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PubMed1996

An open randomized comparative study of an oral contraceptive containing ethinyl estradiol and cyproterone acetate with and without the GnRH analogue goserelin in the long-term treatment of hirsutism.

A multicenter randomized study was carried out to compare the efficacy of combined therapy with a GnRH analog (goserelin) + an oral contraceptive (OC) containing ethinyl estradiol and cyproterone acetate and same OC alone in the treatment of severe hirsutism. The effect of these two therapies was assessed in a subjective and an objective evaluation of hair growth. According to the subjective evaluation, judged by physician and patient. 95% of patients obtained a partial response. The objective response was assessed by measuring the mean diameter of hair from 3 different areas and 1 control area. The decrease in hair diameter compared to pretreatment was statistically significant for both treatments, mainly for the abdomen and face. The difference between the two groups did not reach statistical significance. Therefore, we assume that OC alone remains the treatment of choice for hirsutism. However, the addition of the GnRH analog to OC needs further investigation and could be justified for patients with no response to standard monotherapy.

Acne Vulgaris↗

PubMed1997

A multicenter, uncontrolled clinical investigation of the contraceptive efficacy, cycle control, and safety of a new low dose oral contraceptive containing 20 micrograms ethinyl estradiol and 100 micrograms levonorgestrel over six treatment cycles.

The aim of the trial was to demonstrate the contraceptive efficacy of a new low dose oral contraceptive containing 20 micrograms ethinyl estradiol and 100 micrograms levonorgestrel and to observe cycle control and safety. Data from 805 treated women resulted in 4400 treatment cycles. One pregnancy occurred while on the trial medication as a result of method failure, resulting in a Pearl index of 0.29. Cycle control was good, and cycle length as well as duration and intensity of withdrawal bleeding were not significantly changed during the trial. Intermenstrual bleeding usually occurred as spotting and decreased considerably during the treatment phase. Spotting alone was reported in 12.4% of cycles, breakthrough bleeding alone in 4.5% of cycles, and breakthrough bleeding and spotting together in 1.4% of treatment cycles. The rate of absence of withdrawal bleeding declined throughout the trial to 2.4% in cycle 6. There were no serious adverse events related to treatment, and most adverse events were those commonly observed in clinical trials with oral contraceptives. Headache, breast tension, and nausea were reported by 17.3%, 11.0%, and 7.7% of the women, respectively. There were no clinically relevant changes in laboratory parameters, blood pressure, or weight. In this trial, the new low dose oral contraceptive containing 20 micrograms ethinyl estradiol and 100 micrograms levonorgestrel was shown to be effective, safe, and well tolerated. Cycle control was found to be good and there was a low incidence of adverse events.

Adolescent↗

PubMed2003

The risk of venous thromboembolism in women prescribed cyproterone acetate in combination with ethinyl estradiol: a nested cohort analysis and case-control study.

BACKGROUND: Cyproterone acetate combined with ethinyl estradiol (CPA/EE) is licensed in the UK for the treatment of women with acne and hirsutism and is also a treatment option for polycystic ovary syndrome (PCOS). Previous studies have demonstrated an increased risk of venous thromboembolism (VTE) associated with CPA/EE compared with conventional combined oral contraceptives (COCs). We believe the results of those studies may have been affected by residual confounding. METHODS: Using the General Practice Research Database we conducted a cohort analysis and case-control study nested within a population of women aged between 15 and 39 years with acne, hirsutism or PCOS to estimate the risk of VTE associated with CPA/EE. RESULTS: The age-adjusted incidence rate ratio for CPA/EE versus conventional COCs was 2.20 [95% confidence interval (CI) 1.35-3.58]. Using as the reference group women who were not using oral contraception, had no recent pregnancy or menopausal symptoms, the case-control analysis gave an adjusted odds ratio (OR(adj)) of 7.44 (95% CI 3.67-15.08) for CPA/EE use compared with an OR(adj) of 2.58 (95% CI 1.60-4.18) for use of conventional COCs. CONCLUSIONS: We have demonstrated an increased risk of VTE associated with the use of CPA/EE in women with acne, hirsutism or PCOS although residual confounding by indication cannot be excluded.

Acne Vulgaris↗

PubMed2002

Effects of ethinyl estradiol, estradiol, and testosterone on hindlimb endothelial function in vivo.

