Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00691 (EE2)
 7,802 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

An attempt to confirm the effect of oral contraceptives (OCs) on the plasma dehydroepiandrosterone sulfate (DHEAS) and to explore the biochemical site of their action is presented. 89 women taking estrogen-containing OCs for 6 months or longer and 47 controls were studied. Both groups were of similar age, and with regular menstrual cycles. OCs used were Ovral (ethinyl estradiol, 50 mcg, norgestrel, .05 mg), Demulen 50 (ethinyl estradiol, 50 mcg; ethynodiol diacetate, 1 mg), and Ortho-Novum 1/50 (mestranol, 50 mcg; norethindrone, 1 mg). A single sample of plasma was made from the heparinized blood taken between 7-8 a.m. between Days 15-21 of a contraceptive treatment cycle in the experimental group and between Days 15-21 of a menstrual cycle in the control group. The results of the plasma DHEAS, DHEA, and androstenedione assays showed that all 3 OC preparations caused reductions in the androgenic steroids when compared with the controls. Results of statistical comparisons between the different OCs did not indicate if ethinyl estradiol or mestranol exerted a greater effect. Concentrations of delta-5-P and 17-delta-5-P were found to be lower in the experimental cases than in the controls. It is concluded that OCs cause a decrease in plasma DHEA, DHEAS, and androstenedione, with 1 possible mechanism being the inhibition of delta-5-P synthesis from cholesterol.
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PMID:Effect of oral contraceptives on plasma androgenic steroids and their precursors. 14 99

A sensitive and reliable radioimmunoassay (RIA) for measuring norethindrone (NET) in serum is described. Of a number of ring-A-reduced NET metabolites, only 2 cross-reacted appreciably in this RIA. Ethinyl estradiol and mestranol exhibited cross-reactions of only 1.1 and .4%, respectively. Serum concentrations of NET before and after ingestion of 4 NET-containing oral contraceptives (OCs) by 3 women each were measured by this RIA. In all 12 volunteers, serum NET levels rose rapidly after oral intake, reaching peak levels within .5-4 hours (median, 1.5) and fell precipitiously thereafter. Peak serum NET averaged 10.2 ng/ml after Ortho Novum 1/50 ingestion, 10.4 after Norinyl 1+50, 7.5 after Brevicon, and 4.3 after Micronor ingestion. Individual peak NET levels varied considerably in each group. Average half-lives varied from 2.3-4.4 hours, depending on OC compound ingested. After discontinuation of OCs, serum NET levels remained detectable ( .05 ng/ml) for at least 5 days in all 3 women who took Ortho Novum 1/50 but in none of the other subjects, suggesting that different preparations of identical doses and combinations of OCs may yield different serum NET profiles.
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PMID:A radioimmunoassay for norethindrone (NET): measurement of serum NET concentrations following ingestion of NET-containing oral contraceptive steroids. 75 Jan 88

The estrogen potencies of three new oral contraceptive formulations--Brevicon, Modicon, and Lo/Ovral--were determined. Brevicon and Modicon were found to have estrogen potency equal to mestranol 50 mug and equal to or greater than Norinyl 1 + 50 and Ortho-Novuum 1 + 50. Lo/Ovral, which is identical to Ovral in the type and ratio of progestin but 40 per cent lower in drug content, could be estimated to have an estrogen potency of 0.73 relative to mestranol 50 mug and therefore, by inference, to Brevicon and Modicon.
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PMID:Estrogen potencies of three new low-dose oral contraceptives. 94 52

A consequence of the diminishing the normal functioning of ovaries is progressing decrease in the levels of sex steroids leading to the clinical symptoms termed menopausal syndrome. This study aimed at evaluating the efficiency of Estraderm TTS-50 (Ciba-Geigy) in the treatment of this syndrome. The study involved 33 female patients, aged between 30 and 65 years. Estraderm in the form of patches containing 0.004 g of 17-estradiol was administered for 3 weeks every month, for 9 weeks. Kupperman's index, cytohormonal tests, and blood serum FSH and LH were tested before, during and after the treatment. A diminishing of the most common symptoms manifested by a statistically significant decrease in Kupperman's index and FSH, and LH levels with significant increase in serum estradiol was noted in 75% of patients following a 9-week treatment with Estraderm. Changes in the sex steroids levels led to a marked increase in the percentage of superficial cells, assessed with cytohormonal tests. Transdermal administration of estrogens in the form of Estraderm TTS-50 is the treatment of choice in the menopausal syndrome.
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PMID:[Use of estrogens in skin patches in treatment of pre-menstrual syndrome]. 130 12

