In Vivo Formation of Ethinylestradiol After Intramuscular Administration of Norethisterone Enantate

@article{Friedrich2018InVF,
  title={In Vivo Formation of Ethinylestradiol After Intramuscular Administration of Norethisterone Enantate},
  author={Christian Friedrich and Matthias Berse and Stefan Klein and Beate Rohde and Joachim H{\"o}chel},
  journal={The Journal of Clinical Pharmacology},
  year={2018},
  volume={58}
}
It is known that a small fraction of orally administered norethisterone is metabolically converted to ethinylestradiol. This exploratory, open‐label, nonrandomized study was conducted to investigate the systemic exposure to ethinylestradiol after intramuscular administration of norethisterone enantate in comparison with the exposure to ethinylestradiol after administration of a standard combined oral contraceptive. Sixteen healthy premenopausal women received an oral contraceptive… Expand
Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception.
TLDR
It is shown that there is a paucity of research on most of these topics for most progestins, and major impediments to clear conclusions are a lack of standardized methodologies, comparisons between non-parallel clinical studies and variability of data on serum concentrations between and within studies. Expand
Analytical Method Validation of RP-HPLC Method for Simultaneous Estimation of Levonorgestrel and Ethinylestradiol from Combined DrugProduct
The aim of recent study is to explore a rapid, sensitive and selective Reversed Phase HPLC method for simultaneous quantification of steroidal hormones Levonorgestrel and Ethinylestradiol from drugExpand
Norethisterone Enanthate Increases Mouse Susceptibility to Genital Infection with Herpes Simplex Virus Type 2 and HIV Type 1
TLDR
It is revealed that compared with mice in estrus, treatment of mice with DMPA or NET-EN significantly decreased genital levels of the cell–cell adhesion molecule desmoglein-1 and increased genital mucosal permeability and susceptibility to genital pathogens while also implying thatNET-EN generates less compromise of genital mucosa barrier function than DMPA. Expand
Comparative metabolic analysis between distant sea urchin hybrids (Heliocidaris crassispina ♀ × Strongylocentrotus intermedius ♂) and their parental purebred offspring
TLDR
Observations in this study suggest that the HS hybrids can be a prospective aquaculture urchin species but also enrich the metabolite database and provide biomarker information from a metabolome aspect that may contribute to Aquaculture potential and commercial-value evaluation of new sea urchins varieties. Expand

References

SHOWING 1-10 OF 10 REFERENCES
In vivo conversion of norethisterone and norethisterone acetate to ethinyl etradiol in postmenopausal women.
TLDR
It is concluded that at therapeutic doses of the progestogens, the exposure to metabolically derived ethinyl estradiol is probably of little clinical significance not only in fertile women using oral contraceptive combination preparations containing norethisterone and ethinyl Estradiol, but also in postmenopausal women who receive oral doses of estradio for estrogen replacement. Expand
Formation of ethinylestradiol in postmenopausal women during continuous treatment with a combination of estradiol, estriol and norethisterone acetate.
TLDR
Investigation of the serum concentrations of estradiol, ethinylestradiol and norethisterone in 25 patients of a gynecological practice who were continuously treated for climacteric complaints concluded that in the presence of the highEstradiol concentrations the low conversion rate of norehisterone into ethinylstradiol is probably without clinical significance. Expand
Formation of ethinyl estradiol in women during treatment with norethindrone acetate.
TLDR
NET-A is converted to EE(2), and although the conversion rate is relatively small, higher doses of NET-A, as used clinically, give rise to substantial levels of EE( 2). Expand
Metabolism of levonorgestrel, norethindrone, and structurally related contraceptive steroids.
TLDR
There is limited information on the metabolism of levonorgestrel, norethindrone and structurally related contraceptive steroids, and it appears that neither desogestrel nor gestodene are transformed to the parent compound. Expand
Pharmacokinetics of norethisterone oenanthate in humans.
TLDR
There was a two-fold variation between the subjects in the bioavailability of NET, less than 5% of the bioavailable NET was released after day 60, while in all subjects NET was detectable in the circulation for a longer time after injection than NET-OEN. Expand
In vivo conversion of norethisterone to ethynyloestradiol in perimenopausal women
TLDR
Results from this study show that a small but significant proportion of norethisterone is converted to ethynyloestradiol in vivo. Expand
Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects.
TLDR
Differences in chemical structure, metabolism, pharmacokinetics, affinity, potency, and efficacy via steroid receptors, intracellular action, and biological and clinical effects confirm the absence of a class effect of progestogens. Expand
In vivo conversion of norethisterone to ethynyloestradiol in Friedrich et al 789 perimenopausal women
  • J Steroid Biochem Mol Biol
  • 1990
and Drug Administration
  • Guidance for industry: Bioanalytical method validation. http://www.fda.gov/downloads/ Drugs/Guidances/ucm070107.pdf. Accessed November 20,
  • 2017
Guidance for industry: Bioanalytical method validation