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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]
Whereas the biological half-life of estradiol given by intravenous injection is about 0.5 to 2 hours, the biological half-life of oral estradiol has a range of 13 to 20 hours due to the large and long-lasting pool of estrogen conjugates that is formed during first-pass metabolism and that serves to continuously replenish circulating estradiol ...
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).
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.
The pharmacokinetics of estradiol, including its bioavailability, metabolism, biological half-life, and other parameters, differ by route of administration. [11] Likewise, the potency of estradiol, and its local effects in certain tissues, most importantly the liver, differ by route of administration as well. [11]
Elimination half-life: 7 ... 50 μg EE with levonorgestrel had 2.1- to 2.3 ... can be observed in half of women on birth control pills with 50 ...
This results in a longer circulation half-life for the protein, and raised levels. ... Levonorgestrel: 50 <1 Medroxyprogesterone acetate <1 <1 Megestrol acetate <1 <1
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 ...
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