SUMMARY: This study was designed to evaluate the effects of chronic treatment with estrogen and testosterone on hindlimb vascular function. Spontaneously hypertensive rats (SHR) were sham-operated (SHAM) or ovariectomized and treated with vehicle (OVX), ethinyl estradiol (OVX-EE2), estradiol (OVX-E2), or testosterone (OVX-TESTO) for 3 weeks. Anesthetized SHR were instrumented for the measurement of arterial blood pressure and hindlimb blood flow. Ovariectomy had no significant effect on hindlimb resistance. Resting blood pressure (mm Hg) and hindlimb resistance (mm Hg/ml/min/kg) were higher in OVX-TESTO (158 +/- 4 and 4.7 +/- 0.3) than SHAM control (130 +/- 6 and 3.3 +/- 0.4), OVX (139 +/- 6 and 3.4 +/- 0.3), OVX-EE2 (130 +/- 4 and 3.0 +/- 0.3), and OVX-E2 (120 +/- 4 and 3.3 +/- 0.4). The hemodynamic responses to the endothelium-dependent vasodilator acetylcholine (ACh) were similar in SHAM, OVX, OVX-EE2, and OVX-E2. The hindlimb vasodilatory effects of ACh were consistently greater in OVX-TESTO compared with OVX, OVX-EE2, OVX-E2, and SHAM control rats. The hemodynamic responses to the nitric oxide donor, sodium nitroprusside, were similar in all groups. Our results provide evidence of modulatory influence of testosterone on vasomotor function. It is suggested that the enhanced hindlimb endothelial function represents a compensatory mechanism for testosterone-induced hypertension.

Animals↗

PubMedDate not supplied

[Contraceptive activity and mechanism of action of combinations of a new 17 alpha-acetoxyprogesterone derivative and ethinyl estradiol].

It was shown in experiments on rats and rabbits that a new derivative of 17 alpha-acetoxyprogesterone--mepregnol diacetate--combined with ethinyl estradiol in varied doses and ratios elicits a pronounced contraceptive effect. This steroid combination exerts neither antigonadotropic nor antiovulatory action. The changes detected in the RNA content are apparently of importance in the mechanism of the drug effect on reproduction. A role has been demonstrated of the central cholino- and adrenoreactive systems in providing the contraceptive effect of decreased doses of ethinyl estradiol and mepregnole diacetate.

Animals↗

PubMed1994

Lipoprotein alterations from a triphasic oral contraceptive containing ethinyl estradiol and gestodene. A 12-month trial.

To evaluate the lipid and lipoprotein changes induced by a triphasic oral contraceptive (OC) containing ethinyl estradiol and gestodene, 25 healthy women from the Baltimore metropolitan area were enrolled in an open-label, noncomparative study. Serum lipids were measured prior to starting the OCs and again during the 3rd, 6th and 12th treatment cycles. Mean lipid concentrations in each treatment cycle were compared to baseline levels using the t test for paired samples. Small but statistically significant (P < or = .05) increases in the mean concentrations of total cholesterol, total triglycerides, total high density lipoprotein (HDL) cholesterol, HDL3 cholesterol, apolipoprotein A1 and apolipoprotein B were noted. Although the increases were statistically significant, the mean lipid concentrations were still within the normal range. The mean HDL2 and low density lipoprotein cholesterol concentrations were unchanged, as was the mean total cholesterol/HDL ratio. Healthy women taking a triphasic OC containing ethinyl estradiol and gestodene have minimal changes in lipids and should not be at increased risk of atherosclerosis due to OC-induced lipid alterations.

Adult↗

PubMed2000

Inhibition of gonadotropin surge by a brief mid-cycle regimen of ethinyl estradiol and norethindrone: possible role in in vitro fertilization.

