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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 ...
Testosterone levels with different doses of cyproterone acetate (CPA), segesterone acetate (SGA), norethisterone acetate (NETA), and levonorgestrel (LNG) alone then in combination with transdermal testosterone followed by discontinuation and recovery in healthy young men. [156]
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.
The risk of venous thromboembolism with EE/CPA-containing birth control pills is similar to that with EE and gestodene-, desogestrel-, and drospirenone-containing birth control pills and about 50 to 80% higher than with EE and levonorgestrel-containing birth control pills.
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.
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Hormonal therapies to reduce or stop menstrual bleeding have long been used to manage a number of gynecologic conditions including menstrual cramps (dysmenorrhea), heavy menstrual bleeding, irregular or other abnormal uterine bleeding, menstrual-related mood changes (premenstrual syndrome or premenstrual dysphoric disorder), and pelvic pain due to endometriosis or uterine fibroids.
The estrogenic activity of norethisterone and its prodrugs are due to metabolism into ethinylestradiol. [1] High doses of norethisterone and noretynodrel have been associated with estrogenic side effects such as breast enlargement in women and gynecomastia in men, but also with alleviation of menopausal symptoms in postmenopausal women. [ 252 ]
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