SEARCH · PubMed Health

Results for “ETHYNODIOL DIACETATE”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 127 records · Page 7Linked to original sources

PubMed1978

Hemostatic changes induced by exercise during oral contraceptive use.

Exercise-induced changes in hemostatic measurements were studied in 25 women. Twelve of the subjects were not using oral contraceptives and the remainder were using Demulen (ethynodiol diacetate (1 mg) and ethinyl estradiol (0.05 mg)). Exercise on a treadmill induced similar changes in both groups, but during the use of Demulen the levels of fibrinogen and plasminogen were higher, antithrombin level was lower, and the recalcified clotting and dilute whole blood lysis times were shorter in group 2 than in the corresponding samples obtained from the nonpill users.

Adult↗

PubMedDate not supplied

Radioimmunoassay of norethindrone (17 alpha-ethynyl-17 beta-hydroxy-4-estren-3-one) and ethynyl-estradiol (17 alpha-ethynyl-1,3,5, (10)-estratien-3, 17 beta-diol). Application to human plasma determination of norethindrone after oral administration of this steroid.

The experiment conditions for the evaluation of Norethindrone (17 alpha-Ethynyl-17 beta-hydroxy-4-estren-3-one, NET) and Ethynyl-estradiol (17 alpha-ethynyl-1, 3, 5 (10) estratrien-3, 17 beta-diol, EE) by radioimmunoassay are described. A minimal quantity of 25 pg of these two steroids could be evaluated using different reduced metabolites of NET, very little cross reaction is observed with 200 pg of these metabolites. No effect was observed with estradiol for the EE-antiserum. The NET-antiserum was used to evaluate this steroid and ethynodiol diacetate after oral administration to female volunteers. Maximal values in the plasma (2-3% of the administered dose) was found between 1-3 h after administration and at 24 h a concentration of 0.1-0.3% still remained in the plasma.

Administration, Oral↗

PubMed1975

The effect of combination and low dose progestogen oral contraceptives on serum lipids.

Fasting serum triglyceride, free fatty acid, phospholipid, and cholesterol levels were determined in women who were taking either combination or low dose progestogen oral contraceptives. The contraceptives used were: ethynodiol diacetate and ethynyl estradiol; norgestrel and ethynyl estradiol; norgestrel; and megestrol acetate. Serum lipids significantly increased in women taking combination pills. They significantly decreased in patients taking norgestrel, while they remained almost unchanged in patients taking megestrol acetate. This decrease varied with the type of progestogen used in continuous low dosage therapy. The confusion when interpreting the results from different reports on the effects of oral contraceptives on serum lipids will be reduced if proper attention is given to the types of steroid used.

Adult↗

PubMed1977

Three-year prospective study of carbohydrate metabolism in women using Ovulen.

Twenty-eight women were tested with a standard three-hour oral glucose tolerance test before and after three years of using a combination-type oral contraceptive containing mestranol and ethynodiol diacetate (Ovulen). At the three-year test time there was a significant elevation of the patients' weights and their 1-, 2-, and 3-hour blood glucose and 2- and 3-hour plasma insulin values. Pretreatment control tests had shown no "abnormal" blood glucose curves, whereas at the three-year test 17.2% of the curves were "abnormal". Serial follow-up studies in two women after stopping the medication showed that the abnormal glucose curves reverted to their pretreatment status within 12 months.

Adolescent↗

PubMed2005

Oral contraceptives as substrates and inhibitors for human cytosolic SULTs.