Various methods to prevent premature luteinizing hormone (LH) surge and improve cycle control during hyperstimulation for in vitro fertilization (IVF) are standard of care. The purpose of the present study was to determine the influence of a 5-day regimen of ethinyl estradiol (EE) and norethindrone (NET) on folliculogenesis, gonadotropin surge, and ovulation. In a prospective randomized and comparative study, ten patients were assigned to two groups. A combination of 50 micrograms of EE and 1 mg of NET was used in groups I and II from days 6 through 10, and days 8 through 12, respectively. Blood samples and transvaginal ultrasound imaging were carried out throughout a 28-day cycle. Follicular diameter, plasma levels of LH, follicle-stimulating hormone (FSH), estradiol and progesterone, and endometrial thickness were determined. No LH surge or ovulation was detected in any patient studied. Peak estradiol concentrations were not significantly different between the groups (152.04 +/- 107.1 pg/ml vs 162.1 +/- 56.1 pg/ml [mean +/- SD] for groups I and II, respectively). No differences were noted between the groups for serum concentrations of FSH (range: 2-9 mIU/ml) or LH (range: 2-10 mIU/ml) for any given cycle day. Mean follicular diameters were not different between groups I and II (20.5 +/- 8.1 mm2 vs 20.6 +/- 14.2 mm2). Ultrasound assessment of mid-cycle follicular growth revealed diameters ranging from 18.5 mm2 to 34.0 mm2. Endometrial thickness ranged from 8 to 10 mm. There was no evidence of ovulation on ultrasound examination and either persistence or gradual resolution of follicles through the luteal phase. Peak serum concentrations at mid-luteal phase were < or = 2 ng/ml. In this pilot study, the combination of EE and NET restricted to a 5-day course beginning on day 6 or 8 permitted folliculogenesis but effectively inhibited midcycle LH surge and ovulation. Such regimens may have a role in IVF cycles for prevention of premature LH surges, especially as stimulation regimens evolve toward decreased gonadotropin use for stimulation and strict FSH preparations with the potential need for less complete pituitary suppression.

Adult↗

PubMed1992

Effects of ethinyl estradiol on semen quality and various hormonal parameters in a eugonadal male.

OBJECTIVE: To determine the influence of estrogens on male fertility. DESIGN: A 36-year-old eugonadal male was subjected to two different regimens of treatment with ethinyl estradiol (EE2). Sperm quality, immunoreactive luteinizing hormone (LH) and follicle-stimulating Hormone (FSH), testosterone (T), estrone (E1), estradiol (E2), dehydroepiandrosterone sulfate (DHEAS), prolactin (PRL) and sex hormone-binding globulin were determined at intervals of 2 weeks for 315 days. SETTING: A gender dysphoria clinic. PATIENT: A transsexual male nurse. MAIN OUTCOME MEASURES: It was hypothesized (and confirmed) that by comparing the effects of increasing and constant dose of EE2 on fertility parameters, differences in estrogen-sensitivity would show more clearly. Furthermore, this procedure served to find the minimal dose of EE2 for complete testicular suppression. RESULTS: Low doses of EE2 (20 micrograms/d) had no negative effect on sperm motility and density for a period of approximately 4 weeks, whereas high doses (60 micrograms/d) reduced motility already after a few days and led to a pronounced decrease in sperm density after 2 weeks. After discontinuation of therapy, motility normalized faster than sperm density. Under increasing doses of EE2 there was a constant decrease of FSH that occurred several weeks earlier than that of LH. Under constant dose of EE2 (60 micrograms/d) the decrease of LH was delayed (with respect to FSH) by only a few days. The decrease in T showed a stronger correlation with that of FSH than with that of LH. Volume and fructose content of the seminal fluid correlated with the decrease in T. Rebound effects were observed for FSH, LH, T, and fructose during the therapy-free interval. Ethinyl estradiol therapy had no influence on the serum concentrations of E1, E2, and PRL. Estrone was the dominant estrogen before and after therapy with EE2. Adrenal gland activity was markedly suppressed by EE2, as reflected by the decrease in DHEAS. CONCLUSION: The suppressive effect of EE2 on FSH and sperm motility was more pronounced and consistent than on LH and sperm density. The T decrease appears to be mainly caused by a direct effect of EE2 on the testes.

Adult↗

PubMed1989

Bioequivalence of two oral contraceptive drugs containing norethindrone and ethinyl estradiol.

Two oral contraceptive drugs, Formulation A and Formulation B, both of similar hormonal content, were compared with each other to determine if they were bioequivalent. Both drugs contain 1 mg of norethindrone (NET) and 0.035 mg of ethinyl estradiol (EE). Application of an interval test for the ratio of the computed parameter means demonstrated equivalence for the two formulations with respect to the 0-24 hour area under the plasma level versus time curve (AUC24), the total area under the curve (AUCtot) and for the maximum plasma concentration (Cmax) for both ethinyl estradiol and norethindrone. The data support the hypothesis for bioequivalence of the two formulations with respect to total absorption.

Adult↗

PubMed2001

Beneficial effects of low doses of ethinyl-estradiol on the lipid profile in postmenopausal women.

