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. Medications: Hormone Replacement Dosages (unless otherwise noted)

  1. See Estrogen Replacement Therapy
  2. Micronized Estradiol (Estrace)
    1. Take 1 to 2 mg orally daily
  3. Estradiol transdermal patch (Climara, Minivelle, Vivelle-Dot)
    1. Apply 0.05 mg patch per week (or 0.025, 0.075 or 0.1 mg)
  4. Estradiol transdermal gel (Divigel, Elestrin, Estrogel)
    1. Apply 0.25, 0.5, 0.75 or 1.0 daily (depending on manufacturer)
  5. Evamist transdermal spray (1.53 per spray)
    1. Start with 1 spray daily and advance to max of 3 sprays daily based on response
  6. 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
  7. Estradiol Cypionate (Depo-Estradiol)
    1. Inject 1 to 5 mg IM every 3-4 weeks
  8. Estradiol valerate (Delestrogen)
    1. Inject 2-20 mg IM every other week
    2. Also found in some Oral Contraceptives
  9. Estropipate (1.25-2.5 mg/day)
  10. Conjugated Estrogen (e.g. Premarin, Enjuvia)
    1. Oral (0.3-1.25 mg/day)
    2. Injectable (0.2-2 mg/day)
    3. Transdermal
  11. Diethylstilbestrol (0.1-0.5 mg/day)
  12. Quinestrol (0.1-0.2 mg/week)
  13. Chlorotrianisene (12-25 mg/day)
  14. Methallenestril (3-9 mg/day)
  15. Esterified Estrogen (Menest): 0.3 to 1.25 mg/day

VII. Medications: 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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