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This is a list of progestogens (progesterone and progestins) and formulations that are approved by the FDA Tooltip Food and Drug Administration in the United States. . Progestogens are used as hormonal contraceptives, in hormone replacement therapy for menopausal symptoms, and in the treatment of gynecological
CICs are different from progestogen-only injectable contraceptives (POICs), such as depot medroxyprogesterone acetate (DMPA; brand names Depo-Provera, Depo-SubQ Provera 104) and norethisterone enantate (NETE; brand name Noristerat), which are not combined with an estrogen and are given once every two to three months instead of once a month.
Norethisterone (3-ketolynestrenol), the active metabolite of lynestrenol.. Lynestrenol itself does not bind to the progesterone receptor and is inactive as a progestogen. [7] [8] It is a prodrug, and upon oral administration, is rapidly and almost completely converted into norethisterone, a potent progestogen, in the liver during first-pass metabolism.
Download as PDF; Printable version; In other projects ... Norethisterone enanthate ... so if it is stopped for a period of time, the tissue will be less damaged than ...
Norgestrel is a progestogen, or an agonist of the progesterone receptor. [6] The biological activity of norgestrel lies in the levo enantiomer, levonorgestrel, whereas the dextro isomer is inactive. [6]
Norethisterone and ethinylestradiol levels over 24 hours after a single oral dose of 10 mg NETA in postmenopausal women. [ 25 ] NETA metabolizes into ethinylestradiol at a rate of 0.20 to 0.33% across a dose range of 10 to 40 mg. [ 26 ] [ 27 ] Peak levels of ethinylestradiol with a 10, 20, or 40 mg dose of NETA were 58, 178, and 231 pg/mL ...
Norethisterone and 5α-DHNET have been found to act as weak irreversible aromatase inhibitors (K i = 1.7 μM and 9.0 μM, respectively). [7] However, the concentrations required are probably too high to be clinically relevant at typical dosages of norethisterone.
NETE is a prodrug of norethisterone in the body. [13] Upon reaching circulation, it is rapidly converted into norethisterone by esterases.Hence, as a prodrug of norethisterone, NETE has essentially the same effects as norethisterone, acting as a potent progestogen with additional weak androgenic and estrogenic activity (the latter via its metabolite ethinylestradiol). [14]
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