The purpose of this study was to investigate the beneficial effects of low doses of ethinyl-estradiol on the lipid profile in postmenopausal women. One hundred and five patients (mean age [+/-S D] 42.9 +/- 5.0 years) who underwent a hysterectomy and bilateral salpingo-oophorectomy were included in the study. For the present study serum levels of total cholesterol, high-density lipoprotein (HDL) cholesterol, low-density lipoprotein (LDL) cholesterol, triglycerides, apolipoprotein B (apoB), and lipoprotein(a) [Lp(a)] were investigated. When all patients were considered together (Table 1), EE2 therapy significantly increased serum levels of total cholesterol, HDL cholesterol and LDL cholesterol. The ratio of HDL to LDL cholesterol, Lp(a) and triglyceride concentrations did not change significantly from the baseline value. Although our study was not randomized or controlled with a placebo, the beneficial metabolic effects of ethinyl-estradiol on lipid patterns should be considered in patients needing hormonal replacement therapy in postmenopause.

Adult↗

PubMed2001

Pharmacology and toxicology of ethinyl estradiol and norethindrone acetate in experimental animals.

For over 30 years various combinations of synthetic estrogens and progestins have been used in oral contraceptive formulations. Ethinyl estradiol (EE) and norethindrone acetate (NA) are common synthetic hormones used in oral contraceptives such as Loestrin, Brevicon, Ortho-Novum, Norlestrin, and Norinyl. In recent years these oral contraceptives have been considered for development in other therapeutic indications. Given the use of these agents for other clinical indications with different and larger target populations, an updated comprehensive review of the toxicology literature of estrogens and progestins is warranted. This review will summarize available data on the pharmacology and toxicology of estrogens and progestins with an emphasis on the specific synthetic hormones EE and NA. Ethinyl estradiol and norethindrone acetate alone or in combination, possess low acute and chronic toxicity. In some studies, EE and/or NA increased the incidence of specific tumors in susceptible strains of rodents and dogs, but not monkeys. These agents are not teratogenic when given in combination. Alone EE and NA have clastogenic properties. Overall, the animal data demonstrates that long-term exposure to EE and NA formulations pose very little health risks to humans.

Animals↗

PubMed1997

Effects of prolonged ethinyl estradiol treatment on calcium channel binding and in vivo calcium-mediated hemodynamic responses in ovariectomized rats.

Ethinyl estradiol (EE2), administered orally to ovariectomized (ovex) rats, has been shown to prevent loss of bone mineral density and to decrease serum cholesterol levels. Radioligand binding studies with the dihydropyridine (DHP) [3H]PN200-110 were undertaken to characterize calcium (Ca++) channels in cardiac and aortic tissues from ovex rats treated for 35 days with EE2 (0.1 mg/kg day p.o.) or vehicle, and from vehicle-treated sham-operated controls (sham). Cardiac tissues from EE2-treated rats displayed significant increases in the density (Bmax) of high-affinity DHP binding sites (505 +/- 46 fmol/mg) compared with vehicle-treated ovex rats (303 +/- 35 fmol/mg); DHP Bmax values from EE2-treated cardiac tissues were not significantly different from vehicle-treated shams (385 +/- 76 fmol/mg). Cardiac Ca++ efflux channels from sarcoplasmic reticulum were assessed with [3H]ryanodine. [3H]Ryanodine Bmax values were not affected by EE2 treatment. However, [3H]ryanodine Kd values in preparations from EE2-treated rats were significantly decreased (10 +/- 2 nM) compared with ovex rats (35 +/- 11 nM) and were similar to values in sham rats (8 +/- 2 nM). Cardiac beta adrenoceptors were not affected by EE2 treatment, which thus confirmed the selective regulation of DHP receptors by EE2. Aortic preparations from EE2-treated rats exhibited significant increases in DHP receptors (125 +/- 37 fmol/mg) compared with both vehicle-treated ovex rats (32 +/- 3 fmol/mg) and vehicle-treated shams (24 +/- 9 fmol/mg). There were no differences in the binding affinity (Kd) of [3H]PN200-110 for cardiac or aortic sites among the three groups. To ascertain if EE2-mediated increases in Ca++ channel density and ryanodine binding affinity affected in vivo responses to agonists that use extracellular and intracellular Ca++ stores, responses to BAY k 8644 and norepinephrine were examined in pithed rats from the same three groups. No significant differences in hemodynamic responses occurred among the three groups to BAY k 8644 or norepinephrine. Thus, in female ovex rats, prolonged treatment with EE2 resulted in increased density of cardiac and aortic calcium channels which did not translate into increased calcium-mediated inotropic, rate or pressor responses. Conversely, EE2 treatment in ovex rats prevented the decrease in cardiac [3H]ryanodine binding affinity evident in vehicle-treated ovex rats. These data suggest that EE2 treatment in normotensive ovex rats resulted in modulation of both the L-type and sarcoplasmic reticulum Ca++ channels, and these alterations maintained cardiovascular homeostasis.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗

PubMed1986

Ethinyl estradiol and medroxyprogesterone acetate in patients with epithelial ovarian carcinoma: a phase II study.

