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estrogen

Many estrogens have been described. The most common forms are: 1) estrone [E1] 2) estradiol (17-beta estradiol) [E2] 3) estriol [E3]) estrogens present in maternal circulation are predominantly derived from fetal DHEA sulfate which is hydrolyzed & metabolized to estrogens in placenta Pharmacology: Pharmacokinetics: 1) 1st pass metabolism in liver 2) conjugated in liver, excreted in the bile 3) deconjugated by gut bacteria -> enterohepatic circulation Adverse effects: 1) increased risk of thromboembolic events* 2) increased risk of endometrial carcinoma if administered without progestin 3) increased growth of estrogen-dependent tumors a) breast cancer b) ovarian cancer [3] 4) may increase risk of stroke* 5) 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: - estrogen in serum/plasma - estrogen in urine Mechanism of action: 1) improvement in lipoprotein profile*# 2) estrogen acts directly on coronary arteries inducing vasodilation* 3) enhanced bone mineral density in postmenopausal women 4) may improve mood 5) may diminish risk of osteoarthritis of the hip [4] 6) may increase serum 25-OH vitamin D [7]

Interactions

drug adverse effects of estrogens

Related

androgen or anabolic steroid estrogen deficiency estrogen receptor estrogens in serum hormone replacement therapy (HRT); estrogen replacement therapy; postmenopausal hormone replacement therapy

Specific

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

General

endocrine agent hormone

Figures/Diagrams

Physiologic Inhibitors of Apoptosis

Properties

References

  1. Journal Watch 20(18):141, 2000 Harrington et al N Engl J Med 343:522, 2000
  2. Journal Watch 21(3):28, 2001 Grodstein et al Ann Intern Med 133:933, 2000 Grady & Hulley Ann Intern Med 133:999, 2000
  3. Journal Watch 21(9):72, 2001 Rodriguez et al, JAMA 285:1460, 2001
  4. Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004; 7th edition 2010
  5. 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: 19834106 - Cushman M. Patch instead of pill: A safer menopausal estrogen? Arterioscler Thromb Vasc Biol 2010 Feb; 30:136 PMID: 20089948
  6. 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 PMID: 20525678 http://dx.doi.org/10.1136/bmj.c2519
  7. 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 PMID: 27490916 http://press.endocrine.org/doi/pdf/10.1210/jc.2016-1658

Component-of

estrogen/methyltestosterone tibolone