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Name:
Estradiol
Pregnancy Category X
Drug classes
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.
Indications
- 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)
Contraindications/cautions
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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