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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, respectively.
[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
Levonorgestrel is used in emergency contraceptive pills (ECPs), both in a combined Yuzpe regimen which includes estrogen, and as a levonorgestrel-only method. The levonorgestrel-only method uses levonorgestrel 1.5 mg (as a single dose or as two 0.75 mg doses 12 hours apart) taken within three days of unprotected sex.
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.
Norgestimate is a rapidly and completely converted prodrug, mainly of norelgestromin (17β-deacetylnorgestimate or levonorgestrel 3-oxime), but also of levonorgestrel (3-keto-17β-deacetylnorgestimate) to a lesser extent (22 ± 6% of an administered dose or about 40–70 μg) [2] and of levonorgestrel acetate (levonorgestrel 17β-acetate) in ...
Norethisterone and ethinylestradiol levels over 8 weeks after a single intramuscular injection of 200 mg NETE in premenopausal women. [35] A single intramuscular injection of 50 to 200 mg NETE in oil solution has been found to have a duration of action of 11 to 52 days in terms of clinical biological effect in the uterus and on body temperature ...
Estradiol benzoate 5 to 10 mg + norethisterone enanthate 50 to 100 mg [62] Mestranol 1.0–1.2 mg + norethisterone 10–12 mg in a microcrystalline aqueous suspension of defined particle sizes (125–177 μm) [ 25 ] [ 16 ] [ 62 ] [ 32 ]
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