Oestrogen therapy and endometrial cancer.
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Estradiol Congeners↗
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Results for “ESTRADIOL, THERAPEUTIC”
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Monitoring side effects of contraceptives.
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Adolescent↗
[Clinical aspects and pathology of granulosa cell tumors. A single case report].
Case report on a granuloma cell tumour in a 82 year old patients. Because of estradiol production postmenopausal bleedings from a adenomatous-hyperplastic endometrium had been in the history. Hormonal values became normal following removal of the benign tumour in stage I. The most important pathologic, endocrinologic and therapeutical principles of the tumour have been described.
Aged↗
[Shifting of menstruation in female athletes].
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Contraceptives, Oral↗
[The effect of estrogen therapy on sexuality. Observations on 122 postmenopausal women].
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Climacteric↗
Pharmacokinetics of orally administered estradiol valerate. Results of a single-dose cross-over bioequivalence study in postmenopausal women.
A randomized, single-dose cross-over study in 32 postmenopausal women was performed to demonstrate bioequivalence of two estradiol valerate containing formulations (first sequence of Klimonorm as test preparation). The serum levels of estradiol, free and conjugated estrone were measured until 48 h after an oral dosage of 4 mg estradiol valerate (CAS 979-32-8). The mean AUC(0-48) of estradiol was calculated as 1006.6 +/- 479.4 h x pg x ml-1 (Test) and 1015.2 +/- 555.2 h x pg x ml-1 (Reference). The corresponding (AUC(0-48) of the active metabolite, free estrone, exceeded that of estradiol at 3578.3 h x pg x ml-1 (Test) and 3485.1 h x pg x ml-1 (Reference). Much higher was the AUC(0-48) for conjugated estrone at 132.4 h x ng x ml-1 (Test) and 133.6 h x ng x ml-1 (Reference). Mean estradiol Cmax values of 39.8 +/- 17.7 pg/ml (Test) and 42.9 +/- 21.0 pg/ml (Reference) were attained 8.2 +/- 4.5 h (Test) and 10.0 +/- 5.9 h (Reference) after the administration of 4 mg estradiol valerate. Maximal free estrone concentrations of 163 pg/ml (Test) and 174.3 pg/ml (Reference) were reached after 7.2 h (Test) and 7.5 h (Reference). Maximal conjugated estrone concentrations of 15.5 ng/ml (Test) and 16.2 ng/ml (Reference) were reached after 2.4 h (Test) and 2.0 h (Reference). The terminal elimination half-life of estradiol was calculated at 16.9 +/- 6.0 h (Test) and 15.0 +/- 4.8 h (Reference), that of free estrone at 16.3 h (Test) and 13.5 h (Reference), that of conjugated estrone at 11.8 h (Test) and 10.6 h (Reference). After logarithmic transformation, the 90% confidence intervals of the AUC(0-48) and Cmax ratios for estradiol and also for the metabolites (free and conjugated estrone) were within the acceptance ranges for bioequivalence. Therefore the test preparation and the reference preparation are bioequivalent.
Administration, Oral↗
The effects of desogestrel and ethinylestradiol combination in normal and hyperandrogenic young girls: speculations on contraception in adolescence.
Hormone profile and ovarian morphology were studied in two groups of adolescents (group 1:19 girls with slight signs of hyperandrogenism; group 2: 14 normal adolescents) in basal conditions and during a contraceptive combination of 30 micrograms ethinyl estradiol (EE) and 150 micrograms desogestrel (D). Treatment was associated with a low incidence of side effects in both groups. In group 1, acne generally improved within 12 months while hirsutism was only reduced in some subjects (58%) after 12 months of therapy (basal hair score 8.50 +/- 1.60 vs 5.81 +/- 1.53 p less than 0.001). Significant falls in plasma levels of LH, total and free testosterone and an increase in sex-hormone-binding globulin levels were observed during treatment especially in group 1. High percentage of multifollicular ovaries (75%) characterized hyperandrogenic subjects. Ovarian volume and number of follicles, higher in group 1 than 2 in basal conditions, showed a significant reduction in both groups and normal ovarian morphology was restored in hyperandrogenic subjects. Considering the high incidence of hyperandrogenemia in adolescence and its implications, our data suggest that the EE.D combination suits adolescent biological condition and is one of the suitable contraceptive methods in adolescents which also has therapeutic effects.
