[Clinical evidence of the minimal androgenic activity of norgestimate].
The aim for improving the progestogen component of oral contraceptives is both to increase their selectivity by obtaining a highly effective contraceptive action and to decrease the side effects related to the existing progestogens. The androgenic activity of the existing progestogens modifies the lipid metabolism, particularly a decrease in the high density lipoprotein (HDL) level, which increases the risks of cardiovascular diseases. Thus, the discovery of a progestogen with good anti-ovulatory and minimal androgenic properties would constitute an important progress in the field of oral contraception. Norgestimate (NGM) is a new progestogen presenting an exceptional profile of biological activity, and has proved to be extremely selective, as observed during the clinical trials. The studies described below have been carried out in order to confirm clinically the low androgenic activity of NGM. In two clinical trials, Norgestimate (0.25 mg) associated with 0.035 mg of ethinyloestradiol (NGM 0.25/35) was compared to norgestrel (0.30 mg) associated with 0.030 mg of ethinyloestradiol (Lo/Ovral). In the first trial (1,261 women), the following observations were made: an important increase in the HDL level compared to the base levels in the subjects taking NGM 0.25/35, and an important decrease in the HDL level in those taking Lo/Ovral. The low density lipoprotein (LDL) level increased slightly in the NGM 0.25/35 group, while a higher increase was observed in the Lo/Ovral group. Moreover, the LDL/HDL ratio translates a more favourable lipid profile in the NGM 0.25/35 group, since the values are lower than those observed for the Lo/Ovral group.(ABSTRACT TRUNCATED AT 250 WORDS)
Chapdelaine
A
A
Hôpital Maisonneuve Rosemont, Montréal, Quebec, Canada.
Desmarais
J L
JL
Derman
R J
RJ
D000152:Acne Vulgaris / Q000139:chemically induced; D000328:Adult; D000728:Androgens; D002986:Clinical Trials as Topic; D004997:Ethinyl Estradiol / Q000494:pharmacology; D005260:Female; D006801:Humans; D008075:Lipoproteins, HDL / Q000097:blood; D008077:Lipoproteins, LDL / Q000097:blood; D015337:Multicenter Studies as Topic; D009644:Norgestrel / Q000031:analogs & derivatives* / Q000494:pharmacology; D012738:Sex Hormone-Binding Globulin / Q000032:analysis; D015430:Weight Gain
D000728:Androgens; D008075:Lipoproteins, HDL; D008077:Lipoproteins, LDL; D012738:Sex Hormone-Binding Globulin; D009644:Norgestrel; D004997:Ethinyl Estradiol; C017576:norgestimate
Preuve clinique de l'activité androgénique minimale du norgestimate.