Estradiol
Unchecked
Estradiol (17β-estradiol)
Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol)
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Summary
Common uses
Vasomotor menopausal symptoms0, Genitourinary syndrome of menopause0, Hypoestrogenism (e.g., POI, post-oophorectomy)0, Osteoporosis prevention0, Feminizing hormone therapy0
Pharmacy
Starting dose
Oral 1-2 mg daily; transdermal patch 0.025-0.05 mg/d twice weekly; transdermal gel 0.5-1 g/d; vaginal 10 mcg tablet twice weekly for GSM. Always combine with a progestogen in patients with an intact uterus.
Preparations
Oral 0.5, 1, 2 mg tablets; transdermal patches (twice-weekly and once-weekly); 0.06% gel; 1.53 mg/spray topical; vaginal ring (Estring); vaginal tablet (Vagifem/Yuvafem); vaginal cream
US FDA Max
Indication-specific; lowest effective dose for shortest duration is the WHI-era standard
Pharmacology
Routes
Oral, transdermal, vaginal, IM (estradiol valerate, cypionate)
Onset
Vasomotor relief 2-4 weeks; bone density gains over months
Duration
Route- and formulation-dependent
Half-life
~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing[1]
Bioavailability
Oral ~5% (extensive first-pass to estrone and conjugates); transdermal bypasses first-pass, giving more physiologic estradiol:estrone ratio[1]
Pregnancy
Contraindicated in pregnancy (use is not appropriate during gestation; class label X). Lactation considerations vary by indication.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Estradiol is the principal endogenous estrogen; it binds nuclear estrogen receptors ERα and ERβ to regulate transcription of genes governing reproductive tissue maintenance, bone turnover, lipid metabolism, vascular function, and central thermoregulation.0 Transdermal routes avoid hepatic first-pass and the resulting increase in clotting-factor synthesis, reducing VTE risk relative to oral therapy. The Women's Health Initiative established the now-standard "lowest effective dose for the shortest necessary duration" framing of menopausal HRT[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Estrace (estradiol), Allergan, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/004511s175lbl.pdf