Acne Vulgaris↗
Thermal gradient and response to estrogens or antiestrogens in advanced breast cancer.
The correlations between the thermal gradient of superficial breast cancer lesions (before and 15 days after starting treatment) and the end results of hormonal therapies with estrogen and antiestrogens were investigated. Forty-four women with a median age of over 70 with locally advanced breast cancer and/or metastases mainly located in soft tissues entered the study. Twenty-two patients were treated with diethylstilbestrol sodium diphosphate (20 mg/day i.m.) and the other 22 with tamoxifen (20 mg/day orally). The initial iperthermia was reduced after 15 days in more than 50% of the cases and remained stationary in the others. The cases with a thermal gradient more than 2 degrees C of the tumors did better, in terms of remission, following therapy (64.7% versus 37.0%. However, an early decrease of the same gradient in the course of therapy appears scantily related to the response. The therapeutic results in the 2 groups were very similar: 45.5% complete or partial regression, with a median duration of more than 8 months, in those treated with diethylstilbestrol and 50%, with a median duration of more than 11 month, in those treated with tamoxifen. Only in some cases of the first group of patients the treatment was discontinued due to severe side effects.
Adult↗
Steroid hormones affect limbic afterdischarge thresholds and kindling rates in adult female rats.
UNLABELLED: Catamenial epileptics show particular vulnerability to seizures during menstruation and at the time of ovulation, when circulating estradiol (E(2))/progesterone (P(4)) ratios are high. The present study tested the hypothesis that alterations in neuronal excitability induced by E(2) and P(4) affect thresholds and the development of secondary generalization in kindled rats. METHODS: The effects of endogenous hormones secreted during the estrous cycle, and of exogenous exposure to E(2) and P(4) after ovariectomy (OVX), with and without adrenalectomy (ADX), were tested. Kindling electrodes were implanted in the basolateral amygdala or dorsal hippocampus in adult female rats. The anticonvulsive effects of P(4) on amygdala kindled seizures were also determined in intact subjects. RESULTS: In intact females, afterdischarge thresholds (ADTs) in the amygdala were significantly lower (306+/-48 microA; peak to peak) at mid-day proestrus, just prior to ovulation, when serum E(2) is elevated. ADTs were more than twofold higher (808+/-95 microA) during metestrus, coincident with peak ovarian P(4) secretion. In OVX females, amygdala thresholds were lowest with E(2) replacement and highest with P(4) replacement. Hippocampal ADT was unaffected by hormone replacement after OVX. The rates of both amygdala and hippocampal kindling were significantly accelerated by E(2) and slowed by P(4). E(2) replacement significantly increased serum corticosterone (CORT) levels. In ADX rats, CORT replacement increased kindling rates, synergizing with the effects of E(2). In fully kindled animals, P(4) administration suppressed motor seizures in approximately 60% of cases. CONCLUSIONS: E(2) lowers amygdala ADTs and facilitates kindling. This effect may involve both direct E(2) effects and indirect effects mediated via increased levels of circulating corticosterone. P(4) raises amygdala ADTs, slows kindling development and suppresses fully kindled seizures. Hence, P(4) may have potential therapeutic value for women with catamenial epilepsy.
Amygdala↗
Pregnancy after an unsuccessful oocyte donation cycle.
Clearly, to provide adequate counseling to women with POF, information is critically needed concerning the background incidence of spontaneous improvement in ovarian function as well as carefully designed, controlled studies to evaluate the efficacy of presumed therapeutic intervention. The case presented herein underscores our lack of adequate information about this common reproductive disorder.
