estrogen
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Introduction
Many estrogens have been described.
The most common forms are:
- estrone [E1]
- estradiol (17-beta estradiol) [E2]
- estriol [E3])
estrogens present in maternal circulation are predominantly derived from fetal DHEA sulfate which is hydrolyzed & metabolized to estrogens in placenta
Pharmacokinetics
- 1st pass metabolism in liver
- conjugated in liver, excreted in the bile
- deconjugated by gut bacteria -> enterohepatic circulation
Adverse effects
- increased risk of thromboembolic events*
- increased risk of endometrial carcinoma if administered without progestin
- increased growth of estrogen-dependent tumors
- may increase risk of stroke*
- urinary incontinence (oral estrogens increase risk of & exacerbate urinary incontinence)[4]
* mediated through 1st pass metabolism in liver; transdermal estrogen may not increase risk[5][6]
# Questionable beneficial effect on coronary atherosclerosis
Laboratory
Mechanism of action
- improvement in lipoprotein profile*#
- estrogen acts directly on coronary arteries inducing vasodilation*
- enhanced bone mineral density in postmenopausal women (antiresorptive)
- estrogens presumably inhibit osteoclast activity
- may improve mood
- may diminish risk of osteoarthritis of the hip[4]
- may increase serum 25-OH vitamin D[7]
More general terms
More specific terms
- 17-beta estradiol (E2, Estrace, Estinyl, Delestrogen, Elestrin, Evamist, Imvexxy)
- catechol estrogen
- chlorotrianisene (Tace)
- clomiphene; clomiphene citrate (Clomid, Serophene)
- conjugated estrogens (Premarin)/methyltestosterone Estratest
- conjugated estrogens (Premarin, Enjuvia, Cenestin)
- dienestrol (DV cream, Cycladiene)
- diethylstilbestrol; DES (Stilphostol)
- esterified estrogens (Menest, Estrab)
- estetrol (E4)
- estramustine (Emcyt)
- estriol (E3)
- estrogen patch
- estrone (E1)
- estropipate; piperazine estrone sulfate (Ogen, Ortho-Est)
- ethinyl estradiol
- mestranol (Inostral)
- phytoestrogen
- zeranol; zearalanol
Additional terms
- androgen or anabolic steroid
- estrogen deficiency
- estrogen receptor
- estrogens in serum
- hormone replacement therapy (HRT); estrogen replacement therapy; postmenopausal hormone replacement therapy
Component of
References
- ↑ Journal Watch 20(18):141, 2000 Harrington et al N Engl J Med 343:522, 2000
- ↑ Journal Watch 21(3):28, 2001 Grodstein et al Ann Intern Med 133:933, 2000 Grady & Hulley Ann Intern Med 133:999, 2000
- ↑ 3.0 3.1 Journal Watch 21(9):72, 2001 Rodriguez et al, JAMA 285:1460, 2001
- ↑ 4.0 4.1 4.2 Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004; 7th edition 2010
- ↑ 5.0 5.1 Canonico M et al. Postmenopausal hormone therapy and risk of idiopathic venous thromboembolism: Results from the E3N cohort study. Arterioscler Thromb Vasc Biol 2010 Feb; 30:340. PMID: https://www.ncbi.nlm.nih.gov/pubmed/19834106
Cushman M. Patch instead of pill: A safer menopausal estrogen? Arterioscler Thromb Vasc Biol 2010 Feb; 30:136 PMID: https://www.ncbi.nlm.nih.gov/pubmed/20089948 - ↑ 6.0 6.1 Renoux C et al. Transdermal and oral hormone replacement therapy and the risk of stroke: A nested case-control study. BMJ 2010 Jun 3; 340:c2519 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20525678 <Internet> http://dx.doi.org/10.1136/bmj.c2519
- ↑ 7.0 7.1 Harmon QE, Umbach DH, Baird DD Use of Estrogen-Containing Contraception Is Associated With Increased Concentrations of 25-Hydroxy Vitamin D. J Clin Endocrinol Metab 101: Aug, 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27490916 <Internet> http://press.endocrine.org/doi/pdf/10.1210/jc.2016-1658