Estradiol
Unchecked
From Pharmacopedia
More actions
Estradiol (17β-estradiol)
Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol)
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
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- ↑ 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