Cytosolic sulfotransferases (SULTs) in mammals are involved in the biotransformation and homeostasis of various endogenous and xenobiotic compounds. The current study aimed to examine the sulfation of contraceptive compounds by various human cytosolic SULTs and to investigate the inhibitory effects and mode of action of these compounds on the sulfation of 17beta-estradiol, a major endogenous estrogen. A systematic study using all eleven known human cytosolic SULTs revealed the differential substrate specificity of these enzymes for the eight representative contraceptive compounds and two endogenous estrogens (estrone and 17beta-estradiol) tested as substrates. Activity data showed that SULT1A1 displayed the strongest activity toward 17alpha-ethynylestradiol. Kinetic studies revealed that the V (max) value of the sulfation of 17alpha-ethynylestradiol by SULT1A1 was 1.64 times that of the sulfation of 17beta-estradiol, while the K (m) values were almost equal for the two compounds. The inhibitory effects of three contraceptive compounds on the sulfation of 17beta-estradiol by SULT1A1 were examined. IC(50) values determined were 0.193, 1.84, and 2.98 mM, respectively, for 19-norethindrone acetate, ethynodiol diacetate and mifepristone. Kinetic analyses indicated that the mechanism underlying the inhibition by these contraceptives is of a mixed noncompetitive type. Metabolic labeling experiments confirmed the sulfation of contraceptive compounds and the release of their sulfated derivatives by HepG2 human hepatoma cells. Collectively, the results obtained suggest a role of sulfation in the metabolism of contraceptive compounds in vivo. Moreover, in view of their inhibitory effects on the sulfation of 17beta-estradiol, these compounds may potentially act to disrupt the homeostasis of endogenous estrogens.

Arylsulfotransferase↗

PubMed1978

The effects on sexual response and mood after sterilization of women taking long-term oral contraception: results of a double-blind cross-over study.

Twenty women using oral contraception for a minimum of 2 years with no side effects volunteered to take part in this experiment which commenced after they had undergone laparoscopic sterilization. In a double-blind cross-over design, patients were administered either 1.0 mg ethynodiol diacetate + 0.1 mg mestranol ("Ovulen") each day for 21 days or an identical-looking placebo for the same number of days. The following month the alternative (cross-over) tablet was given. On days 12 and 25 of each cycle the women completed a modified form of Pitt's Depression Index and a short Sexual Response Score. The result indicated that the active pill ("Ovulen") was associated with a decreased sexual response, but with no increase in the depression index (relative to placebo). The significance of these findings is discussed in relation to previous work, the methodology of the study and hormone-behaviour experiments.

Adult↗

PubMed1978

Endocrinological and physiological features after steroid treatment of male rats.

The effects of medroxyprogesterone acetate (Provera), testosterone propionate (TP), ethinyl estradiol (EE), and ethynodiol diacetate (ED) treatments on sperm population in different segments of the male rat reproductive tract, reproductive organ weights, circulating androgens and fertility were studied. Ten microgram TP given for five days reduced the sperm population and organ weights. A marked reduction in the number of sperm and reproductive organ weights was observed in males orally treated with estrogens. Only long-term (20 days) treatment with Provera (1 mg/day) significantly reduced sperm population and reproductive organ weights. Combination of TP and Provera resulted in a more pronounced reduction in sperm counts and organ weights. Among steroids studied, estrogen was the only compound which suppressed fertility and circulating steroid levels.

Androgens↗

PubMed1984

Liver regeneration in oral contraceptive treated female rats--effects of moderate malnutrition.

Treatment of well-nourished female rats with a combination of 5 micrograms ethynyl estradiol and 100 micrograms ethynodiol diacetate, increased the DNA content, 3H thymidine incorporation into DNA and mitotic activity in the non-regenerating liver, but impaired liver regeneration after partial hepatectomy. In rats which were moderately malnourished by feeding 25 percent less calories and 50 percent of recommended allowance for vitamins A and B2, OC treatment had similar stimulatory effect on non-regenerating liver, but did not impair liver regeneration after partial hepatectomy. Analysis of nucleotide bases after hydrolysis of unpolymerized nucleotides and nucleosides revealed significant perturbations due to OC treatment. However, the impaired liver regeneration due to OC treatment of well-nourished rats could not be attributed to diminished availability of bases, particularly thymidine. Data on mitotic index and binucleate cell numbers suggest that besides inhibiting mitosis (DNA duplication), OC treatment of well-nourished rats may also impair partitioning of binucleate cells.

Animals↗

PubMed1986

Increased adrenocortical responsiveness to exogenous ACTH in oral contraceptive users.