Twenty-four postmenopausal women with vaginal atrophy due to oestrogen deficiency were treated with 17 beta-oestradiol administered as vaginal tablets containing 10 and 25 micrograms, respectively, in a slow-release system (Vagifem, Novo Nordisk, Denmark). All the women were treated for 2 weeks with each dose in a double-blind, cross-over study. Plasma concentrations of unconjugated oestradiol and unconjugated oestrone were measured at regular intervals for 24 h on days 1 and 14 of each treatment regimen. Cytological and clinical evaluations of the vaginal and urethral epithelium were also carried out. Initially, when the epithelium was still atrophic, dose-dependent absorption of oestradiol was demonstrated. After 14 days of treatment maturation of the vaginal epithelium was seen with both regimens and the absorption of oestradiol then declined significantly on both the 10 and the 25 micrograms dose. Oestrone levels remained unchanged and gonadotrophin levels were unaffected during treatment. Vaginal cytology showed maturation on both the 10 and the 25 micrograms dose, whereas urethral cytology showed a reduction in parabasal cells that was significant only on 25 micrograms. Clinical and subjective improvement was apparent on both doses and acceptance of treatment was good.
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PMID:Low-dose oestradiol in the treatment of urogenital oestrogen deficiency--a pharmacokinetic and pharmacodynamic study. 147 44

A placebo-controlled, double-blind study of triphasic oral contraceptives for prospectively confirmed premenstrual syndrome (PMS) was conducted with 82 subjects, 59 of whom completed the study and who were later confirmed to have moderate to severe premenstrual symptoms. 212 subjects were recruited between April 1987 - June 1988, and completed a menstrual history form and a 95-item retrospective questionnaire on premenstrual symptoms. Subjects took Synphasic (Syntex, Mississauga, Canada) containing 35 mcg ethinyl estradiol and 0.5 mg, 1.0 mg, and 0.5 mg norethindrone. Subjects were monitored for 1 menstrual cycle for baseline, then took triphasic or placebo for 3 cycles. 23 oral contraceptive taking and 36 placebo subjects completed the trial: completers had higher status occupations and lower symptom severity scores than dropouts. Both pill and placebo groups showed significant clinical improvement on every symptom except headache. Symptom scores decreased significantly between baseline and 3rd treatment cycle, and between menstrual phase scores and the variables "mood swings," "more sleep," "unhappy," and "tense" in the 2nd treatment cycle compared with the 1st treatment cycle in both groups. In the pill group ratings of premenstrual breast pain were significantly lower in the 3rd treatment cycle compared with baseline (p0.05), and to the 1st treatment cycle (p0.01). No significant changes in breast pain were found in the placebo group. Some pill cycles showed significant reduction in edema. Those in the pill group who were initially rated as "depressed" showed greater improvement in work impairment, sleep requirements, and energy level premenstrually. The pill group, however, reported significantly lower sexual interest during treatment. This is the 1st reported double-blind, placebo-controlled, prospectively confirmed study of oral contraceptives for PMS.
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PMID:A prospective treatment study of premenstrual symptoms using a triphasic oral contraceptive. 156 78

The ovum donation program at Chang Gung Memorial Hospital currently confronts the difficulty of limited oocyte resources. The oocytes might be donated from the surplus oocytes of IVF patients. However, after the successful introduction of embryo cryopreservation, patients preferred to have their surplus embryos cryop-reserved and thus, few surplus oocyts were available for donation from IVF program. In addition, official policies discourage use of oocytes donated by consanguineous relatives of either one of the recipient couple or for financial rewards. Among the first three oocytes recipients, with ovarian failure, one chemical pregnancy resulted. Oral premarin and transvaginal and intramuscular progesterone were administered as hormone replacement. The fourth recipient, who had had bilateral oophorectomy, received transdermal estradiol patch (Estraderm) and transvaginal progesterone (Utrogestan) as hormone replacement. The Estraderm/Utrogestan protocol became standard in later cases since the first ongoing pregnancy was achieved in patient 4. We feel this protocol satisfies the required ample levels of hormone replacement for ovum donation.
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PMID:Ovum donation program at Chang Gung Memorial Hospital, Taipei. 158 41

