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Template:Composition of conjugated estrogens and properties of constituents

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Composition of conjugated estrogens and properties of constituents
Compound Synonym Proportion (%) Relative potency
in the vagina (%)
Relative potency
in the uterus (%)
RBATooltip Relative binding affinity for
ERα (%)
RBA for
ERβ (%)
ERα / ERβ
RBA ratio
Conjugated estrogens 100 38 100
Estrone 49.1–61.5 30 32 26 52 0.50
Equilin Δ7-Estrone 22.4–30.5 42 80 13 49 0.26
17α-Dihydroequilin Δ7-17α-Estradiol 13.5–19.5 0.06 2.6 41 32 1.30
17α-Estradiol 2.5–9.5 0.11 3.5 19 42 0.45
Δ8-Estrone 3.5–3.9 ? ? 19 32 0.60
Equilenin Δ6,8-Estrone 2.2–2.8 1.3 11.4 15 20–29 0.50–0.75
17β-Dihydroequilin Δ7-17β-Estradiol 0.5–4.0 83 200 113 108 1.05
17α-Dihydroequilenin Δ6,8-17α-Estradiol 1.2–1.6 0.018 1.3 20 49 0.40
17β-Estradiol 0.56–0.9 100 ? 100 100 1.00
17β-Dihydroequilenin Δ6,8-17β-Estradiol 0.5–0.7 0.21 9.4 68 90 0.75
Δ8-17β-Estradiol Small amounts ? ? 68 72 0.94
Notes: All listed compounds are present in conjugated estrogen products specifically in the form of the sodium salts of the sulfate esters (i.e., as sodium estrone sulfate, sodium equilin sulfate, etc.).[1][2] Sources: [1][3][2][4][5]

References

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  1. ^ a b Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.
  2. ^ a b Marc A. Fritz; Leon Speroff (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 751–. ISBN 978-1-4511-4847-3.
  3. ^ Bhavnani BR, Stanczyk FZ (July 2014). "Pharmacology of conjugated equine estrogens: efficacy, safety and mechanism of action". J. Steroid Biochem. Mol. Biol. 142: 16–29. doi:10.1016/j.jsbmb.2013.10.011. PMID 24176763.
  4. ^ Sweetman, Sean C., ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2087. ISBN 978-0-85369-840-1.
  5. ^ Bhavnani BR, Tam SP, Lu X (October 2008). "Structure activity relationships and differential interactions and functional activity of various equine estrogens mediated via estrogen receptors (ERs) ERalpha and ERbeta". Endocrinology. 149 (10): 4857–70. doi:10.1210/en.2008-0304. PMID 18599548.