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Hormonal antineoplastic drugs
Esterified estrogens
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    Esterified estrogens

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    Not to be confused with Estrogen ester or Conjugated estrogens.
    Esterified estrogens
    Estrone sulfate.svg
    Estrone sulfate, the primary active component in esterified estrogens (constitutes about 75 to 85% of total content).
    Equilin sulfate.svg
    Equilin sulfate, the second most major active component in esterified estrogens (constitutes about 6 to 16% of total content).
    Combination of
    Sodium estrone sulfate Estrogen
    Sodium equilin sulfate Estrogen
    Clinical data
    Trade names Estratab, Menest, others
    Other names Esterified oestrogens; EEs; Esterified equine estrogens; Esterified equine oestrogens; EEEs
    Routes of
    administration    		 By mouth
    Drug class Estrogen
    ATC code
    • None
    Identifiers
    PubChem SID
    DrugBank
    UNII

    Esterified estrogens (EEs), sold under the brand names Estratab and Menest among others, is an estrogen medication which is used hormone therapy for menopausal symptoms and low sex hormone levels in women, to treat breast cancer in both women and men, and to treat prostate cancer in men. It is formulated alone or in combination with methyltestosterone. It is taken by mouth.

    Side effects of EEs include nausea, breast tension, edema, and breakthrough bleeding among others. It is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. EEs are a prodrug mainly of estradiol and to a lesser extent of equilin.

    EEs were introduced for medical use by 1970. They are available in only a few countries, such as Chile and the United States. They have also been marketed in Argentina and Switzerland in the past.

    Medical uses

    EEs are used in hormone therapy for menopausal symptoms, female hypogonadism, ovariectomy, and primary ovarian failure and in the treatment of breast cancer and prostate cancer.

    Estrogen dosages for menopausal hormone therapy
    Route/form Estrogen Low Standard High
    Oral Estradiol 0.5–1 mg/day 1–2 mg/day 2–4 mg/day
    Estradiol valerate 0.5–1 mg/day 1–2 mg/day 2–4 mg/day
    Estradiol acetate 0.45–0.9 mg/day 0.9–1.8 mg/day 1.8–3.6 mg/day
    Conjugated estrogens 0.3–0.45 mg/day 0.625 mg/day 0.9–1.25 mg/day
    Esterified estrogens 0.3–0.45 mg/day 0.625 mg/day 0.9–1.25 mg/day
    Estropipate 0.75 mg/day 1.5 mg/day 3 mg/day
    Estriol 1–2 mg/day 2–4 mg/day 4–8 mg/day
    Ethinylestradiola 2.5–10 μg/day 5–20 μg/day –
    Nasal spray Estradiol 150 μg/day 300 μg/day 600 μg/day
    Transdermal patch Estradiol 25 μg/dayb 50 μg/dayb 100 μg/dayb
    Transdermal gel Estradiol 0.5 mg/day 1–1.5 mg/day 2–3 mg/day
    Vaginal Estradiol 25 μg/day – –
    Estriol 30 μg/day 0.5 mg 2x/week 0.5 mg/day
    IM or SC injection Estradiol valerate – – 4 mg 1x/4 weeks
    Estradiol cypionate 1 mg 1x/3–4 weeks 3 mg 1x/3–4 weeks 5 mg 1x/3–4 weeks
    Estradiol benzoate 0.5 mg 1x/week 1 mg 1x/week 1.5 mg 1x/week
    SC implant Estradiol 25 mg 1x/6 months 50 mg 1x/6 months 100 mg 1x/6 months
    Footnotes: a = No longer used or recommended, due to health concerns. b = As a single patch applied once or twice per week (worn for 3–4 days or 7 days), depending on the formulation. Note: Dosages are not necessarily equivalent. Sources: See template.

    Available forms

    EEs are available in the form of 0.3 mg, 0.625 mg, 1.25 mg, and 2.5 mg oral tablets.Estratest is a combination formulation of 1.25 mg EEs with 2.5 mg methyltestosterone.

