II. Physiology

  1. See Estradiol

III. Symptoms: Excess Estrogen (e.g. Premenstrual Syndrome)

  1. Swollen or engorged Breast tenderness
  2. Water retention
  3. Irritability
  4. Headaches
  5. Visual disturbance
  6. Memory difficulty
  7. Sweet craving

IV. Pharmacokinetics: Relative Potency

  1. Ethinyl Estradiol: 100
  2. Mestranol: 67

V. Precautions

  1. Mestranol is potentially a carcinogen (animal studies)
  2. MI, CVA, DVT, PE and Breast Cancer risk are all FDA Black box warnings

VI. Preparations: Hormone Replacement Dosages (uncless otherwise noted)

  1. Ethinyl Estradiol
    1. Hormone Replacement: 0.005 to 0.02 mg/day
    2. Oral Contraceptive: 0.03 to 0.10 mg/day
  2. Micronized Estradiol (1-2 mg/day)
  3. Estradiol Cypionate (2-5 mg every 3-4 weeks)
  4. Estradiol valerate (2-20 mg every other week)
  5. Estropipate (1.25-2.5 mg/day)
  6. Conjugated Estrogen (e.g. Premarin, Enjuvia)
    1. Oral (0.3-1.25 mg/day)
    2. Injectable (0.2-2 mg/day)
    3. Transdermal
  7. Diethylstilbestrol (0.1-0.5 mg/day)
  8. Quinestrol (0.1-0.2 mg/week)
  9. Chlorotrianisene (12-25 mg/day)
  10. Methallenestril (3-9 mg/day)
  11. Esterified Estrogen (Menest): 0.3 to 1.25 mg/day

VII. Preparations: Native Estrogen with Selective Actions in Tissues (NEST)

  1. Background
    1. Native Estrogen with Selective Actions in Tissues (NEST) are plant-derived Estrogens (Phytoestrogens)
    2. Low potency and therefore 1000-fold higher doses are required (measured in mg NOT mcg)
      1. Nextstellis contains 14.2 mg of Estetrol, while most OCPs contain 20-30 mcg Ethinyl Estradiol
  2. Estetrol (E4)
    1. Estetrol is a new plant-derived Estrogen (E4) formulation available in 2021 as component of Nextstellis OCP
    2. Carries same Estrogen-related effects and contraindications
  3. References
    1. (2021) Presc Lett 28(7): 38

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Related Studies

Cost: Medications

estrogen (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing)

Ontology: Estrogens (C0014939)

Definition (NCI_NCI-GLOSS) A type of hormone made by the body that helps develop and maintain female sex characteristics and the growth of long bones. Estrogens can also be made in the laboratory. They may be used as a type of birth control and to treat symptoms of menopause, menstrual disorders, osteoporosis, and other conditions.
Definition (NCI) A class of natural or synthetic hormones that binds to a cytoplasmic receptor and initiates translocation of the hormone-receptor complex to the nucleus of target cells of tissues rich in estrogen receptors, including the endometrium, myometrium, oviduct, vagina, fallopian tube, cervix, brain, liver, placenta, ovarian cells, Leydigs cells, kidney, prostate, pancreas, heart, and skin. (NCI)
Definition (MSH) Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
Definition (CSP) hormones which stimulate the female reproductive organs, and the development of secondary female sex characteristics.
Concepts Steroid (T110) , Pharmacologic Substance (T121) , Hormone (T125)
MSH D004967
SnomedCT 325478009, 41598000, 61946003
LNC LP14661-0, MTHU003480
English Estrogen, Estrogens, estrogens (medication), estrogens, oestrogen products, oestrogens, estrogen products, oestrogen, estrogen substance, estrogenic preparation, Estrogens (product), Agonists, Estrogen Receptor, Receptor Agonists, Estrogen, Estrogen Receptor Agonists, Compounds, Estrogenic, Estrogenic Compounds, Agents, Estrogenic, Estrogenic Agents, Estrogen product, Oestrogen product, Oestrogen, Estrogen (substance), Estrogenic drug, Estrogenic preparation (product), Estrogenic preparation, Oestrogenic drug, Oestrogenic preparation, estrogen, Estrogen preparation, NOS, Estrogen, NOS, Estrogenic drug, NOS, Oestrogen preparation, NOS, Oestrogen, NOS, Oestrogenic drug, NOS, Estrogenic preparation (substance), Estrogens (substance), Oestrogens, Therapeutic Estrogen, ESTROGENS
French Composés oestrogéniques, Composés estrogéniques, Agents estrogéniques, Agents oestrogéniques, Estrogènes, Oestrogènes
Swedish Östrogener
Czech estrogeny
Finnish Estrogeenit
Italian Composti estrogenici, Estrogeno, Sostanze estrogeniche, Estrogeni
Japanese エストロゲン, 卵胞ホルモン, 卵胞ホルモン類, 発性ホルモン物質, 発情ホルモン, エストロジェン
Polish Estrogeny
Norwegian Østrogen
Spanish estrógenos (producto), estrógenos, Efecto Estrógeno, droga estrogénica, estrógeno (sustancia), estrógeno, preparado estrogénico (producto), preparado estrogénico (sustancia), preparado estrogénico, Estrógenos
Portuguese Estrógenos, Efeito Estrogênio, Estrogênios
German Östrogene

Ontology: Mestranol (C0025506)

Definition (NCI) A semisynthetic estrogen. Metabolized by the liver to ethynyl estradiol, mestranol serves as the estrogen component in several combination oral contraceptives. (NCI04)
Definition (MSH) The 3-methyl ether of ETHINYL ESTRADIOL. It must be demethylated to be biologically active. It is used as the estrogen component of many combination ORAL CONTRACEPTIVES.
Concepts Pharmacologic Substance (T121) , Steroid (T110)
MSH D008656
SnomedCT 326365002, 126096002, 395785001, 77885004
English Ethinyl Estradiol 3-Methyl Ether, Mestranol, mestranol, 19-Norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-methoxy-, (17alpha)-, Mestranol [contraceptive], (17alpha)-3-Methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17-ol, ETHINYL ESTRADIOL METHYL ETHER 03, Mestranol [combined oral contraceptive], MESTRANOL, oral contraceptives mestranol preparations, mestranol preparations (medication), mestranol preparations, Mestranol [Chemical/Ingredient], Ethinyl Estradiol 3 Methyl Ether, Mestranol [combined oral contraceptive] (product), Mestranol (product), Mestranol product, Mestranol (substance), Mestranol preparation (product), Mestranol preparation, Mestranol preparation, NOS, Mestranol [combined oral contraceptive] (substance), Mestranol preparation (substance)
French Éthinyl oestradiol 3-méthyl éther, Mestranol
Swedish Mestranol
Czech mestranol
Finnish Mestranoli
Japanese エチニルエストラジオール3-メチルエーテル, メストラノール
Spanish preparado con mestranol (producto), mestranol (producto), preparado con mestranol, mestranol (anticonceptivo oral combinado), mestranol (anticonceptivo oral combinado) (producto), mestranol (sustancia), mestranol, preparado de mestranol (sustancia), Mestranol, Éter 3-Metil del Etinil Estradiol
Polish Mestranol
Norwegian Etinyløstradiol 3-metyleter, Mestranol
German Mestranol
Italian Mestranolo
Portuguese Etinil Estradiol 3-Metil Éter, Mestranol