American Journal of Obstetrics and Gynecology
Pharmacologic and pharmacokinetic characteristics of norgestimate and its metabolites
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Cited by (59)
Modeling hormonal contraception in female rats: A framework for studies in behavioral neurobiology
2022, Frontiers in NeuroendocrinologyCitation Excerpt :Another illustration that classification by generation is problematic is the classification of norgestimate (NOR) as a third-generation progestin (Anand et al., 2015; Davtyan, 2012; Tricotel et al., 2015). NOR is rapidly metabolized to form 17-desacetylnorgestimate, which can later be metabolized to LNG (Ahire et al., 2017; Kuhl, 2005; McGuire et al., 1990). LNG is a progestin most often classified as second-generation, even by the same authors (Anand et al., 2015; Davtyan, 2012; Tricotel et al., 2015).
Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception
2021, Pharmacology and TherapeuticsCitation Excerpt :Interestingly, 5α-NET is more potent via PR-A than PR-B, while 3α,5α-NET is a partial agonist for PR-B but not PR-A (Larrea et al., 2001). NGM is metabolized to LNG-17-acetate and NGMN, also known as 17-deacetyl-noregestimate or LNG-3-oxime (Juchem et al., 1993; McGuire et al., 1990), with NGMN being the main progestogenic metabolite (Fig. 2, Table 1). Both NGM and NGMN elicit progestogenic and androgenic activity (Juchem et al., 1993; Phillips, Demarest, Hahn, Wong, & McGuire, 1990; Prifti, Lelle, Strowitzki, & Rabe, 2004).
Effects of hormonal contraceptive phase and progestin generation on stress-induced cortisol and progesterone release
2019, Neurobiology of StressCitation Excerpt :The varying androgenicity of the progestins may contribute to the differences in free cortisol response to stressors across progestin generation, with more androgenic progestins leading to blunted cortisol responses to stress. However, levonorgestrel, the most prevalently used second-generation progestin in this study, is highly androgenic (Kaplan, 1995; Lemus et al., 1992; McGuire et al., 1990; Schindler et al., 2003; Sitruk-Ware, 2004; Sitruk-Ware and Nath, 2011; Van der Vange et al., 1990). Thus, despite the negative relationship between androgens and the steroid response to stress, the androgenicity of progestins does not appear to impart a similar effect on the stress steroid response.
UPLC-MS/MS assay for the simultaneous determination of ethinyl estradiol, norgestimate and 17-Desacetyl norgestimate at low pg/mL in human plasma
2016, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life SciencesCitation Excerpt :NGM is rapidly metabolized to 17-Desacetyl norgestimate (DNGM) and norgestrel (NG). DNGM is pharmacologically active and the pharmacologic profile is similar to that of NGM [3–6]. Given the rapid metabolism of NGM, the circulating concentrations of NGM are extremely low, which was one of the major challenges to quantify NGM in plasma or serum.
Quantification of 17-desacetyl norgestimate in human plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and its application to bioequivalence study
2015, Journal of Pharmaceutical AnalysisCitation Excerpt :As the norgestimate serum concentrations following single or multiple dosing are generally below assay detection within 5 h, a major norgestimate serum metabolite, 17-desacetyl norgestimate (which exhibits a serum half-life ranging from 12 and 30 h), appears rapidly in serum with concentrations greatly exceeding that of norgestimate. The 17-deacetylated metabolite (pka 12.22) is pharmacologically active and the pharmacologic profile is similar to that of norgestimate [10–14]. Reported literature has mentioned, to assess the effect of anticonvulsants [8] and rosuavastatin [10], the pharmacokinetics of 17-desacetyl norgestimate and plasma was analyzed for 17-desacetyl norgestimate with validated LC–MS/MS method, but analytical method details are not available for monitoring plasma levels.