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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]
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 ...
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.
Norethisterone is a substrate for and is known to be an inhibitor of 5α-reductase, with 4.4% and 20.1% inhibition at 0.1 and 1 μM, respectively. [11] However, therapeutic concentrations of norethisterone are in the low nanomolar range, so this action may not be clinically relevant at typical dosages.
[7] [4] Norgestrel is available as a generic medication. [13] In 2022, the version with ethinylestradiol was the 264th most commonly prescribed medication in the United States, with more than 1 million prescriptions. [14] [15] In July 2023, the US Food and Drug Administration (FDA) approved norgestrel for over-the-counter sale. [2]
Combined oral contraceptive pills are a type of oral medication that were originally designed to be taken every day at the same time of day in order to prevent pregnancy. [26] [37] There are many different formulations or brands, but the average pack is designed to be taken over a 28-day period (also known as a cycle).
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