To evaluate the effects of changing steroid milieu on adrenocortical function, basal levels and responses of cortisol, 17-hydroxyprogesterone (17PO), androstenedione (A), dehydroepiandrosterone (DHEA), and testosterone to exogenous synthetic ACTH were investigated in six normal women during the early follicular (EF) and midluteal (ML) phases of the menstrual cycle and in five women on an oral contraceptive (OC) agent (35 micrograms ethinyl estradiol and 1 mg ethynodiol diacetate, Demulen). Baseline serum steroid and cortisol binding globulin (CBG) levels were measured on days 3-7 and 21-23 of the menstrual cycle in the normal subjects and on days 3-7 of OC treatment cycles. ACTH stimulation (10 micrograms m-2 i.v. bolus) was performed following dexamethasone suppression (0.5 mg p.o. q 6 h X 4). Basal levels of cortisol and CBG as well as cortisol responses to ACTH were increased in OC users relative to normal women tested during both the EF and ML phases of the cycle. In addition, 17PO levels were increased during the ML phase both before and following dexamethasone suppression compared to levels present in the EF phase and in OC users, no doubt because of increased ovarian steroidogenesis.

17-alpha-Hydroxyprogesterone↗

PubMed1983

Glycohemoglobin (Hb A1) levels in oral contraceptive users.

In a group of 33 healthy women, among whom 15 utilized the combined oral contraceptive pill, and 18 utilized the progesterone oral pill (ethynodiol diacetate, 0.5 mg, Femulen, we have examined the percentage of glycohemoglobin (Hb A1). In the progesterone oral pill users the percentage of Hb A1 remained unchanged, that is 5.4% before, and 5.2% 3-6 mth after using it, whereas in women taking the combined oral contraceptive pill the values increased from 5.9% before to a mean of 8.7% after 3-6 mth after administration. This increase seems to be related to the estrogen of the which, as in pregnancy, may induce glucose intolerance. From this study it may be seen that, despite its disadvantages such as reduced effectiveness and menstrual disruption, the progesterone-only pill is preferable. At the same time, the screening by the Hb A1 evaluation, a sure, inexpensive and easily performed procedure, makes it possible to detect a nonsuspected diabetes or a borderline diabetes and thus to change the contraception method used for another method.

Adolescent↗

PubMed1986

Progestins and oral contraceptive-induced lipoprotein changes: a prospective study.

In order to determine the effects on plasma lipoproteins of oral contraceptives containing progestins with varying androgenic potency, 136 healthy women were randomized into 3 groups and followed prospectively for one year while receiving either 50 mcg ethinyl estradiol and 1.0 mg ethynodiol diacetate (EED), 50 mcg ethinyl estradiol and 1.0 mg norethindrone acetate (ENA), or 50 mcg ethinyl estradiol and 0.5 mg d-1 norgestrel (ENG). Comparison was made to a self-selected group of 50 women using alternative means of contraception. Plasma cholesterol increased by 7-9% and triglycerides by 32-57% in all 3 groups (p less than 0.05). ENG use resulted in other significant lipoprotein changes including an 18% increase in low density lipoprotein cholesterol (LDL-C), a 13% fall in high density lipoprotein cholesterol (HDL-C) and a 27% decline in HDL2 cholesterol (HDL2-C) (p less than 0.05). Apoprotein A-I (Apo A-I) increased by 9% with ENA and by 11% with EED (p less than 0.05), but did not change significantly with ENG. This prospective study demonstrates that in oral contraceptive agents with identical estrogen, progestins with different androgenic potency produce major and different changes in plasma lipoproteins.

Adolescent↗

PubMed1991

Incidence of breakthrough bleeding during oral contraceptive therapy.

A phase IV, open-label, multicenter survey of 983 obstetrician-gynecologists was conducted to evaluate the incidence of intermenstrual bleeding in 6,382 women receiving a low-dose monophasic oral contraceptive, ethynodiol diacetate, 1 mg, with ethinyl estradiol, 35 micrograms (EDA 1 mg with EE 35 micrograms) over a six-month period. Most patients (75%) did not experience intermenstrual bleeding during therapy. Follow-up questionnaires were sent to the physicians of the 1,526 women reporting breakthrough bleeding or spotting; 1,027 follow-up questionnaires (67%) were returned. The questionnaires revealed that approximately one-fifth of the patients were placed on EDA 1 mg with EE 35 micrograms to regulate preexisting bleeding; of them, 71% reported an improvement, 13% reported worsening, and 16% reported no change in their cycle regularity. Most breakthrough bleeding or spotting (91%) occurred in the first three months of therapy in women with preexisting irregular bleeding as well as in those using the oral contraceptive solely for birth control. Although a fair proportion of women experienced intermenstrual bleeding, very few (5.1%) discontinued therapy because of it. Thus, the study demonstrated that the incidence of breakthrough bleeding and spotting appears to be within or below the range reported for other monophasic and multiphasic oral contraceptives. Further, in agreement with previously published reports, the data suggest that cycle control will improve after three months of oral contraceptive use.

