| ESTROGENS, ESTERIFIED
Estratab, Menest, Menrium, Neo-Estrone
Classifications: hormone; estrogen; Therapeutic: estrogen; female hormone replacement therapy (hrt)
Pregnancy Category: X
0.3 mg, 0.625 mg, 1.25 mg, 2.5 mg tablets
At the cellular level, estrogens increase cervical secretions, result in proliferation of the endometrium, and increase uterine
tone. Estrogens also can affect bone calcium deposition and accelerate epiphyseal closure. Estrogens appear to prevent osteoporosis
associated with the onset of menopause; they generally do not reverse bone density loss that has already developed.
Binds to intracellular receptors that stimulate DNA and RNA to synthesize proteins responsible for effects of estrogen.
Atrophic vaginitis, kraurosis vulvae and abnormal bleeding (hormonal imbalance), female hypogonadism, castration, primary
ovarian failure, vasomotor symptoms associated with menopause, palliative therapy of breast and prostatic carcinomas; prevention
Breast cancer; cervical cancer; endometrial cancer; endometrial hyperplasia; prostate cancer; hepatic disease or cancer;
hypercalcemia; lupus (SLE); history of thromboembolic disease; known or suspected pregnancy (category X); lactation.
Hypertension; gallbladder disease; diabetes mellitus; heart failure; kidney dysfunction; migraine headaches; seizure disorders.
Route & Dosage
Adult: PO 0.31.25 mg/d for 21 d each month, adjust to lowest level that gives symptom control (≤0.625
Female Hypogonadism, Primary Ovarian Failure, Female Castration
Adult: PO 2.57.5 mg/d in 13 divided doses for 20 d followed by a 10-d rest period, during last 5 d of estrogen, give a PO
Adult: PO 10 mg t.i.d. for 23 mo
Prostatic Cancer (palliation)
Adult: PO 1.252.5 mg t.i.d. for several weeks
Prevention of Osteoporosis
Adult: PO 0.3 mg q.d.
- Give with food or fluid of patient's choice.
- Give cyclically, except when used for palliation of cancer.
- Store tablets at 15°30° C (59°86° F) in a tightly closed container.
Adverse Effects (≥1%)CNS:
Headache, dizziness, depression
, libido changes. CV: Thromboembolic disorders
, hypertension. GI: Nausea
, vomiting, diarrhea
, bloating, cholestatic jaundice
Mastodynia, spotting, changes in menstrual flow, dysmenorrhea, amenorrhea. Metabolic:
Reduced carbohydrate tolerance, fluid retention. Other:
Leg cramps, intolerance to contact lenses.
, phenytoin, rifampin
decrease estrogen effect by increasing its metabolism
; oral anticoagulants
may decrease hypoprothrombinemic effects; interfere with effects of bromocriptine;
may increase levels and toxicity
of cyclosporine, tca
decrease effectiveness of clofibrate.
Well absorbed with first pass metabolism
Metabolized in GI mucosa
and liver to estrone
, further metabolized to inactive metabolites. Elimination:
In urine and bile. Half-Life:
Assessment & Drug Effects
- See nursing implications under estradiol.
- Monitor for and report breakthrough vaginal bleeding.
- Assess for relief of menopausal symptoms.
- Lab tests: Monitor serum phosphatase levels with prostate cancer.
- Monitor bone density annually when used for osteoporosis prophylaxis.
Patient & Family Education
- Be aware of importance of taking drug exactly as prescribed: Specifically, do not omit, increase, or decrease doses without
advice of physician. Know what to do when a dose is missed.
- Review package insert to ensure understanding of estrogen therapy.