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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 ...
[25] [26] [27] Norethisterone is marketed widely throughout the world. [28] It is available as a generic medication. [29] In 2022, it was the 135th most commonly prescribed medication in the United States, with more than 4 million prescriptions. [30] [31] It is on the World Health Organization's List of Essential Medicines. [32]
Estradiol and levonorgestrel (Climara Pro) – 45 μg/24 hours / 15 μg/24 hours; Estradiol and norethisterone acetate (Combipatch) – 50 μg/24 hours / 0.14 mg/24 hours; 50 μg/24 hours / 0.25 mg/24 hours
The ovulation-inhibiting dose of norgestrel appears to be greater than 75 μg/day, as ovulation occurred in 50 to 75% of cycles with this dosage of norgestrel in studies. [17] The ovulation-inhibiting dosage of levonorgestrel, which is twice as potent as norgestrel, is approximately 50 to 60 μg/day.
The levonorgestrel intrauterine system (LNG-IUS) is a type of long-term birth control that releases the progestin into the uterine cavity. [46] [25] Levonorgestrel is released at a constant, gradual rate of 0.02 mg per day by the polydimethylsiloxane membrane of the device, which renders it effective for up to five years. [46]
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]
Hormone levels following a single intramuscular injection of EV/NETE (5 mg/50 mg) in healthy young men. [9] Testosterone levels were maximally suppressed by about 94%, to ~30 ng/dL, when measured at day 7. [9] EV/NETE is a combination of EV, an estrogen, and NETE, a progestogen with weak androgenic activity.
All contain an estrogen, ethinylestradiol or mestranol, [1] [2] in varying amounts, and one of a number of different progestogens. (Regarding the estrogen, the inactive 3-methyl ether of ethinylestradiol, which must be metabolized by the liver into the active ethinylestradiol; 50 μg of mestranol is equivalent to only 35 μg of ethinylestradiol and should not be used when high-dose [50 μg ...
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