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The influence of 2 mg/day oral estradiol on levels of hepatic proteins such as SHBG, CBG, and AGT is much lower than that with 10 μg/day oral ethinylestradiol. [128] [68] Vaginal micronized estradiol at 0.25 mg/day increased SHBG levels by about 10% after 2 weeks of therapy in women.
A higher dosage of estradiol gel containing 1.5 mg estradiol per daily application has been found to produce mean estradiol levels of 40 to 100 pg/mL and estrone levels of 90 pg/mL, while 3 mg per day has been found to result in respective mean estradiol and estrone levels of 60 to 140 pg/mL and 45 to 155 pg/mL. [15]
Doses of estradiol of as high as 200 mg per day by intramuscular injection for several weeks have been administered to humans in studies. [141] [142] Serious adverse effects have not been described following acute overdose of large doses of estrogen- and progestogen-containing birth control pills by small children. [102]
Likewise, other studies found that levels of estradiol and estrone are very similar after oral administration of roughly equimolar doses of estradiol (1.5 mg) and estradiol valerate (2 mg). [110] [111] [112] A study of high-dose oral estradiol valerate found levels of estradiol of about 250 pg/mL after a single 10-mg dose in three women. [107]
0.5–5 mg/day Various: Estrogen: SC implant: 50–200 mg every 6–24 mos Estradiol valerate: Progynova: Estrogen: Oral: 2–10 mg/day Progynova: Estrogen: Sublingual: 1–8 mg/day Delestrogen [c] Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol cypionate: Depo-Estradiol: Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks ...
100 mg 1x/6 months Footnotes: a = No longer used or recommended, due to health concerns. b = As a single patch applied once or twice per week (worn for 3–4 days or 7 days), depending on the formulation.
Estradiol cypionate is usually used at a dosage of 1 to 5 mg by intramuscular injection every 3 to 4 weeks in the treatment of menopausal symptoms such as hot flashes and vaginal atrophy, at a dosage of 1.5 to 2 mg by intramuscular injection once a month in the treatment of female hypoestrogenism due to hypogonadism, and at a dosage of 2 to 10 ...
Conjugated estrogens (Premarin) – 25 mg/vial; Estradiol cypionate (Depo-Estradiol, Estradiol Cypionate) – 5 mg/mL (1 mg/mL and 3 mg/mL discontinued) Estradiol valerate (Delestrogen, Estradiol Valerate) – 10 mg/mL, 20 mg/mL, 40 mg/mL; Polyestradiol phosphate (Estradurin) was previously available in the U.S. but was discontinued.
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