II. Physiology
- See Estradiol
III. Symptoms: Excess Estrogen (e.g. Premenstrual Syndrome)
IV. Pharmacokinetics: Relative Potency
- Ethinyl Estradiol: 100
- Mestranol: 67
V. Precautions
- Mestranol is potentially a carcinogen (animal studies)
- MI, CVA, DVT, PE and Breast Cancer risk are all FDA Black box warnings
VI. Preparations: Hormone Replacement Dosages (unless otherwise noted)
- Micronized Estradiol (Estrace)
- Take 1 to 2 mg orally daily
- Ethinyl Estradiol
- Oral Contraceptive: 0.03 to 0.10 mg/day (primary use)
- Hormone Replacement: 0.005 to 0.02 mg/day
- Other Estrogen formulations are typically used for Hormone Replacement
-
Estradiol Cypionate (Depo-Estradiol)
- Inject 1 to 5 mg IM every 3-4 weeks
-
Estradiol valerate (Delestrogen)
- Inject 2-20 mg IM every other week
- Also found in some Oral Contraceptives
- Estropipate (1.25-2.5 mg/day)
- Conjugated Estrogen (e.g. Premarin, Enjuvia)
- Oral (0.3-1.25 mg/day)
- Injectable (0.2-2 mg/day)
- Transdermal
- Diethylstilbestrol (0.1-0.5 mg/day)
- Quinestrol (0.1-0.2 mg/week)
- Chlorotrianisene (12-25 mg/day)
- Methallenestril (3-9 mg/day)
- Esterified Estrogen (Menest): 0.3 to 1.25 mg/day
VII. Preparations: Native Estrogen with Selective Actions in Tissues (NEST)
- Background
- Native Estrogen with Selective Actions in Tissues (NEST) are plant-derived Estrogens (Phytoestrogens)
- Low potency and therefore 1000-fold higher doses are required (measured in mg NOT mcg)
- Nextstellis contains 14.2 mg of Estetrol, while most OCPs contain 20-30 mcg Ethinyl Estradiol
- Estetrol (E4)
- Estetrol is a new plant-derived Estrogen (E4) formulation available in 2021 as component of Nextstellis OCP
- Carries same Estrogen-related effects and contraindications
- References
- (2021) Presc Lett 28(7): 38