    Side effects

    See also: Conjugated estrogens § Side effects, and Estrogen (medication) § Side effects

    Pharmacology

    See also: Pharmacodynamics of estradiol and Pharmacokinetics of estradiol

    EEs consist primarily of sodium estrone sulfate and sodium equilin sulfate, and are very similar to conjugated estrogens (CEEs, conjugated equine estrogens; brand name Premarin). However, EEs and CEEs differ in the sources of their contents and in the percentages of their constituents; CEEs consist of approximately 53% sodium estrone sulfate and 25% sodium equilin sulfate, while EEs contain about 75 to 85% sodium estrone sulfate and 6 to 11% sodium equilin sulfate. EEs have been found to produce similar serum levels of estrone and estradiol relative to CEEs, although with higher levels of estrone and lower levels of equilin. One study found that the risk of venous thrombosis may be less with EEs relative to CEEs.

    Relative oral potencies of estrogens
    Estrogen HF VE UCa FSH LH HDL-C SHBG CBG AGT Liver
    Estradiol 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0
    Estrone ? ? ? 0.3 0.3 ? ? ? ? ?
    Estriol 0.3 0.3 0.1 0.3 0.3 0.2 ? ? ? 0.67
    Estrone sulfate ? 0.9 0.9 0.8–0.9 0.9 0.5 0.9 0.5–0.7 1.4–1.5 0.56–1.7
    Conjugated estrogens 1.2 1.5 2.0 1.1–1.3 1.0 1.5 3.0–3.2 1.3–1.5 5.0 1.3–4.5
    Equilin sulfate ? ? 1.0 ? ? 6.0 7.5 6.0 7.5 ?
    Ethinylestradiol 120 150 400 60–150 100 400 500–600 500–600 350 2.9–5.0
    Diethylstilbestrol ? ? ? 2.9–3.4 ? ? 26–28 25–37 20 5.7–7.5
    Sources and footnotes
    Notes: Values are ratios, with estradiol as standard (i.e., 1.0). Abbreviations: HF = Clinical relief of hot flashes. VE = Increased proliferation of vaginal epithelium. UCa = Decrease in UCa. FSH = Suppression of FSH levels. LH = Suppression of LH levels. HDL-C, SHBG, CBG, and AGT = Increase in the serum levels of these liver proteins. Liver = Ratio of liver estrogenic effects to general/systemic estrogenic effects (hot flashes/gonadotropins). Sources: See template.
    Protein binding and metabolic clearance rates of estrogens
    Compound RBA to
    SHBG (%)    		 Bound to
    SHBG (%)    		 Bound to
    albumin (%)    		 Total
    bound     (%)    		 MCR
    (L/day/m2)
    17β-Estradiol 50 37 61 98 580
    Estrone 12 16 80 96 1050
    Estriol 0.3 1 91 92 1110
    Estrone sulfate 0 0 99 99 80
    17β-Dihydroequilin 30 ? ? ? 1250
    Equilin 8 26 13 ? 2640
    17β-Dihydroequilin sulfate 0 ? ? ? 375
    Equilin sulfate 0 ? ? ? 175
    Δ8-Estrone ? ? ? ? 1710
    Notes: RBA for SHBG (%) is compared to 100% for testosterone. Sources: See template.

    Chemistry

    See also: List of estrogens, Estrogen ester, and List of estrogen esters

    EEs contain synthetic, plant-derived estrogens and are manufactured from soybeans and yams.

    History

    EEs were introduced for medical use by 1970.

    Society and culture

    Generic names

    Estrogens, esterified is the generic name of the drug and its USP. It is also known as esterified estrogens.

    Brand names

    EEs are marketed under a variety of brand names including Amnestrogen, Estragyn, Estratab, Evex, Femibel, Femogen, Menest, Neo Estrone Tab, and Oestro-Feminal alone, and, in combination with methyltestosterone, under the brand names Covaryx, Delitan, Eemt, Essian, Estratest, Feminova-T, Menogen, and Syntest.

    Availability

    See also: List of estrogens available in the United States

    EEs are or have been marketed in Argentina, Chile, Switzerland, and the United States. Both EEs and the combination of EEs and methyltestosterone are listed as being marketed only in Chile and the United States as of present.

    See also



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