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Name: Estradiol

Pregnancy Category X

Drug classes

  • Hormone
  • Estrogen

Therapeutic actions

Estradiol is the most potent endogenous female sex hormone. Estrogens are important in the development of the female reproductive system and secondary sex characteristics; affect the release of pituitary gonadotropins; cause capillary dilatation, fluid retention, protein anabolism and thin cervical mucus; conserve calcium and phosphorus and encourage bone formation; inhibit ovulation and prevent postpartum breast discomfort. They are responsible for the proliferation of the endometrium; absence or decline of estrogen produces signs and symptoms of menopause on the uterus, vagina, breasts, cervix; efficacy as palliation in male patients with androgen-dependent prostatic carcinoma; is attributable to their competition with androgens for receptor sites, thus decreasing the influence of androgens.


  • Palliation of moderate to severe vasomotor symptoms, atrophic vaginitis or kraurosis vulvae associated with menopause (estradiol oral, transdermal, cream, estradiol valerate)
  • Treatment of female hypogonadism, female castration, primary ovarian failure (estradiol oral, transdermal, estradioll cypionate, valerate)
  • Palliation of inoperable prostatic cancer (estradiol oral, estradiol valerate)
  • Palliation of inoperable, progressing breast cancer (estradiol oral)
  • Prevention of postpartum breast engorgement (estradiol valerate)


Contraindicated in the presence of allergy to estrogens, allergy to tartrazine (in 2-mg oral tablets), breast cancer (except in specific, selected patients), estrogen-dependent neoplasm, undiagnosed abnormal genital bleeding, active thrombophlebitis or thromboembolic disorders or
history of such from previous estrogen use, pregnancy (associated with serious fetal defects; women of childbearing ageshould be advised of the potential risks and birth control measures suggested).

Use caution in the presence of metabolic bone disease, renal insufficiency, CHF, lactation.

Adverse effects

  • CNS: Steepening of the corneal curvature with a resultant change in visual acuity and intolerance to contact lenses, headache, migraine, dizziness, mental depression, chorea, convulsions
  • GI: Gallbladder disease (in postmenopausal women), hepatic adenoma, nausea, vomiting, abdominal cramps, bloating, cholestatic jaundice, colitis, acute pancreatitis
  • CV: Increased blood pressure, thromboembolic and thrombotic disease
  • Hematologic: Hypercalcemia, decreased glucose tolerance
  • GU: Increased risk of endometrial cancer in postmenopausal women, breakthrough bleeding, change in menstrual flow, dysmenorrhea, premenstrual-like syndrome, amenorrhea, vaginal candidiasis, cystitis-like syndrome, endometrial cystic hyperplasia
  • Dermatologic: Photosensitivity, peripheral edema, chloasma, erythema nodosum or multiforme, hemorrhagic eruption, loss of scalp hair, hirsutism, urticaria, dermatitis
  • Local: Pain at injection site, sterile abscess, postinjection flare
  • Other: Weight changes, reduced carbohydrate tolerance, aggravation of por-phyria, edema, changes in libido, breast tenderness

Topical Vaginal Cream

  • Systemic absorption may cause uterine bleeding in menopausal women and may cause serious bleeding of remaining endometrial foci in sterilized women with endometriosis.

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