Furuhjelm M, Karlgren E, Carlstrom K (Dept of Obstetrics and Gynecology, Sabbatsberg Hospital, Karolinska Institutet, Stockholm, Sweden). Intravaginal administration of conjugated estrogens in premenopausal and postmenopausal women. Int J Gynaecol Obstet 17: 335-339, 1980 Daily doses of 0.625 mg of conjugated estrogens were administered intravaginally for 14 days to 12 postmenopausal women (six with highly atrophic and six with slightly atrophic vaginal mucosa), resulting in vaginal mucosae similar to those found in premenopausal women in all 12 subjects. In a second experiment, serum estrogens, folliclestimulating hormone (FSH) and luteinizing hormone (LH) were determined before and hourly for six hours after a single intravaginal dose of 0.625 mg of conjugated estrogens was given to five postmenopausal women and to five premenopausal women on cycle days 6-8. Serum levels of unconjugated immunoreactive estrogens and total estrone increased rapidly in four of five postmenopausal women. Luteal phase values were found after only two hours, but there were no effects on serum FSH and LH. One of the postmenopausal women, who had an unatrophied vaginal mucosa, showed a considerable lower resorption of estrogens. There were no significant changes in the serum estrogen levels of the premenopausal women. Thus, we conclude that daily vaginal administration of 0.625 mg of conjugated estrogens for 14 days is sufficient to restore an atrophic vaginal mucosa to a premenopausal condition. Furthermore, the condition of the vaginal mucosa seems to influence the resorption, thus indicating an inbuilt mechanism of protection against overdosage of intravaginally applied estrogens.

The effect of oral estrogen replacement therapy upon somatic and psychical disturbances and sexuality was studied in a double-blind investigation in 48 postmenopausal women using hormone preparations with two different levels of micronized estradiol-17 beta (E2) as active estrogen component. The patients were treated for 8 months in four 2-month periods with two preparations containing 1-2 mg of E2 (TrisekvensR and EstrofemR), with one preparation containing 1-4 mg of E2 (TrisekvensR forte) and with a placebo preparation. Investigations performed before and during treatment included general clinical chemical analysis, serum levels of FSH, LH and E2 and evaluation of the patients' somatic and psychical disturbances and sexuality. The patients were classified into three subgroups according to their pretreatment scores for mental distress and/or depression: severe (group I), moderate (group II), or no (group III) mental distress and/or depression. No significant differences between the three subgroups were found in pretreatment values from the general clinical chemical analysis or the hormone assays. Estrogen treatment significantly reduced S-total cholesterol values in all three subgroups; otherwise no significant effects were revealed by the general clinical chemical analysis. During the period of optimal wellbeing, serum E2 levels corresponded to luteal phase values. The gonadotropin levels, although depressed by approx. 50%, were still within the postmenopausal range. There were no significant differences between the two subgroups in hormone levels obtained during optimal estrogen treatment. Twenty-one patients had the best test results when treated with the larger dose (TrisekvensR forte) and 23 with the smaller dose (TrisekvensR and EstrofemR) and 4 during placebo treatment.(ABSTRACT TRUNCATED AT 250 WORDS)

Daily doses of 0.625 mg of conjugated estrogens were administered intravaginally for 14 days to 12 postmenopausal women (six with highly atrophic and six with slightly atrophic vaginal mucosa), resulting in vaginal mucosae similar to those found in premenopausal women in all 12 subjects. In a second experiment, serum estrogens, follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were determined before and hourly for six hours after a single intravaginal dose of 0.625 mg of conjugated estrogens was given to five postmenopausal women and to five premenopausal women on cycle days 6-8. Serum levels of unconjugated immunoreactive estrogens and total estrone increased rapidly in four of five postmenopausal women. Luteal phase values were found after only two hours, but there were no effects on serum FSH and LH. One of the postmenopausal women who had an unatrophied vaginal mucosa, showed a considerable lower resorption of estrogens. There were no significant changes in the serum estrogen levels of the premenopausal women. Thus, we conclude that daily vaginal administration of 0.625 mg of conjugated estrogens for 14 days is sufficient to restore an atrophic vaginal mucosa to a premenopausal condition. Furthermore, the condition of the vaginal mucosa seems to influence the resorption, thus indicating an inbuilt mechanism of protection against overdosage of intravaginally applied estrogens.