The aim of the study was to investigate the effect of 25 micrograms 17 beta-estradiol administered as a small vaginal tablet (Vagifem, Novo Nordisk A/S) on the symptoms of the vagina related to atrophy. The study was designed as a double-blind randomized placebo controlled study running for 12 weeks. The women were treated once daily for 2 weeks with the active or the placebo tablet. During the subsequent 10 weeks the women were treated twice a week. One hundred and sixty-four women were included. Ten dropped out for minor reasons, most of these due to lack of effect in the placebo group. In the Vagifem group 78.8% were suffering from moderate to severe atrophy of the vagina, compared with 81.9% in the placebo group. After 2 weeks the percentages were 14.3 and 35.3, respectively. After 12 weeks of treatment, 10.7% in the Vagifem group compared with 29.9% in the placebo group had moderate to severe atrophy (P less than 0.0001). A substantial part of the women complained about subjective symptoms such as vaginal dryness and dyspareunia. After 12 weeks of treatment, a significant improvement was found in the Vagifem group (P less than 0.002). Before treatment 53.1% in the treatment group and 41.0% in the placebo group were suffering from urological symptoms. After 2 weeks, 60.5% of the women in the Vagifem group underwent a change for the better compared to 35.3% in the placebo group. After 12 weeks of treatment the percentages in the two groups feeling an improvement were 62.8% and 32.4%. In this study local low-dose treatment with 25 micrograms 17 beta-estradiol was found to have a significant effect on the postmenopausal urogenital symptoms related to atrophy.
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PMID:Low-dose 17 beta-estradiol vaginal tablets in the treatment of atrophic vaginitis: a double-blind placebo controlled study. 158 79

To prevent hyperplasia and carcinoma of the endometrium during Estrogen Replacement Therapy (ERT), addition of progestogens once a month is considered mandatory. There is, however, no good scientific basis for this assumption. Since the addition of progestogens has several disadvantages, it is important to minimise the frequency of progestogen addition. Vaginosonography is a rather new technique, which has not yet been used for monitoring ERT. This study uses the growth of the endometrium, as it was measured by vaginosonography, as a parameter for stimulation of the endometrium by estrogens. ERT with Estraderm 50 twice a week was started in postmenopausal women. The endometrial thickness at the beginning was less than 3 millimeters. During estrogen treatment the endometrial thickness was determined every 6 to 10 weeks. As long as there was little or no increase during the estrogen treatment, no progestogen was added. Where there was a considerable growth, progestogen was added. With the use of vaginosonography, it is possible, to distinguish "fast growers" (women whose endometrium responded fast) from "slow growers".
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PMID:[Endometrial growth in continuous, estrogen substitution monotherapy with Estraderm TTS (0.05 mg/die) in 31 postmenopausal females]. 163 98

We recently reported that estrogen exerts distinct effects on the GH/IGF-1 axis that are dependent on the route of delivery, probably reflecting a first-pass effect on hepatic IGF-1 production. Oral administration reduces IGF-1 and increases GH levels; transdermal administration elevates IGF-1 without changing GH concentrations. Since mesenchymal tissue is a target for GH and IGF-1 action, we studied changes in the GH/IGF-1 axis following oral (ethinyl estradiol, 20 micrograms/day) versus transdermal (Estraderm 100 TTS, Ciba Geigy, 100 micrograms 17 beta-estradiol per day) estrogen delivery and compared corresponding effects on connective and bone tissue metabolism. Mean 24 h GH levels, IGF-1, markers of fibroblast (procollagen III) and osteoblast (procollagen I, osteocalcin) function, and indices of bone turnover (fasting urinary hydroxyproline and calcium to creatinine ratios, UOHPr/Cr and UCa/Cr) were measured before and after 2 months of either oral or transdermal therapy in two groups of postmenopausal women. Transdermal estrogen administration significantly (p less than 0.05) increased IGF-1, procollagen III, procollagen I, osteocalcin, and UOHPr/Cr. In contrast, oral estrogen administration had a suppressive effect; the levels of IGF-1 (p = 0.001), procollagen III (p = 0.018), procollagen I (p = 0.002), osteocalcin (p = 0.015), and UOHPr/Cr (p = 0.004) were significantly different from those measured during transdermal administration. Both treatments significantly reduced UCa/Cr (p less than 0.015). IGF-1 changes during estrogen therapy were significantly related (p less than 0.05) to changes in procollagen III, procollagen I, osteocalcin, and UOHPr/Cr. Transdermally delivered estrogen stimulates IGF-1 production, increases osteoblastic function, and stimulates bone and nonbone collagen synthesis.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Impact of short-term estrogen administration on growth hormone secretion and action: distinct route-dependent effects on connective and bone tissue metabolism. 164 49


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