 volunteers, consisting of a control cycle, a cycle with an oral preparation (Marvelon), followed by two CVR treatment cycles, and a second study with 12 volunteers, having the same design but one CVR treatment cycle. A dose-response relationship was seen in the endocrine and clinical performance of the CVR. With CVR 75/15, ovulation occurred in two subjects, and increases in serum estradiol concentrations were seen in two additional subjects. With CVR 100/15, slight estradiol increases were seen in four subjects, but progesterone remained low. With CVR 150/15, both estradiol and progesterone serum concentrations remained low. With CVR 75/15 extra bleeding was common, but with CVR 150/15 this did not occur. No major side effects occurred, and no abnormal Papanicolaou smears or histological findings of the endometrium were found. All volunteers completed all cycles, and the three-week CVR use was generally well accepted. In conclusion, the release rate of CVR 75/15 was insufficient. A vaginal ring with a daily release rate between 100 and 150 micrograms of 3-keto-desogestrel in combination with 15 micrograms of ethinylestradiol seems suitable for contraceptive purposes, and will be further tested in larger clinical studies.
authors: Department of Obstetrics and Gynecology, Helsinki University Central Hospital, Finland.
authors: D
authors: D
authors: Apter
authors: B
authors: B
authors: Cacciatore
authors: U H
authors: UH
authors: Stenman
authors: U
authors: U
authors: Alapiessa
authors: R
authors: R
authors: Assendorp
mesh_terms: D000328:Adult; D000735:Androstenedione / Q000097:blood; D003274:Contraceptive Devices, Female; D003687:Dehydroepiandrosterone / Q000097:blood; D017135:Desogestrel; D013196:Dihydrotestosterone / Q000097:blood; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000097:blood; D004997:Ethinyl Estradiol / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008597:Menstrual Cycle / Q000187:drug effects; D009652:Norpregnenes / Q000494:pharmacology*; D010053:Ovary / Q000187:drug effects; D011374:Progesterone / Q000097:blood; D011372:Progestins / Q000494:pharmacology*; D013739:Testosterone / Q000097:blood
chemical_list: D009652:Norpregnenes; D011372:Progestins; D013196:Dihydrotestosterone; C044815:etonogestrel; D013739:Testosterone; D000735:Androstenedione; D004997:Ethinyl Estradiol; D003687:Dehydroepiandrosterone; D011374:Progesterone; D004958:Estradiol; D017135:Desogestrel