Pharmacologic and pharmacokinetic characteristics of norgestimate and its metabolites

Am J Obstet Gynecol. 1990 Dec;163(6 Pt 2):2127-31. doi: 10.1016/0002-9378(90)90552-i.


Biotransformation, pharmacologic, and pharmacokinetic studies of norgestimate and its metabolites indicate that 17-deacetyl norgestimate, along with the parent drug, contributes to the biologic response. The postulated metabolic pathway, which is based on the identification of urinary products had indicated that three metabolites of norgestimate, 17-deacetyl norgestimate, 3-keto norgestimate, and levonorgestrel, might participate in the response. The pharmacologic evaluation of these metabolites demonstrates that only 17-deacetyl norgestimate has a pharmacologic profile consistent with that of norgestimate, and significant concentrations of this metabolite have been measured in the serum of women after the administration of norgestimate. These studies indicate that 17-deacetyl norgestimate contributes to the pharmacologic response to norgestimate.

Publication types

  • Review

MeSH terms

  • Animals
  • Biotransformation
  • Contraceptives, Oral* / chemistry
  • Contraceptives, Oral* / metabolism
  • Contraceptives, Oral* / pharmacokinetics
  • Contraceptives, Oral* / pharmacology
  • Drug Combinations
  • Female
  • Humans
  • Levonorgestrel
  • Molecular Structure
  • Norgestrel / analogs & derivatives*
  • Norgestrel / chemistry
  • Norgestrel / metabolism
  • Norgestrel / pharmacokinetics
  • Norgestrel / pharmacology
  • Oximes


  • Contraceptives, Oral
  • Drug Combinations
  • Oximes
  • norgestrel acetate
  • Norgestrel
  • Levonorgestrel
  • norgestimate
  • norelgestromin