Adult↗
The vascular activity of some isoflavone metabolites: implications for a cardioprotective role.
Legume-derived isoflavones such as genistein, diadzein and equol have been associated with a reduction in risk of cardiovascular disease. In the current study, we explore the vascular activity of several isoflavone metabolites namely dihydrodaidzein, cis and trans-tetrahydrodaidzein and dehydroequol for potential cardioprotective properties. Rat isolated aortic rings were used. 17beta-oestradiol, equol, and all four of the metabolites studied significantly antagonized contractile responses to noradrenaline. The direct vasodilatory action of these compounds were examined and in contrast to 17beta-oestradiol, the vasodilatory effect of which was demonstrated to be endothelium independent, the dilatory action of all four compounds could be inhibited by endothelium denudation. Further, the dilatory action of both dihydrodaidzein and cis-tetrahydrodaidzein were inhibited by the nitric oxide synthase inhibitor, N(omega)-nitro-L-arginine (NOLA), by the soluble guanylate cyclase inhibitor, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) and by 40 mM KCl. Dilatory responses to dehydroequol and trans-tetrahydrodaidzein, on the other hand, were inhibited by 40 mM KCL but not by NOLA nor ODQ. Finally, we examined the protective potential of these compounds in inhibiting endothelium damage by oxidized low density lipoprotein (ox-LDL). Trans-tetrahydrodaidzein was at least 10 fold more potent than 17beta-oestradiol in protecting against ox-LDL induced damage. We conclude that the isoflavone metabolites, dihydrodaidzein, cis- and trans-tetrahydrodaidzein and dehydroequol, may potentially represent a novel series of cardioprotective therapeutics.
Animals↗
The effects of norethisterone in postmenopausal women on oestrogen replacement therapy: a model for the premenstrual syndrome.
The influence of norethisterone on mood and behaviour was investigated in prospective placebo-controlled study in 58 postmenopausal hysterectomized women who were being treated with subcutaneous oestradiol and testosterone implants. Norethisterone, 2.5 or 5 mg daily, was given for 7 days and a placebo for two periods of 7 days. Psychological, behavioural and physical variables were assessed using the Menstrual Distress Questionnaire. There were widespread adverse effects which were dose-related. Significant changes in five of the eight symptom complexes studied (pain, concentration, behavioural change, water retention and negative affect) were found with 5 mg/day of the progestogen. The symptoms were similar to the typical complaints of the premenstrual syndrome, such that a combination of oestradiol and testosterone implants with cyclical oral norethisterone appears to be a model for this condition. The dose of this progestogen should therefore be the minimum to achieve the desired therapeutic effect.
Adult↗
Direct gonadotrophic effect of growth hormone on oestradiol production by human granulosa cells in vitro.
In-vitro studies in both rodents and man suggest that GH can stimulate ovarian steroidogenesis, but it is not clear whether this effect is mediated by changes in circulating concentrations of insulin-like growth factor-1 (IGF-1) or whether it is a direct action on the ovary (or, indeed, both). In this study the effects of biosynthetic human GH (hGH) on the production of oestradiol and IGF-1 by human granulosa cells in culture were examined using ovarian tissue (from both normal and polycystic ovaries) which had not previously been exposed to exogenous gonadotrophin therapy. Addition of hGH (1 or 10 ng/ml) to the incubation medium resulted in a significant (1.7 to 3.6 fold) increase in oestradiol accumulation after 48h in culture. Human GH also had a significant additive effect on the dose-related responsiveness of granulosa cell oestradiol production to hFSH. Concentrations of IGF-1 in the medium were undetectable in each of these experiments. These studies demonstrate that hGH has a potent, direct stimulatory effect on production of oestradiol by the human ovary which is independent of the effect of FSH. These findings have important implications for understanding the physiological role of hGH in human ovarian function as well as for therapeutic use of biosynthetic hGH for induction of ovulation.
Cells, Cultured↗
[The modulators of the estrogenic activity].
