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)

This is a review of estrogen receptors, largely taken from the authors' works, including estrogen receptors in the rat estrous cycle, in response to exogenous estrogens, endogenous estrogens, early responses, and the action of antiestrogens. Their method of measuring nuclear estrogen-receptor complexes entails incubating nuclear fractions with labeled estradiol, and with labeled estradiol in an excess of diethylstilbestrol, and quantitating the difference. Specific nuclear binding was documented in uterus, vagina, and pituitary of rats, in response to estradiol, diethylstilbestrol, estrone, and estriol, with a maximum of binding sites in proestrus, and the peak of estrogen secretion. The amount of estradiol bound increased with estradiol dose, but the rate of disappearance of bound nuclear estrogens was also more rapid with estrogen dose. Estradiol and estriol exhibited equal influences on early events such as RNA synthesis, but estriol did not maintain nuclear estrogen complex after 3 hours, nor permanent increase in uterine dry weight. These data lead the authors to suggest that a certain level of nuclear-receptor must be retained for at least 6 hours, as opposed to the theory that pivotal events like increased uterine blood flow, fluid imbibition, glucose transport, histamine release, and synthesis of the IP protein, is all that is required for uterine growth. Using the estrogen antagonists nafoxidine (Upjohn, 11,100 A), Cl-628, and clomiphene, and the charcoaldextran assay of total cytoplasmic estrogen-receptor binding, it was shown that the antagonists do stimulate nuclear binding, for up to 19 days in rats, but inhibit synthesis or replenishment of cytoplasmic receptors. Thus, the often observed fact that these estrogen antagonists are not antagonistic at 24 hours, but do antagonize estradiol later, is explained by prolonged retention of nuclear receptors.
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PMID:Estrogen-receptor binding: relationship to estrogen-induced responses. 17 88

Differences in vitamin E status between young Caucasian women using oral contraceptives (OCs) for 1 yr or more and control females were obtained with regard to the following parameters: 1) hemolysis, 2) plasma total tocopherols by spectrophotometric analysis, 3) individual tocopherols by a thin-layer gas-liquid chromatographic (TLC-GLC) technique, and 4) dietary intakes of vitamin E, polyunsaturated and saturated lipids, cholesterol and kilocalories. Ten subjects were on Ortho-Novum- or Norinyl-1/50, 8 on Ortho-Novum- or Norinyl-1/80, and 10 had never taken OCs. Analyses of 24-hr recalls and 7-day dietary records revealed no significant differences among groups for intakes of nutrients listed above. No significant differences among groups were observed from hemolytic values. Plasma total tocopherol concentrations measured by spectrophotometric and TLC-GLC techniques revealed that OC-1/80 subjects had significantly lower values than controls. Marginally inadequate vitamin E status as assessed by the various techniques was observed in approximately one subject in the control and OC-1/50 groups and in 2 of the OC-1/80 women. Large individual variations in vitamin E status were observed for subjects in all groups on similar estimated vitamin E intakes. TLC-GLC measurements of total tocopherols in plasma seemed to be perhaps a more sensitive indicator of vitamin E status of subjects than spectrophotometric analysis of tocopherols.
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PMID:Vitamin E status of young women on combined-type oral contraceptives. 72 56

The effects of Ovral (norgestrel plus ethinyl estradiol) on plasma growth hormone (GH) levels and glucose tolerance were investigated in Sprague-Dawley and a carbohydrate-sensitive strain (BHE) of rats. Sodium pentobarbitol was used to stimulate GH production. Fasting blood glucose levels were not altered by treatment with Ovral in either strain. However, under a glucose load, Sprague-Dawley rats developed an impaired tolerance during the latter part of the glucose tolerance test, while treatment with the oral contraceptive improved an impaired response to glucose load in BHE animals. A good correlation between changes in GH and glucose tolerance during treatment could not be established. Sprague-Dawley rats had a significant (p less than .01) decrease in the rate of body weight increase compared with controls.
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PMID:The effects of an oral contraceptive on plasma growth hormone and glucose tolerance in two strains of rats. 84 89

17beta-[6,7- 3H]Estradiol was incubated with adult human liver slices in Krebs-Ringer phosphate buffer containing glucose. Of the identified 3H recovered, 51-76 percent consisted of estrone-3-sulfate (E13S) and 17 beta-estradiol-3-sulfate (E23S). E13S was the main metabolite and was found in both tissue and medium. E23S was present only in the medium. Minor amounts of estrogen glucuronides were formed. When a human liver homogenate was incubated with [3H]E2 in a medium fortified with excess uridine diphosphate glucuronic acid only some 4 percent of conjugation with glucuronic acid was observed. It is suggested that human liver favors sulfurylation as the conjugating mechanism for E2 and E1.
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PMID:In vitro metabolism of 17beta-estradiol by human liver tissue. 118 Oct 8

