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Estradiol levels with 50 to 100 μg/day transdermal estradiol patches applied to the forearm and to the scrotum in a crossover study in 2 men with prostate cancer. [14] In 35 men treated continuously with one 100 μg/day estradiol patch scrotally, the mean estradiol level was ~500 pg/mL (range ~125–1,200 pg/mL).
[223] [224] Estraderm, a reservoir patch and the first transdermal estradiol patch to be marketed, was introduced in Europe in 1985 and in the United States in 1986. [225] [226] The first transdermal matrix estradiol patches to be introduced were Climara and Vivelle between 1994 and 1996, and were followed by many others. [223] [227]
Estradiol/levonorgestrel (E2/LNG), sold under brand name Climara Pro, is a combination of estradiol (E2) and levonorgestrel (LNG) which is used in menopausal hormone therapy. [ 1 ] [ 2 ] [ 3 ] It is a 22-cm 2 transdermal patch containing 4.4 mg estradiol and 1.39 mg levonorgestrel and delivers 45 μg/day estradiol and 15 μg/day levonorgestrel.
In other words, a 100 μg/day Climara estradiol patch may be expected to produce circulating estradiol levels of around 100 pg/mL. [205] Transdermal estradiol patches produce an estradiol to estrone ratio of about 1:1. [10] [12] Following removal of an estradiol patch, circulating estradiol levels decrease to baseline within 24 hours. [10]
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Estradiol valerate was first described in 1940 and was introduced for medical use in 1954. [19] [20] [21] Along with estradiol cypionate, it is one of the most widely used esters of estradiol. [22] Estradiol valerate is used in the United States, Canada, Europe, and throughout much of the rest of the world. [23] [24] It is available as a ...