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

Immediate metabolic effects of Stediril and Eugynon, hormonal contraceptives containing 0.5 mg DL-norgestrel and 0.05 mg ethinyl estradiol, were studied in 39 women aged 18-43 years and 10 men aged 21-36 years. All subjects were volunteers who had taken no hormone preparations during the 3 months immediately preceding the study. Blood samples were taken at 9 and 11 AM and at 1 and 4 PM on 2 successive days; the contraceptive was administered immediately after the first sample was taken on the second day. From the measured values for arterial oxygen and carbon dioxide partial pressures, blood pH, and hemoglobin, values for oxygen saturation, standard bicarbonates, buffer abases, and base excess were calculated using the Thews nomogram. The primary effect of hormone administration was shown to be metabolic acidosis, which is partly compensated during the next 7 hours by the respiratory system. No signs of primary respiratory alkalosis were noted.
 ...
PMID:[Acid-base balance immediately after administration of an oral contraceptive (author's transl)]. 2 17

Longitudunal and cross-dectional blood coagulation studies were made in patients receiving oral contraceptive therapy and in unmedicated women used as control subjects. These studies have included use of a new procedure, plasma fibrinogen chromatgraphy, which, by assay for a high molecular weight fibrinogen complexes in plasma, detects or excludes the presence of small thrombi, even when these are of the clinically silent type. New contraceptives users (n=154) received either Ovulen (100 pg of mestranol) or Demulen (50pg of ethinyl estradiol) and were followed serially for one year. During the cross-sectional study (193 women and 1,350 samples), serial examination was preformed on those taking oral contraceptives for 3 months to 10 years. Over-all, pathologic plasma fibrinogen chromatographic findings, indicative of thrombosis, were detected in 6 per cent of hte control examinations and in 27 per cent samples from oral contraceptive users. These findings suggest that oral contraceptive users developed mainlyclinically silent thrombotic lesions, with four-to-fivefold greater frequency than the control subjects. Consequently, it is inferred that they are at four-to fivefold greaterrisk of developing clinically overt disease, a risk factor estimate in line with that derived by epidemiologic study.
 ...
PMID:Association between oral contraceptive use and thromboembolism: a new approach to itsinvestigation based on plasma fibrinogen chromatography. 5 Jul 41

A study comparing 2 triphasic hormonal contraceptive preparations (combinations of ethinyl estradiol and levonorgestrel) is reported. SH B 264 AB was used by 594 women for 6628 cycles with no pregnancies, while 634 women used SH B 261 AB for 6025 cycles with 1 pregnancy. A lower incidence of breakthrough bleeding and spotting was observed among SH B 264 AB users, and this preparation ("Triquilon") is preferred to the other. Triquilon users had a menstrual cycle length of 26-30 days and an amenorrhea rate of .4%. There was a low rate of breakthrough bleedings and spottings, which was higher when patients forgot to take their pills. In the vast majority of Triquilar users, body weight and blood pressure remained constant. Subjective side effects (e.g. nausea, dizziness, headache) were infrequent and decreased as the length of Triquilar use increased. A separate study of 1440 cycles of Triquilar use and 1343 cycles of Microgynon use showed that, while the contraceptive effectiveness was the same, the incidence of breakthrough bleeding and spotting was significantly less frequent among Triquilar users.
 ...
PMID:[The first three-stage preparation for hormonal contraception. Clinical results (author's transl)]. 11 12

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.
 ...
PMID:Effect of oral contraceptives on plasma androgenic steroids and their precursors. 14 99

