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The elimination half-life of levonorgestrel is 24 to 32 hours, although values as short as 8 hours and as great as 45 hours have been reported. [4] [6] About 20 to 67% of a single oral dose of levonorgestrel is eliminated in urine and 21 to 34% in feces. [6]
[213] [97] [12] [10] Estradiol patches delivering a daily dosage of 0.05 mg (50 μg) achieve mean estradiol and estrone levels of 30 to 65 pg/mL and 40 to 45 pg/mL, respectively, while a daily dosage of 0.1 mg (100 μg) attains respective mean levels of 50 to 90 pg/mL and 30 to 65 pg/mL of estradiol and estrone. [15]
Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). [1] [2] [6] In one study, the EC 50 Tooltip half-maximal effective concentration value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM).
[108] [109] [114] [110] Low doses (e.g., 50 μg/day) and high doses (e.g., 100 μg/day) of transdermal estradiol for menopausal replacement do not differ in terms of VTE risk. [ 115 ] [ 114 ] [ 116 ] [ 110 ] The higher risk of VTE with oral estradiol can be attributed to the first pass and a disproportionate effect on liver synthesis of ...
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.
[1] [3] With a typical oral contraceptive dosage of norgestimate of 200 to 250 μg/day, an amount of 50 to 60 μg/day levonorgestrel may be produced. [22] This is similar to the ovulation-inhibiting dosage of levonorgestrel, and suggests that norgestimate may act in considerable part as a prodrug specifically of levonorgestrel.
However, a more recent meta-analysis suggested that there is actually a significantly longer half-life for many of the now available progestogen-only pill formulations. For example, Norgestrel and Drosperinone, in particular, appear to have a longer window of efficacy. More variation in dose timing may still effectively prevent pregnancy. [28]
[4] [1] In spite of differing from it only by the presence of an additional double bond between the C15 and C16 positions, gestodene is not metabolized into levonorgestrel in the body. [1] The biological half-life of gestodene is 12 to 15 hours. [2] [4] Gestodene is eliminated 50% in urine and 33% in feces. [1]
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