Pharmacodynamics<unk>  is a progestogen. It is one of the active metabolites of norgestimate. Unlike many related progestins,<unk>  reportedly has negligible androgenic activity. However, it produces levonorgestrel as an active metabolite to some extent, which does have some androgenic activity. Nonetheless, transdermally-administered<unk>  does not counteract the increase in sex hormone-binding globulin levels produced by ethinyl estradiol. Relative affinities (%) of<unk>  and metabolites Compound<unk>  10 0 ? ? ? 0 ? Levonorgestrel () 150–162 45 0 1–8 17–75 50 0 Notes: Values are percentages (%). Reference ligands (100%) were prome- gestone for the , metribolone for the , for the , for the , aldosterone for the , for , and cortisol for . Sources: Pharmacokinetics Upon application of a transdermal patch containing<unk>  and ethinyl estradiol, plateau levels of both are reached by approximately 48 hours, and steady-state levels are reached within 2 weeks of application. Absorption following application to the buttock, upper outer arm, abdomen, and upper torso was assessed and, while absorption from the abdomen was slightly lower, it was considered to be therapeutically equivalent for the various areas. Mean levels of<unk>  at steady-state ranged from 0.305 ng/mL to 1.53 ng/mL, with an average of about 0.725 ng/mL. The plasma protein binding of<unk>  is 99%, and it is bound to albumin but not to sex hormone-binding globulin. The metabolism of<unk>  takes place in the liver and is via transformation into levonorgestrel (conversion of the C3 oxime into a ketone) as well as hydroxylation and conjugation. However, because<unk>  is used parenterally, first-pass metabolism in the liver and gastrointestinal tract that normally occurs with oral administration are avoided. The biological half-life of<unk>  is 17 to 37 hours. The metabolites of<unk> , along with those of ethinyl estradiol, are eliminated in the urine and feces.
Norelgestromin
Levonorgestrel
Chloroethynylnorgestrel
Gestodene
5α-Dihydrolevonorgestrel
Ethinylestradiol sulfonate
Etonogestrel
Telapristone