Contraceptives, Oral, Hormonal↗

PubMed1981

Androgen control of an inhibitory modulator of phosphodiesterase in rat epididymis and prostate.

When rats were injected with the progestin ethynodiol diacetate in doses that suppressed spermatogenesis and the growth of accessory sex glands, the level of phosphodiesterase in epididymal and prostate tissues increased 5- to 10-fold. This increase was prevented by concurrent administration of testosterone propionate. A similar increase in phosphodiesterase activity was observed in the epididymides and prostates of castrated animals, with reversal by treatment with androgen. In immature rats approaching puberty, the phosphodiesterase activity in epididymis and prostate increased while the blood testosterone level remained low; as the testosterone level rose with the onset of puberty, the phosphodiesterase activity decreased. Incubation of enzymically active extracts of accessory tissues from castrated rats with heat-treated extracts of the corresponding normal tissues resulted in strong inhibition of the initially high phosphodiesterase activity. The addition of heat-treated extracts of accessory glands from castrated rats to enzymically active extracts of the corresponding tissues from normal rats resulted in a marked elevation of their phosphodiesterase activities. Of the two heat-stable modulators, the inhibitor factor was dialyzable. The dependence of this factor on testosterone suggests a mechanism of action by which the steroid hormone, by inducing the production in its target tissues of an inhibitory modulator of phosphodiesterase, controls the maintenance of functional levels of cAMP.

3',5'-Cyclic-AMP Phosphodiesterases↗

PubMedDate not supplied

Contraceptive steroid effects on lipids and lipoproteins in cynomolgus monkeys.

Seventy-three adult female cynomolgus monkeys fed an atherogenic diet were studied to determine the effect of two different combination contraceptive steroid preparations containing equivalent amounts of estrogen but different progestin components on plasma lipids and lipoproteins. Our hypothesis was that any high density lipoprotein (HDL) lowering effect of the contraceptive steroid preparations was proportional to the rise in total serum cholesterol caused by the progestins. For 2 years, one group (Ovral [Wyeth Laboratories], n = 23) received 75 micrograms norgestrel and 7.5 micrograms ethinyl estradiol daily, while another (Demulen [Searle & Co.], n = 25) received 150 micrograms ethynodiol diacetate and 7.5 micrograms ethinyl estradiol daily. The control group (n = 24) received no treatment. On average, the two oral contraceptive groups had higher total serum cholesterol and triglyceride concentrations but lower HDL cholesterol concentrations and smaller low density lipoproteins (LDL) compared with the control group. There was an inverse relationship between total serum cholesterol and HDL cholesterol for all three groups, but at any given total serum cholesterol concentration between 350 and 500 mg/dl, the Ovral group had HDL cholesterol concentrations that averaged 37% and 14% lower than the control and Demulen groups, respectively. The decrease in HDL concentrations with oral contraceptive treatment was associated with a sharp decrease in (HDL2b)gge protein (82% for Ovral and 59% for Demulen) and a corresponding increase in (HDL3b,c)gge protein as determined by gradient gel electrophoresis. Of 23 animals in the Ovral group, six had HDL subfractions greater than 10 nm diameter (HDL2b)gge compared with 22 of 24 animals in the control group. Although LDL size, on average, was smaller and plasma triglycerides were greater with oral contraceptive treatment compared with controls, there was no apparent relationship between LDL size and plasma triglyceride concentrations.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1997

Progesterone in Periplaneta americana and Neobellieria bullata adults from the procuticle phase until first progeny production.

