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[11] [93] A single 2 mg oral dose of norethisterone has been found to result in peak circulating levels of the drug of 12 ng/mL (40 nmol/L), whereas a single 1 mg oral dose of norethisterone in combination with 2 mg estradiol resulted in peak levels of norethisterone of 8.5 ng/mL (29 nmol/L) one-hour post-administration. [11]
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]
Progestogen-only injectable contraceptives (POICs) are a form of hormonal contraception and progestogen-only contraception that are administered by injection and providing long-lasting birth control. [ 2 ] [ 3 ] As opposed to combined injectable contraceptives , they contain only a progestogen without an estrogen , and include two progestin ...
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 ...
These include the 19-nortestosterone derivatives norethisterone, noretynodrel, and tibolone, as well as the norethisterone prodrugs [251] norethisterone acetate, norethisterone enanthate, lynestrenol, and etynodiol diacetate. [1] The estrogenic activity of norethisterone and its prodrugs are due to metabolism into ethinylestradiol. [1]
Estradiol valerate/norethisterone enantate (EV/NETE), sold under the brand name Mesigyna among others, is a form of combined injectable birth control which is used to prevent pregnancy in women.
Estradiol is an estrogen, or an agonist of the estrogen receptors, whereas norethisterone acetate is a progestin (synthetic progestogen), or an agonist of the progesterone receptors. [14] Relugolix suppresses ovarian sex hormone production , whereas estradiol and norethisterone acetate provide hormonal add-back to reduce hypogonadal and ...
In 2022, the combination of ethinylestradiol with norethisterone or with norethisterone acetate was the 80th most commonly prescribed medication in the United States, with more than 8 million prescriptions. [5] [6] It is available as a generic medication. [7]