Moderate to severe vasomotor symptoms, vulval and vaginal atrophy associated with the menopause, female hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, palliation in breast cancer (women and men with metastatic disease, prevention of osteoporosis, advanced androgen-dependent carcinoma of the prostate, for palliation only
For treatment of moderate to severe vasomotor symptoms, vulval and vaginal atrophy associated with the menopause: the lowest dose that will control symptoms should be selected. Attempts to discontinue or taper medication should be made at 3-month to 6-month intervals. The usual initial dosage is 1 - 2 mg daily. Administration should be cyclic [e.g. 4 weeks on and 1 week off]. For treatment of female hypoestrogenism due to hypogonadism, castration, or primary ovarian failure: Treatment is initiated with a dose of 1 - 2 mg daily. For treatment of breast cancer, for palliation only, in appropriately selected women and men with metastatic disease: 10 mg TID for at least three months. For treatment of advanced androgen-dependent carcinoma of the prostate, for palliation only: 1-2 mg TID. The effectiveness of therapy can be judged by phosphatase determinations as well as by symptomatic improvement of the patient.
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Mode of Action
It acts by regulating the tran-scription of a limited number of genes. It diffuses through cell membranes, distributes itself throughout the cell, and binds to and activates the nuclear oestrogen receptor, a DNA-binding protein that is found in oestrogen-responsive tissues. The activated oestrogen receptor binds to specific DNA sequences, or hormone-response elements, which enhance the transcription of adjacent genes and in turn lead to the observed effects.
Physical/history examination before initiating oestrogen therapy should be done; fluid retention; women with narrow vagina; uterovaginal prolapse; treatment unresponsive infection; Cushing syndrome; BP monitor; 4 weeks before surgery; history of endometriosis
Selected breast cancer; estrogen dependent neoplasia; undiagnosed abnormal genital bleeding; history of thrombophlebitis; thrombo-embolic disorders; pregnancy; severe hepatic /renal /CVS impairment; porphyria.
Changes in menstrual flow; break through bleeding; dysmenorrhoea; amenorrhoea during and after treatment; GI disturbances; allergic reactions; visual disturbances; mental depression; convulsion; fluid retention; aggravation of existing hypertension; tenderness and enlargement of the breasts; headache; pre-mature closure of epiphysis; aggravation of endometriosis.
Drug interactions: Drug affected by estrogens: Oral anti-coagulants; tricyclic anti-depressants; corticosteroids; hydantoins; and dantrolene. Drugs that may affect estrogens are: rifampicin; barbiturates and hydantoins.