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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]
Estradiol: 0.5 mg/day: 1–1.5 mg/day: 2–3 mg/day Vaginal: Estradiol: 25 μg/day – – Estriol: 30 μg/day: 0.5 mg 2x/week: 0.5 mg/day IM Tooltip Intramuscular or SC injection: Estradiol valerate – – 4 mg 1x/4 weeks Estradiol cypionate: 1 mg 1x/3–4 weeks: 3 mg 1x/3–4 weeks: 5 mg 1x/3–4 weeks Estradiol benzoate: 0.5 mg 1x/week: 1 ...
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]
An example pseudopregnancy regimen in women which has been used in clinical studies is intramuscular injections of 40 mg/week estradiol valerate and 250 mg/week hydroxyprogesterone caproate. [3] It has been found to result in estradiol levels of about 3,100 pg/mL at 3 months of therapy and 2,500 pg/mL at 6 months of therapy. [3]
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 ...
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 ...
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