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Name: Premarin
Pregnancy Category X
Drug classes
Therapeutic actions
Estrogens are endogenous female sex hormones important in the
development
of the female reproductive system and secondary sex characteristics.
They
affect the release of pituitary gonadotropins; cause capillary
dilatation, fluid retention, protein anabolism, and thin cervical
mucus;
conserve calcium and phosphorus; 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. Their 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
- Oral: palliation of moderate to severe vasomotor symptoms, atrophic
vaginitis, or kraurosis vulvae associated with menopause
- Treatment of female hypogonadism; female castration; primary ovarian
failure
- Osteoporosis: to retard progression
- Palliation of inoperable prostatic cancer
- Palliation of mammary cancer
- Prevention of postpartum breast engorgement
- Unlabeled use: postcoital contraceptive
- Parenteral: treatment of uterine bleeding due to hormonal imbalance in
the absence of organic pathology
- Vaginal cream: treatment of atrophic vaginitis and kraurosis vulvae
associated with menopause
Contraindications/cautions
Contraindicated in the presence of allergy to estrogens, 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
age should 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
porphyria, 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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