Pharmacologic and pharmacokinetic characteristics of norgestimate and its metabolites

Pharmacokinetics of Norelgestromin and Ethinyl Estradiol from Two Consecutive Contraceptive Patches

“…The mean t 1/2 value of NGMN observed in this study is similar to that reported with norgestimate-containing oral contraceptives. 12 The similar t 1/2 value for NGMN between the patch and norgestimate-containing oral contraceptives is consistent with simple absorption and metabolism through the gastrointestinal tract and liver (in the case of oral contraceptives) and through the skin (in the case of the patch). There is no evidence to support a greater depot effect of the skin than of the gastric mucosa following patch delivery of these hormones.…”

“…Subjects were admitted to the study unit the evening prior to dosing on day 1 through the morning of day 2, from the morning of day 8 through the morning of day 9, and from the morning of day 18 through the last blood draw on day 20. Subjects visited the study unit on days 3, 4, 7, 10, 11,12,13,14,15,16, and 17 for pharmacokinetic and safety evaluations.…”

Influence of alitretinoin on the pharmacokinetics of the oral contraceptive ethinyl estradiol/norgestimate

“…Norgestimate is rapidly metabolized after oral administration, and concentrations in human serum are typically low. The major metabolite, 17‐deacetyl norgestimate, has a pharmacological profile similar to that of norgestimate, and contributes to its pharmacological activity 13 . The AUC of 17‐deacetyl norgestimate was reduced by 12% after administration of OC plus alitretinoin, compared with OC alone.…”

Tailoring Combination Oral Contraceptives to the Individual Woman

“…5 Norgestimate is a prodrug: following oral administration, it is rapidly absorbed and almost completely converted to levonorgestrel-3-oxime (norelgestromin) and other progestationally active metabolites (including levonorgestrel) within 5 hours postdose. 48 The progestational activity of desogestrel is mediated by its metabolite, etonogestrel. 49 Unlike progesterone, etonogestrel has no glucocorticoid-like activity and does not bind to the MR. 20 Gestodene is absorbed without modification.…”