The acute and chronic effects of estradiol (E2) on the serum levels of four delta5,3-beta hydroxysteroids and their four delta4, 3-keto products were studied in four ovariectomized women with and without adrenal stimulation by ACTH. Six hour infusions of saline and of synthetic 1-24 ACTH were administered and later repeated with a two hour infusion of E2 50 mug/h. The patients were then given 50 mug of ethinyl estradiol (EE2) p.o. for 4 to 6 weeks and the control and ACTH infusions were again repeated. Levels of pregnenolone3 (Pe), 17alpha-hydroxypregnenolone (17 Pe), progesterone (Po), 17alpha-hydroxyprogesterone (17 Po), dehydroepiandrosterone (DHEA), androstenedione (Adione), androstenediol (Adiol), and testosterone (T), as well as cortisol and DHEA-sulfate were measured by radioimmunoassay on serum samples taken at 1200 and 1300 h. There was no significant effect of E2 or EE2 in the doses administered with or without exogenous ACTH on 3 betaOHSD activity as reflected in absolute steroid levels or in the ratio of concentrations of each delta5:delta4 steroid pair. During the 4th and 5th hour of ACTH infusion, the plasma level of 17 Pe (mean 22.5-fold stimulation) was most elevated, followed by 17 Po (12.5-fold), Pe (10-fold), cortisol (5.9-fold) and Po (4.5-fold), with smaller increases for the other steroids. These results, as well as the pattern of change in plasma levels in one of the subjects in whom fifteen minute samples were measured, provide further evidence suggesting that the major pathway for cortisol biosynthesis in vivo proceeds from Pe via 17 Pe, and not via Po.
 ...
PMID:Effects of estrogens on adrenal 3 beta-hydroxysteroid dehydrogenase in ovariectomized women. 18 11

Norethindrone (ENT), which is a representative in estrane series of progestogen, is not only strongly progestational but also estrogenic and in some cases, antiestrogenic. To understand progestational effect and antiestrogenic effect, the interactions of ENT on estrogen and progestogen receptors were studied in the uterine cytosol of white female rabbit. The 274,200 X G supernatant of uterine homogenate was used as cytosol. 3H-Estradiol, 3H-Progesterone, 3H-ENT or cold ENT were incubated with uterine cytosol at 4 degrees C for 2 hours. Results are as follows: 1. Sucrose gradient centrifugation [5 approximately 20% linear and 40,000 rpm (159,200 X G) for 16 hours at 4 degrees C]: ENT was bound to extrogen 8S receptor in immature rabbit uterus (Fig. 2 & 3), and to progestogen 8S receptor in estrogen primed rabbit uterus (Fig. 5). 2. Kinetic study, determined by dextran coated charcoal (0.001% dextran and 0.1% charcoal): (1) In the uterine cytosol of immature rabbit, 3H-estradiol-receptor binding was observed with Kd divide by 3.6 X 10-9 M and it was revealed that ENT was a competitive inhibitor to this binding with Ki divide by 2.6 X 10-6 M, as in Fig. 6. (2) 8S component, obtained by centrifugation of uterine cytosol (Fig. 1) in estrogen primed rabbit, binds 3H-progesterone with Kd divide by 8.1 X 10-10 M and Bm (maximal binding sites) divide by 5.0 X 10-8 M/mg of protein, and ENT was a competitive inhibitor in this binding with Ki divide by 2.3 X 10-9 M (FIG. 7 & 8). 3H-ENT-8S binding was demonstrated with Kd divide by 1.1 X 10-9 M and Bm divide by 8.7 X 10-8 M/mg of cytosol protein (Fig. 8). These results indicate: (a) ENT is bound to both estrogen and progestogen receptors in 8S macromolecules of uterine cytosol, (b) competitive inhibition of ENT to these bindings indicated that ENT is bound to these receptors at the steroid binding sites where estradiol and progesterone bind to, (c) ENT has much more affinity to progestogen receptor (Ki divide by 2.3 X 10-9 M) than to estrogen receptor (Ki divide 2.6 X 10-6 M), (d) while ENT is bound to progestogen and estrogen receptors at the same time, Bm of ENT (8.7 X 10-8 M/mg of cytosol protein) is more than Bm of progesterone (5.0 X 10-9 M/mg of cytosol protein), and Kd of ENT (1.1 X 10-9 M) was less than Ki of ENT (2.3 X 10-9 M) in the binding to progesterone-receptor. Biologically, while ENT is bound to progestogen -receptor with high affinity and to estrogen receptor with low affinity, ENT is actually progestational in low dose and antiestrogenic in high dose but the anti-estrogenicity seems to be incomplete in vivo as ENT may be metabolized to a potent estrogenic compound, ethinyl estradiol
 ...
PMID:[Interaction of norethindrone on estrogen and progesterone receptors in the rabbit uterine cytosol (author's transl)]. 18 90