A significant amount of progesterone-like immunoreactive material (150 ng/g) was measured by EIA in the procuticle phase of adult of both sexes of Periplaneta americana. This peak markedly decreased to 1-10 ng/g during sclerotization and was unlikely to be of dietary origin. In the case of 0-hr-old P. americana adults 96-98% of progesterone-like material was localized in the digestive tract and Malpighian tubules. In contrast, a relatively low level of progesterone-like immunoreactive material was measured in 0-hr-old Neobellieria bullata adults. Activity of 3beta-HSD/isomerase converting pregnenolone to progesterone was high (22-43 fmol/mg protein/20 min) in 0-hr-old P. americana adults and significantly fell during sclerotization. High progesterone levels (13-16 ng/g), measured by HPLC-RIA, coexist with high levels of 3beta-HSD/isomerase activity. Orally active human contraceptives (ethisterone, ethynodiol, ethynodiol diacetate, lynestrenol, mestranol, norgestrel, norethynodrel, tamoxifen citrate, and mifepristone) which act on mammalian steroid receptors had no significant effects on progeny production in either polytrophic or meroistic insect ovaries even at concentration of 5000 mg/kg.

3-Hydroxysteroid Dehydrogenases↗

PubMed1988

Programmed ovulation induction and oocyte retrieval for in vitro fertilization.

Forty-two patients underwent programmed ovulation induction for oocyte retrieval. They were treated in the preceding cycles with a progestagen, ethynodiol diacetate, at a dose of 2 mg twice daily. Two groups were defined based upon the stimulation protocol: Group A1 was stimulated with clomiphene citrate and human menopausal gonadotropin (hMG), and Group A2 with follicle-stimulating hormone (FSH) and hMG. They were compared to two randomized control groups of patients who received the same induction but were classically monitored. There was a high proportion of spontaneous ovulations in the programmed group (8/42) compared to the nonprogrammed group (0/42). There was a nonsignificant difference in the number of oocytes obtained or embryos replaced per cycle. Four pregnancies were obtained in the programmed group (24% per transfer), against 10 in the nonprogrammed patients (32% per transfer). The results of this method seem to be better using FSH for ovulation stimulation and a verification of the serum estradiol on the day of induction with human chorionic gonadotropin (hCG) and the following day (semiprogrammed method).

Adult↗

PubMed1977

Evaluation of hypercoagulability in users of oral contraceptives.

Soluble fibrin monomer complexes (SFMC) were determined in users of different oral contraceptives. Quantitative gel filtration of beta-alanin precipitated plasma samples yielded the relative (per cent of total fibrinogen content) and absolute (mg per 100 ml plasma) amount of SFMC. Increased levels of SFMC were observed in users of oral contraceptives, when compared to age, parity and socioeconomic background matched control groups. This increase was more pronounced in users of Neogynon (0.05 mg ethinyl estradiol, 0.25 mg norgestrel) than in the one using Microgynon (0.03 mg ethinyl estradiol, 0.15 mg norgestrel). Users of Ovulen (0.1 mg mestranol, 1 mg ethynodiol diacetate) in addition to the rise of SFMC levels exhibited elevated fibrinogen levels in plasma. The data presented indicate a limited state of hypercoagulability in users of oral contraceptives.

Adult↗

PubMed1981

Effects of steroids on the in vitro forward migration of human spermatozoa.

The effects of 14 steroids at concentrations between 0.1 and 10 micrograms/ml on human spermatozoal forward migration in vitro were tested. Oestradiol-17 beta at a concentration of 0.1 microgram/ml significantly activated spermatozoal forward migration in ejaculated human semen. However, the effect of oestradiol-17 beta at concentrations of 2 and 10 micrograms/ml on ejaculated human sperm motility was not significantly different from the control where no steroid was added. Progesterone, testosterone, oestriol, oestrone, oestradiol-17d, and ethinyl oestradiol significantly inhibited human spermatozoal forward migration at concentrations of 10 micrograms/ml. Chlormadinone acetate and medroxyprogesterone acetate at concentrations of 2 and 10 micrograms/ml significantly inhibited human spermatozoal forward migration, while norethynodrel, ethynodiol diacetate, norgestrel and lynoestrenol significantly inhibited human spermatozoal forward migration at concentrations between 0.1 and 10 micrograms/ml. However, norethindrone had no demonstrable effect on human spermatozoal forward migration at the above concentrations.

Dose-Response Relationship, Drug↗