Estrone sulfate, the primary active component in esterified estrogens (constitutes about 75 to 85% of total content).
Equilin sulfate, the second most major active component in esterified estrogens (constitutes about 6 to 16% of total content).
|Sodium estrone sulfate||Estrogen|
|Sodium equilin sulfate||Estrogen|
|Trade names||Estratab, Menest, others|
|Other names||Esterified oestrogens; EEs; Esterified equine estrogens; Esterified equine oestrogens; EEEs|
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.
|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 μg/day||5–15 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|
|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.|
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.
|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 (specifically hot flashes relief and gonadotropin suppression). Type: Bioidentical = Identical to those found in humans. Natural = Naturally occurring but not identical to those found in humans (e.g., estrogens of other species). Synthetic = Man-made, does not occur naturally in animals or in the environment. Sources: See template.|
|Notes: RBA for SHBG (%) is compared to 100% for testosterone. Sources: See template.|
EEs were introduced for medical use by 1970.
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.
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.