A norgestimate-containing oral contraceptive: review of clinical studies.
Despite the well-documented efficacy and safety of low-dose oral contraceptives, the development of newer formulations containing highly selective progestins with minimal or no androgenic activity has been a goal of pharmaceutical research. The efficacy and safety of norgestimate, a progestin with inherently low androgenicity, in combination with ethinyl estradiol, has been examined in several phase II and phase III clinical studies, and these are reviewed. Norgestimate/ethinyl estradiol has proved to be a low-dose oral contraceptive with high selectivity that provides the cycle control of older oral contraceptive formulations with comparable efficacy. Results of comparison studies between norgestimate/ethinyl estradiol and formulations containing norgestrel, a progestin with relatively greater androgenic activity, in combination with ethinyl estradiol, are reported for effects on lipid and lipoprotein levels and carbohydrate metabolism. Norgestimate/ethinyl estradiol consistently produced statistically significant increases in high-density lipoprotein cholesterol and improvement in the ratio of low-density lipoprotein cholesterol to high-density lipoprotein. In contrast, norgestrel/ethinyl estradiol produced statistically significant decreases in high-density lipoprotein cholesterol and potentially adverse changes in the low-density/high-density lipoprotein ratio. Phase II studies have confirmed that norgestimate/ethinyl estradiol has low androgenic activity and causes minimal effect on coagulation factors and carbohydrate metabolism.
Kafrissen
M E
ME
R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869-0602.
D001777:Blood Coagulation / Q000187:drug effects; D001835:Body Weight / Q000187:drug effects; D050260:Carbohydrate Metabolism; D003276:Contraceptives, Oral / Q000009:adverse effects / Q000494:pharmacology*; D004702:Endocrine Glands / Q000187:drug effects; D005260:Female; D006801:Humans; D008055:Lipids / Q000097:blood; D008074:Lipoproteins / Q000097:blood; D008597:Menstrual Cycle / Q000187:drug effects; D009644:Norgestrel / Q000031:analogs & derivatives* / Q000494:pharmacology
D003276:Contraceptives, Oral; D008055:Lipids; D008074:Lipoproteins; D009644:Norgestrel; C017576:norgestimate