The biological, pharmacological and therapeutic properties of estrogens/antiestrogens are related to their chemical structure. Tamoxifen, used for the treatment of hormone-dependent breast cancer, and other analogue derivatives of triarylethylene or presenting a cyclic or heterocyclic structure, mimic some of the activities of estrogens. They have major therapeutic potential as selective estrogen receptor modulators in the prevention of breast cancer and various post-menopausal conditions.
Breast Neoplasms↗
[Transdermal administration of estrogens in women with the postcastration and climacteric syndromes].
The authors report on the results of a follow-up of 64 women aged 25-64 years, to whom oestrogens were administered transdermally by means of the preparation Estraderm TTS 25 or 50 for three months. 55 women were treated for postcastration syndrome and nine women for climacteric syndrome. The authors deal with the problems of dosage of the transdermal oestrogen therapy, study the side-effects of treatment and evaluate the results of therapy. In conclusion, they recommend the transdermal form of treatment by Estraderm TTS because of its very good therapeutic effect, acceptability by the patients, and only minimal local and general side-effects.
Administration, Cutaneous↗
Epidemiology of cardiovascular disease in women and the role of sex steroid hormone use.
Women in the United States are at significant risk for CVD. After a 10- to 12-year delay in onset, the rate of increase in CAD with age in women is the same as that in men. Cardiovascular risk correlates positively with total serum cholesterol, LDL and triglyceride levels and inversely with HDL cholesterol. Triglycerides are an independent risk factor in women. The close correlation between cholesterol levels and myocardial infarction has been documented in population-based studies in men and women and in dietary and drug intervention trials in men. For every 1% decrease in cholesterol, there is a corresponding 2% decrease in cardiovascular risk in both sexes. For adults it is recommended that total cholesterol levels be less than 200 mg/dL. Fifty percent of women in the United States have cholesterol levels that exceed that number. Cholesterol screening, identification of high-risk individuals and early institution of overall risk management strategies are keys to reducing morbidity and mortality. Ideal therapeutic interventions are those that are lipid neutral or have a beneficial effect on the lipid profile.
Cardiovascular Diseases↗
Plasma gonadotropin-releasing hormone profiles after intravenous and subcutaneous bolus injection in thin and obese women.
Other studies of plasma gonadotropin-releasing hormone profiles after bolus injection have revealed earlier, sharper peaks and higher blood gonadotropin-releasing hormone levels with the intravenous (IV) than with the subcutaneous route of administration. We used both routes to administer gonadotropin-releasing hormone by bolus injection to thin and obese subjects. Plasma gonadotropin-releasing hormone profiles after IV administration were similar in both groups. The subcutaneous route produced flatter, delayed, and lower peaks, an effect markedly exaggerated in obese subjects, who demonstrated 95% lower peak gonadotropin-releasing hormone levels compared with the IV route and 64% lower levels than thin subjects after subcutaneous administration. These findings may be relevant to therapeutic failures observed in obese subjects using the subcutaneous route.
Adult↗
[Bone density in anorexia nervosa--with comments on prevention and therapy of osteoporosis].
Anorectic women often have reduced bone density, which may predispose them to osteoporosis and fractures. The mechanisms involved and their relative contribution are still a matter of discussion. Most studies have been done in young adults, but during the past few years children and adolescents have also been investigated. In this paper we present preliminary data on bone mineral parameters in young anorectic females during the first few months of inpatient treatment. Measurement of trabecular bone density (TBD), bone mineral density (BMD) and body composition were done by peripheral quantitative computed tomography (pQCT) at the distal end of the radius and by dual-energy X-ray absorptiometry (DEXA) in ap-projection. Hormonal parameters and clinical course were monitored. Baseline values of TBD and BMD seemed to be generally within the normal range. Follow-up measurements showed a significant reduction in TBD but not in BMD in most patients during the first two months of treatment despite clinical improvement. There was no clear correlation with hormonal or clinical parameters. Further evaluations are necessary. Possible therapeutic consequences are discussed.
Adolescent↗