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Biomedical subjects

E Baracat

Publications and source records attributed to E Baracat.

6 recordsLinked to original sources
PubMed1999

Estrogen activity and novel tissue selectivity of delta8,9-dehydroestrone sulfate in postmenopausal women.

Recent basic and clinical advances have consolidated the concept of tissue-selective estrogens, i.e. molecules that express different degrees of partial agonist, full agonist or antagonist activity in different tissues or cells. Delta8,9-Dehydroestrone sulfate (delta8,9-DHES) is a conjugated estrogen and a component of conjugated equine estrogens (CEE). It is metabolized in the human in at least a 1:1 ratio to its 17beta form, 17beta-delta8,9-DHES. To evaluate its activity in different clinical and biochemical parameters, a clinical research study was conducted with delta8,9-DHES and estrone sulfate as a comparator in postmenopausal women. Delta8,9-DHES was given orally at a daily dose of 0.125 mg for 12 weeks in a group of 10 women. Two additional groups of women received either estrone sulfate alone (1.25 mg/day) or the combination of delta8,9-DHES and estrone sulfate at the previously specified doses. A significant and consistent suppression of hot flushes (number, severity, and total score) was observed with delta8,9-DHES, reaching more than 95% suppression in all parameters of vasomotor symptoms. This level of activity was equal to that obtained with the much higher dose of estrone sulfate, and it was sustained for the duration of the treatment period (12 weeks). Measurements of a bone resorption marker, i.e. urinary excretion of N-telopeptide, demonstrated that delta8,9-DHES at 8 weeks produced a degree of suppression (40%) similar to that observed with the higher dose of estrone sulfate. Gonadotropin secretion (FSH and LH) was significantly suppressed in women receiving delta8,9-DHES, similar to that observed with estrone sulfate alone or with the combination of the two. Other parameters, such as total cholesterol, low density lipoprotein cholesterol and high density lipoprotein cholesterol were not modified significantly, whereas serum globulins (sex hormone-binding globulin and corticosteroid-binding globulin) showed only marginal increases after delta8,9-DHES administration. Taken together with preclinical data, it is found that delta8,9-DHES is an active estrogen with a distinct pharmacological profile that results in significant clinical activity in vasomotor, neuroendocrine (gonadotropin and PRL) and bone preservation parameters, whereas displaying little or no efficacy, at the dose tested, on other peripheral parameters normally affected by estrogens. Collectively, this information supports the concept that delta8,9-DHES is an integral component of CEE, with distinct tissue selectivity contributing to the CEE's overall clinical activity, and places this estrogen as a distinct member of a novel class of centrally active molecules with unique peripheral tissue selectivity.

Adult↗
PubMed1998

Effect of estrogen-progestin hormonal replacement therapy on plasma antithrombin III of postmenopausal women.

BACKGROUND: This study was performed to evaluate antithrombin III levels in postmenopausal women receiving hormonal replacement treatment. METHODS: It is a prospective randomized study concerning 19 postmenopausal patients, aged 40 to 65 years, who received either continuous daily oral equine conjugated estrogen 0.625 mg (group A, N=10) or daily transdermal 17beta-estradiol 50 microg (group B, N=9). Medroxyprogesterone acetate (5 mg/day, 14 days monthly) was given to all patients. Blood samples were obtained before and after 3, 6, 9 and 12 months of treatment. Coagulation tests included Antithrombin III (functional method), prothrombin time, partial activated prothrombin time, thrombin time, factor V, fibrinogen, platelet count and euglobulin lysis time. Friedman analysis of variance and Mann-Whitney test were used for statistical analysis. RESULTS: Antithrombin III level was reduced (p<0.05) in group A but not in group B, although it remained within normal range. No changes were detected in the other coagulation tests. CONCLUSIONS: These data suggest that oral conjugated estrogen replacement reduces functional ATIII, whereas transdermal estradiol replacement therapy does not modify it.

Administration, Cutaneous↗
PubMed1996

Comparative bioavailability study of an once-a-week matrix versus a twice-a-week reservoir transdermal estradiol delivery systems in postmenopausal women.

An open-label, randomised, crossover study was conducted with in healthy postmenopausal women to compare the relative bioavailability of a matrix transdermal estradiol delivery system worn for 7 consecutive days, versus a reservoir transdermal patch worn for 4 days followed by its immediate replacement by another patch worn for further 3 consecutive days. There was a minimum 7-day washout period between the two study periods. Both systems were labelled to release approximately 50 micrograms/day of estradiol. Twenty-six subjects were evaluated with regard to estradiol serum levels. Blood samples were taken immediately before and at regular intervals until 192 h after the initiation of each study treatment (patch application) and assayed for estradiol. There was no difference between the patches with regard to Cmax. Based on the relative bioavailability, one matrix patch proved to be bioequivalent to two reservoir patches worn consecutively for 7 days. These results demonstrate the ability of one matrix patch to deliver consistent therapeutic levels of estradiol over a 7-day period.

Administration, Cutaneous↗
PubMed1991

[Quantitative variation in lysosomes in the epithelium of the human uterine tube in the menstrual cycle and after the menopause].

Quantitative variation of the lysosomes in the epithelium of the human uterine tube in the menstrual cycle and in post-menopausal period. The authors counted the lysosomes in the human uterine tube in the menstrual cycle and in post-menopausal period. The post-menopausal women were separated in two groups: one received oral estrogens during twenty one day and the other did not. Fragments of uterine ampullae were removed, fixed and submitted to Gomori acid phosphatase method. Results show that the number of lysosomes during the proliferative phase was significantly greater than in secretory phase and post-menopausal period. The number of lysosomes in post-menopausal period was significantly greater in women treated with estrogens. Our result show that estrogens are responsible for the increase of the number of lysosomes.

Adult↗