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Mode of Action
Estrogens which act by regulating the transcription of a limited number of genes. An estrogen 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.
These are mixtures of oestrogens, obtained exclusively from natural sources, occurring as the sodium salts of water-soluble oestrogen sulphates blended to represent the average composition of material derived from pregnant horse‘s urine. It contains estrone, equilin, and 17α–dihydroequilin, together with smaller amounts of 17α–estradiol, equilenin, and 17α–dihydroequilenin. Each component has a varying degree of affinity to the target-organ oestrogen receptor site.