Data are reported from the combined results of two studies assessing the lipid and carbohydrate effects of a triphasic preparation of norgestimate and ethinyl estradiol (Ortho TriCyclen, Tri-Cilest) over a 2-year period in 1,783 healthy women. Mean values for serum levels of high-density lipoprotein cholesterol (HDL-C) were increased significantly, with a percent change at 24 months of 13.2. Values for the ratio of low-density lipoprotein cholesterol to HDL-C were reduced throughout the study period (mean change of -6.4% at cycle 24). There were no clinically significant changes in fasting blood glucose levels or insulin levels or in values for glycosylated hemoglobin. These results are consistent with those of previous studies and indicate that the triphasic preparation of norgestimate and etinyl estradiol is a selective and minimally androgenic oral contraceptive agent. Long-term therapeutic benefit may accrue from the favorable influences on the lipid profile.
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PMID:Lipid and carbohydrate effects of a new triphasic oral contraceptive containing norgestimate. 132 56

Research in the area of oral contraception currently focuses on the development of selective progestogens that combine targeted progestational and antiovulatory activity with a minimal potential for androgenicity. The present dual-center study was conducted to investigate the efficacy, tolerability, and safety of a new monophasic oral contraceptive (OC) containing 250 micrograms norgestimate in combination with 35 micrograms ethinyl estradiol (Ortho-Cyclen or Cilest). Ninety-seven healthy women of childbearing age participated in the study: 37 received the new norgestimate/ethinyl estradiol combination OC as primary therapy and 31 were switched over from other OCs. The norgestimate/ethinyl estradiol formulation was well tolerated and was associated with excellent cycle control. After six cycles of use, there were no statistically significant differences in the incidence of spotting or breakthrough bleeding compared with baseline, nor were there any significant changes in the incidence of headache, nausea, or mastalgia. Body weights remained constant for the duration of the study, as did systolic and diastolic blood pressures. Of particular note was the absence of any statistically significant alterations in metabolic parameters, including blood glucose or lipoprotein levels. These findings are consistent with the results of several other European studies and indicate that the norgestimate/ethinyl estradiol combination OC combines superior cycle control with minimal risk of androgenic side effects.
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PMID:Clinical experience with a new norgestimate-containing oral contraceptive. 134 20

The performance of a new low-dose oral contraceptive (Mercilon) containing only 20 micrograms ethinyloestradiol combined with 150 micrograms desogestrel is reviewed. Eight multicentre clinical trials have been completed and provide information on 10,672 women studied over 73,477 cycles. The high efficacy of Mercilon was indicated by the finding that only 10 pregnancies were reported; nine of these occurred in women who omitted to take Mercilon on a number of days and only one in a woman who took all the tablets according to instructions. Cycle control was good; as with all oral contraceptives, the incidence of breakthrough bleeding and spotting was highest in the first treatment cycle and by the sixth treatment cycle the values were usually < 5% and < 7%. More than 80% of women had regular cycles. Side effects were few, the most common being headache, nausea and breast tenderness with incidences in the sixth treatment cycle of less than 2%, 6% and 6%, respectively. There were no significant changes in body weight or blood pressure. Pharmacodynamic investigations showed no adverse effects. Only 1 of 5 studies found an increased response to a glucose tolerance test compared to the pretreatment test. In 8 of 10 studies, serum HDL-C concentrations increased on treatment and this was associated with increases in apoproteins A1 and A2. Serum triglyceride levels also increased but no change occurred in serum cholesterol or LDL-C levels. Haematological factors were assessed in 8 studies and only minor changes were observed. Serum binding protein (SHBG, CBG, caeruloplasmin) concentrations increased and serum androgen levels decreased. Measurements of blood FSH, LH, oestradiol and progesterone indicated adequate inhibition of ovulation. Mercilon is the only oral contraceptive containing 20 micrograms ethinyloestradiol to have high efficacy, to have no adverse pharmacodynamic effects and, importantly, to produce an acceptable bleeding pattern not significantly different from that of oral contraceptives with a higher content of ethinyloestradiol.
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PMID:Clinical experience and pharmacological effects of an oral contraceptive containing 20 micrograms oestrogen. 145 94

