Treatment of moderate to severe vasomotor symptoms associated with the menopause. Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. When prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered. Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure. Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease. Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only). Prevention of osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and for whom non-estrogen medications are not considered to be appropriate.
Estradiol is the most potent physiologic estrogen and, in fact, is the major estrogenic hormone
secreted in humans. Estradiol controls the development and maintenance of the female
sex organs, the secondary sex characteristics and the mammary glands as well as certain
functions of the human uterus and accessory organs, particularly the proliferation of the
endometrium, the development of the decidua, and the cyclic changes in the cervix and
vagina. The production of estradiol by the ovaries is under the control of pituitary
gonadotropins, follicle stimulating hormone (FSH) and luteinizing hormone (LH).
In menopausal women, the depletion of ovarian follicles leads to lower plasma estradiol and
elevated plasma FSH and LH.
Oral: Prostate cancer: 10 mg 3 times/day for at least 3 month. Menopausal vasomotor symptoms: 1-2 mg/day on a cyclical or continuous regimen Prevention of postmenopausal osteoporosis: 0.5 mg/day in cyclical regimen. Hypogonadism: 1-2 mg/day in a cyclic regimen. Vaginal: Vulvular and vag atrophy: Insert 2-4 g/day for 2 wk. Maintenance: 1 g 1-3 times/wk. Postmenopausal vag atrophy; Urogenital symptoms: Insert a ring and keep in place for 90 days. Atrophic vaginitis: Insert 1 tab once daily for 2 wk. Maintenance: 1 tab twice wkly. Attempt to discontinue or taper medication at 3-6 monthly intervals.
Interaction with laboratory tests: The use of sex steroids may influence biochemical parameters of, for example, liver, thyroid, adrenal and renal function, plasma levels of (carrier) proteins such as corticosteroid-binding globulin and lipid/lipoprotein fractions, parameters of carbohydrate metabolism, and parameters of coagulation and fibrinolysis.
Interactions with other medicines: Long-term treatment with hepatic enzyme-inducing drugs (e.g. several anticonvulsants and antimicrobials) can increase the clearance of sex hormones and may reduce clinical efficacy. Such hepatic enzyme-inducing properties have been established for hydantoins, barbiturates, primidone, carbamazepine, and rifampicin and are also suspected for oxcarbazepine, topiramate, felbamate, griseofulvin and the herbal remedy St John’s Wort (hypericum perforatum). Maximal enzyme induction is generally not seen before 2-3 weeks but may be sustained for at least 4 weeks after cessation of drug therapy. In rare cases, reduced oestradiol levels have been observed under the simultaneous use of certain antibiotics (e.g. penicillins and tetracycline). Substances which undergo substantial conjugation (e.g. paracetamol) may increase the bioavailability of oestradiol by competitive inhibition of the conjugation system during absorption. In individual cases, the requirement for oral antidiabetics or insulin can change as a result of the effect on glucose tolerance.
Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy. Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child.
GI disturbances, genitourinary changes, haematologic disorders, CV and CNS effects, endocrine and metabolic disorders, cholestatic jaundice, local skin reactions, chorea, contact lens intolerance, steeping of corneal curvature, pulmonary thromboembolism, carbohydrate intolerance.
Pregnancy Category X. Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Acute toxicity studies indicate that even in the case of inadvertent intake of a multiple of the therapeutic dose, no acute toxicity risk is to be expected. Overdose may cause nausea and vomiting and withdrawal bleeding may occur in some women. Management of acute overdose should be supportive.
Store in a cool (below 30°C) and dry place, away from light & children.
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