The influence of daily oral cyclical estrogen therapy on the plasma lipid and lipoprotein levels in postmenopausal women was determined. Included were 39 women with distressing postmenopausal vasomotor symptoms. Ethinyl estradiol (EE2) .05 mg was given to 20 women and estradiol valerinate (EV) to 19 others. The drugs were given as tablets once daily for 3-week cycles with 1-week intervals. After overnight fasts, blood samples were taken before and during treatment at 1, 3, and 6 months. During EV therapy, the HDL-TC and the HDL-phosphlipid concentrations increased 10-15% after 6 cycles. The net effect on the risk of development of ischemic cardiovascular disease due to the change in plasma lipids induced by EE2 is uncertain. The plasma lipid changes during EV therapy might possibly retard the development of atherosclerosis. However, the lipid metabolism of postmenopausal women may be different from that of fertile women.
 ...
PMID:Metabolic and hormonal effects of post-menopausal oestrogen replacement treatment. II. Plasma lipids. 20 45

Estradiol 17 beta prevented the fall in the microbicidal activity of the myeloperoxidase-H2O2-halide system induced by high H2O2 concentrations. In contrast, when the H2O2 (and halide) concentrations were low the myeloperoxidase-H2O2-halide antimicrobial system was inhibited by estradiol. These properties of estradiol 17 beta were shared by estradiol 17 alpha, estrone, estriol, ethinyl estradiol, and phenol, but not by estradiol-3-benzoate, testosterone, progesterone, hydroxyprogesterone, cortisone, hydrocortisone, or deoxycorticosterone.
 ...
PMID:Effect of estrogens on the myeloperoxidase-mediated antimicrobial system. 22 68

Estrogen receptor activity was preserved in fixed, paraffin-embedded tissue and demonstrated by binding of estrogen which, in turn, was detected immunocytochemically. Estrogen was added to rat endocervial epithelium to protect specifically receptors during fixation. The protective estrogen was apparently lost during embedding and had to be resupplied before staining. Estradiol-mediated immunocytochemical staining was inhibited by diethylstilbestrol and nafoxidine hydrochloride.
 ...
PMID:Estrogen receptor immunocytochemistry. 36 29

A multicenter randomized double-blind trial was conducted to compare 55 women using Loestrin-20 (20 ug ethinyl estradiol and 1 mg norethisterone acetate) as an oral contraceptive with a like number of women using Microgynon-30 (30 ug ethinyl estradiol and 150 ug levonorgestrel). 7 family planning clinics agreed to collaborate in the trial and enrollment of patients which began in November 1974. The number of participating clinics was increased to 12 at a later date. 133 patients were recruited between November 1974 and September 1976. 23 were excluded from the analysis. 55 of the remaining 110 patients were admitted to each of the 2 treatment groups. It was found that women who used Loestrin-20 discontinued treatment because of abnormal bleeding more frequently that women using Microgynon-30, but that the discontinuation rates for other reasons were closely similar in the 2 treatment groups. Of the 13 women who stopped using Loestrin-20 because of abnormal bleeding, 6 complained of oligomenorrhea or amenorrhea while the other 7 complained of irregular bleeding. Of the 2 women who stopped using Microgynon-30 because of bleeding problems, 1 complained that the bleeding was irregular and the other that it was prolonged. Although the sample size is small, Loestrin-20 clearly provides poor cycle control and consequently is less acceptable than Microgynon-30. Loestrin-20 may be less effective than Microgynon-30, but the difference in the accidental pregnacy rates is not statistically significant.
 ...
PMID:A randomized double-blind trial of two low dose combined oral contraceptives. 37 92


1 2 3 4 5 6 7 8 9 10 Next >>