Estrogen

Aka: Estrogen, Ethinyl Estradiol, Mestranol, Conjugated Estrogen, Native Estrogen with Selective Actions in Tissues

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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 (unless otherwise noted)

  1. Micronized Estradiol (Estrace)
    1. Take 1 to 2 mg orally daily
  2. Ethinyl Estradiol
    1. Oral Contraceptive: 0.03 to 0.10 mg/day (primary use)
    2. Hormone Replacement: 0.005 to 0.02 mg/day
      1. Other Estrogen formulations are typically used for Hormone Replacement
  3. Estradiol Cypionate (Depo-Estradiol)
    1. Inject 1 to 5 mg IM every 3-4 weeks
  4. Estradiol valerate (Delestrogen)
    1. Inject 2-20 mg IM every other week
    2. Also found in some Oral Contraceptives
  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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