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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]
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, respectively.
A high dosage of 20 mg/day norethisterone or norethisterone acetate has been found to significantly stimulate the sebaceous glands, whereas lower dosages of 5 mg/day and 2.5 mg/day norethisterone and norethisterone acetate, respectively, did not significantly stimulate sebum production and were consequently regarded as devoid of significant ...
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. Through its progestogenic activity, NETE has potent antigonadotropic effects and can inhibit fertility and suppress sex hormone levels.
The most common side effects of the medication include hot flushes, excessive sweating or night sweats, uterine bleeding, hair loss or thinning, and decreased interest in sex. [8] The medication was approved for medical use in the United States in May 2021, [8] [11] [12] and in the European Union in July 2021. [9]
Fibroids are benign (non-cancerous) muscle tumors of the uterus that can cause heavy menstrual bleeding, pain, bowel or bladder problems and infertility. [2] Some women may not experience any symptoms, but many do, including heavy bleeding with periods. [2]
Side effects can include nausea, headache, blood clots, breast pain, depression, and liver problems. [2] Use is not recommended during pregnancy, the initial three weeks after childbirth, and in those at high risk of blood clots. [2] [4] It, however, may be started immediately after a miscarriage or abortion. [4]
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.