Format

Send to

Choose Destination
See comment in PubMed Commons below

Selectivity and minimal androgenicity of norgestimate in monophasic and triphasic oral contraceptives.

Author information

1
Eastern Virginia Medical School, Norfolk.

Abstract

The contraceptive progestin norgestimate (NGM) has a high affinity for uterine progestin receptors and a lack of affinity for androgen receptors similar to that of natural progesterone. NGM's selectivity results in excellent efficacy, cycle control, and minimal androgenicity when it is combined with ethinyl estradiol (EE). Clinical studies of a monophasic regimen of NGM/EE indicate a positive impact on lipid metabolism, revealing an increase in serum levels of high-density lipoprotein cholesterol with a concomitant and significant decrease in the low-density lipoprotein/high-density lipoprotein cholesterol ratio. Little impact on carbohydrate metabolism was noted. Serum levels of sex hormone binding globulin, an indicator of androgen-estrogen balance, also increased significantly with NGM/EE in accordance with its low androgenic activity. A significant between-regimen difference in SHBG was seen in a comparison study of NGM/EE and LNG/EE triphasic formulations (a mean rise of 68.6% with NGM/EE vs a decrease of 6.1% with LNG/EE). NGM's lack of estrogenicity was evidenced by unchanged prolactin levels and absence of effect on the coagulation system. In a large study of the monophasic formulation in 59,701 women, some improvement in acne was reported as well as minimal weight gain. An overview of clinical data is provided from United States and European trials as well as some preclinical data relevant to NGM's selectivity.

PIP:

The contraceptive progestin norgestimate (NGM) has a high affinity for uterine progestin receptors and a lack of affinity for androgen receptors, similar to that of natural progesterone. NGM's selectivity results in excellent efficacy, cycle control, and minimal androgenicity when it is combined with ethinyl estradiol (EE). Clinical studies of a monophasic regimen of NGM/EE indicate a positive impact on lipid metabolism, revealing an increase in serum levels of high-density lipoprotein (HDL)-cholesterol with a concomitant and significant decrease in the low-density lipoprotein/HDL cholesterol ratio. Little impact on carbohydrate metabolism was noted. Serum levels of sex hormone binding globulin (SHBG), an indicator of androgen-estrogen balance, also increased significantly with NGM/EE in accordance with its low androgenic activity. A significant between-regimen difference in SHBG was seen in a comparison study of NGM/EE and levonorgestrel (LNG)/EE triphasic formulations (a mean increase of 68.6% with NGM/EE vs. a decrease of 6.1% with LNG/EE). NGM's lack of estrogenicity was seen through unchanged prolactin levels and an absence of effect on the coagulation system. In a large study of the monophasic formulation in 59,701 women, some improvements in acne were reported as well as in minimal weight gain. An overview of clinical data is provided from the US and European trials as well as some preclinical data relevant to NGM's selectivity.

PMID:
1324552
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Loading ...
    Support Center