12 healthy volunteers attending the family planning clinic at Shanghai, First Maternity and Infant China, Hospital, enrolled in the study, Oral contraceptives (OCs) were prescribed: Marvelon (150 mcg of desogestrel--DSG), Mercilon (150 mcg of DSG), and Microgynon (150 mcg of levonorgestrel--LNG). The patients were divided into 6 groups of 2 persons each in a randomized cross-over study. OCs were taken on day 6 of the cycle up to day 21, then stopping for 7 days. Each OC was used for 3 months. During the pretreatment cycle between days 6 and 9 of the follicular phase and 21 and 22 of the luteal phase a blood sample was taken after fasting for determination of lipids, sex hormone binding globulin (SHGB), ceruloplasmin, and testosterone. After glucose loading, significant increases of glucose and insulin occurred at 1, 2, and 3 hours during treatment with Microgynon only. The ratio for total areas of insulin to glucose did not change significantly nor did glycosilated hemoglobin A1 levels. Serum triglyceride concentrations increased significantly for both Marvelon (27%-43%) and Mercilon (29-40%). Serum high density lipoprotein (HDL) cholesterol concentrations were significantly elevated with Marvelon but less so with Mercilon, while HDL-C decreased significantly with Microgynon. The serum low density lipoprotein (LDL) cholesterol changes were not significant, but LDL-C concentrations declined with DSG formulations and increased with Microgynon. Apoprotein A1 and A2 increased significantly for both Marvelon and Mercilon. Apoprotein A2 increased with Microgynon. Serum SHBG increased markedly with Marvelon (335-380%). Serum testosterone concentrations decreased significantly (33.2-40.4% with Microgynon) and so did ceruloplasmin values. The antiestrogenic effect of strong LNG in Microgynon produced significant metabolic changes. The effect of 30 mcg EE in Marvelon and 20 mcg EE of Mercilon was equal.
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PMID:A cross-over study of three oral contraceptives containing ethinyloestradiol and either desogestrel or levonorgestrel. 153 80

Research in the area of oral contraception currently focuses on the development of selective progestogens that combine targeted progestational and antiovulatory activity with a minimal potential for androgenicity. The present dual-center study was conducted to investigate the efficacy, tolerability, and safety of a new monophasic oral contraceptive (OC) which contains 250 mcg norgestimate in combination with 35 mcg ethinyl estradiol (EE; Ortho-Cyclen or Cilest). 97 healthy women of childbearing age were part of this study; 37 received the new norgestimate/EE combination OC as primary therapy and 31 were switched over from the other OCs. The formulation was well-tolerated and was associated with excellent cycle control. After 6 cycles of use, there was no statistically significant difference in the incidence of spotting or breakthrough bleeding as compared with the baseline. Nor were there any significant changes in the incidence of headache, nausea, or mastalgia. Body weights remained constant for the duration of the study as did systolic and diastolic blood pressures. Of particular interest was the absence of any statistically significant alterations in metabolic parameters, including blood glucose or lipoprotein levels. These findings are consistent with the results of several other European studies and indicate that the norgestimate/EE combination OC combines superior cycle with minimal risk of androgenic side effects.
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PMID:Clinical experience with a new norgestimate-containing oral contraceptive. 167 78

Of the contraceptive choices open to a post-partum woman with gestational diabetes, this discussion concentrates on low-dose oral contraceptives. Although gestational diabetes usually clears at delivery, 75% of these women will go on to developed impaired glucose tolerance or overt diabetes, especially if they are obese or if their glucose level had been high. Many elect permanent sterilization, but those requiring reversible contraception usually choose the IUD or the pill. IUDs carry a high risk of infection and are less effective in diabetics. The author compared a low-dose combined pill with 400 mcg norethindrone and 35 mcg ethinyl estradiol (Ovcon 35), and a pill containing levonorgestrel (Triphasil), to barrier contraception in 230 women with recent gestational diabetes. After 6-13 months of use 11-17% of each group had impaired glucose tolerance, and 15-20% of each group had diabetes (n.s.). Insulin levels rose from 28.5 mIU/mL to 59.7 in controls, 32.0 to 71.8 in Ovcon 35 users, and from 40.2 to 85.1 in Triphasil users (p0.05). HDL values rose significantly in the group taking Ovcon, and LDL values fell significantly in all 3 groups. These low-dose pills can be used safely in postpartum gestational diabetic women, as long as they do not smoke, are encouraged to lose weight, and have no sign of cardiovascular disease as evidenced by albuminuria and an ophthalmoscopic exam.
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PMID:Contraceptive options for the gestational diabetic woman. 167 21


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