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A dosage of 1 mg/day oral estradiol valerate has been found to produce approximate circulating concentrations of 50 pg/mL estradiol and 160 pg/mL estrone, while a dosage of 2 mg/day results in circulating levels of 60 pg/mL estradiol and 300 pg/mL estrone. [108]
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]
Transdermal gel: 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. ...
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.
[26] [35] Aside from estradiol cypionate, the only other injectable estrogen formulations that remain available in the United States are estradiol valerate (10 mg/mL, 20 mg/mL, and 40 mg/mL in oil) and conjugated estrogens (25 mg/vial in solution). [26]
TD gel: 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 ...
Transdermal gel: 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. ...
Estradiol is not produced in the gonads only; in particular, fat cells produce active precursors to estradiol, and will continue to do so even after menopause. [51] Estradiol is also produced in the brain and in arterial walls. In men, approximately 15 to 25% of circulating estradiol is produced in the testicles.
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