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estradiol
generic
Black Box Warnings .
Endometrial Cancer Risk
unopposed estrogen use incr. risk if intact uterus; adding progestin may decr. risk of endometrial hyperplasia (possible precursor to endometrial CA); use adequate diagnostic measures such as endometrial sampling to rule out malignancy if undiagnosed persistent or recurrent abnormal genital bleeding
Cardiovascular and Other Risks
estrogens +/- progestins not indicated for cardiovascular dz or dementia prevention; incr. risk of stroke and DVT (from WHI estrogen-alone substudy) and MI, stroke, PE/DVT, and invasive breast CA (from WHI estrogen/progestin substudy) in postmenopausal pts; incr. risk of probable dementia in postmenopausal pts 65 yo and older on a WHI regimen x4-5y; WHI regimens = conj. estrogens 0.625 mg/day w/ or w/o medroxyprogesterone 2.5 mg/day, other doses or estrogen/progestin combos not studied, but assume similar risk; use lowest effective estrogen dose, shortest duration based on individual tx goals and risks
Adult Dosing .
Dosage forms: TAB: 0.5 mg, 1 mg, 2 mg
vasomotor sx, mod-severe menopausal
- [1-2 mg PO qd]
- Info: cycle 21 days on, 7 days off; add progestin x10-14 days/4wk cycle if intact uterus; use lowest effective estrogen dose, shortest effective tx duration
vulvovaginal atrophy, menopausal
- [1-2 mg PO qd]
- Info: cycle 21 days on, 7 days off; add progestin x10-14 days/4wk cycle if intact uterus; use lowest effective estrogen dose, shortest effective tx duration; not preferred if local sx only
osteoporosis prevention, postmenopausal
- [0.5 mg PO qd]
- Info: cycle 21 days on, 7 days off; add progestin x10-14 days/4wk cycle if intact uterus; weigh estrogen tx risk/benefit
hypoestrogenism
- [2-4 mg PO qd]
- Info: for hypogonadism, oophorectomy, or primary ovarian failure; titrate to lowest effective maint. dose; add progestin if intact uterus
metastatic breast CA, palliative tx
- [10 mg PO tid for at least 3mo]
advanced prostate CA, palliative tx
- [1-2 mg PO tid]
transgender hormone therapy, feminizing (off-label)
- [2-6 mg/day PO divided qd-bid]
- Alt: 2-6 mg/day SL divided qd-bid; Info: adjust dose based on pt tx goals, clinical response, and estradiol levels; refer to WPATH or Endocrine Society guidelines
renal dosing
- [see below]
- renal dz: not defined, caution advised
- HD/PD: not defined, caution advised
hepatic dosing
- [see below]
- hepatic impairment: contraindicated
Peds Dosing .
- Dosage forms: TAB: 0.5 mg, 1 mg, 2 mg
puberty induction, female (off-label)
- [associated w/ hypogonadism, 11 yo and older]
- Dose: 2-4 mg PO qd; Start: 0.25 mg PO qd x6mo, then incr. to 0.5 mg PO qd x6mo, then incr. by 0.5 mg/day PO q6-12mo; Alt: start 5 mcg/kg/dose PO qd, then incr. by 2.5 mcg/kg/day PO q6-12mo; Max: 4 mg/day; Info: add progesterone micronized or medroxyprogesterone after breakthrough bleeding occurs w/ at least 2y of estrogen tx if intact uterus; after puberty induction, titrate to lowest effective maint. dose for hypoestrogenism until menopausal age
- [associated w/ constitutional causes, 13 yo and older]
- Dose: 0.25-0.5 mg PO qd x3-6mo; Alt: 5-10 mcg/kg/dose PO qd x3-6mo; Info: may incr. dose after 6mo if spontaneous puberty progression not achieved; reassess tx need q3-6mo
renal dosing
- [not defined]
- renal impairment: consider adult renal dosing for guidance
- HD/PD: consider adult renal dosing for guidance
hepatic dosing
- [not defined]
- hepatic impairment: consider adult hepatic dosing for guidance