Patients with ovarian carcinoma refractory to chemotherapy received a sequential combination of ethinyl estradiol and medroxyprogesterone acetate in two dose regimens. There was no difference in therapeutic activity of the two dose regimens. Of 65 patients, nine (14%) responded to treatment and 13 (20%) had stable disease. Vascular complications occurred in three patients; hemiplegia developed in one of those. Nine patients had significant nausea and vomiting, and one experienced severe depression that required treatment withdrawal. The sequential and combined use of ethinyl estradiol and medroxyprogesterone acetate may provide an alternative treatment for certain patients with ovarian carcinoma that does not respond to optimum chemotherapy. Additional studies are required to determine if synergism exists between this treatment and other modalities of therapy. Further investigation is required into the vascular disorders that complicate therapy to determine whether appropriate preventive measures are possible.

Adult↗

PubMed1982

A multicenter clinical investigation employing ethinyl estradiol combined with dl-norgestrel as postcoital contraceptive agent.

Six hundred ninety-two women were enrolled in a multicenter clinical trial to evaluate a combination of ethinyl estradiol and dl-norgestrel as a postcoital contraceptive. When compared with various formulas predicting the probability of pregnancy in this group, the number of pregnancies observed appears to be reduced by approximately 84%. The combination of 200 micrograms of ethinyl estradiol and 2 mg of dl-norgestrel seems to be effective as a postcoital contraceptive with several advantages over estrogens alone.

Adolescent↗

PubMed1985

Combined toxic effects of tetracycline and ethinyl estradiol on liver function of mice.

The combined effects of ethinyl estradiol (EE) (0.5 micrograms/g s.c. once daily for 4 days) and tetracycline (TC) or doxycycline (DC) (50 micrograms/g i.v.) on liver weight and water content, serum transaminases, alkaline phosphatase, urea, triglycerides, and cholesterol as parameters of various liver functions were investigated in mice. It became apparent that depending on the parameter tested synergistic and antagonistic effects may occur, e.g., synergistic effects were observed with the serum transaminases and liver cholesterol; antagonistic effects were seen with the serum urea and serum cholesterol.

Alanine Transaminase↗

PubMed1990

Blood-brain barrier permeability: regional alterations after acute and chronic administration of ethinyl estradiol.

In this study we measured the effect of acute and chronic estrogen treatment on cerebrovascular permeability to sucrose and inulin. Animals were subcutaneously injected once with 0.1 micrograms/rat of ethinyl estradiol or injected daily with the same drug dose for 3 weeks. Control rats received the same amount of arachis oil vehicle. Three weeks treatment but not the single injection of ethinyl estradiol produced significant increases in the cerebrovascular permeability-surface area product for sucrose and inulin in almost all brain regions.

Animals↗

PubMed1991

Androgen synthesis in human fetal testis exposed in utero to a combination of norethindrone acetate and ethinyl estradiol.

The effect of norethindrone acetate (NET-Ac) and ethinyl estradiol (EE2) on the 3 beta-hydroxysteroid dehydrogenase (HSD)-delta5-isomerase complex of the human fetal testis was studied by administration of 20 mg NET-Ac and 0.04 mg EE2 p.o on a single day to 4 women, pregnant 10-16 weeks, before abortion was induced, the other 4 patients serving as controls. Testosterone and androstenedione formation from radioactive dehydroepiandrosterone was measured in 8 fetuses by incubation of testicular tissue in vitro. The presence of normal feta Leydig cells was confirmed by electron microscopy. There was no difference between the enzyme activities of testicles in the experimental and control groups. The findins give values of 3 beta-HSD-isomerase activity in human fetal testis and suggest that the steroidogenic function of the fetal testis exposed for a short time to normally used contraceptive steroids remains at the same magnitude.

Androgens↗

PubMed1990

Regulation of rat hepatocyte epidermal growth factor receptor by the liver tumor promoter ethinyl estradiol.

We have previously demonstrated that the liver tumor promoter ethinyl estradiol (EE) greatly enhanced the DNA synthetic response of rat hepatocytes in primary culture to epidermal growth factor (EGF). This effect was associated with a 2-fold increase in surface EGF receptor number. In this report, we demonstrate that the increase in cell surface [125I]EGF binding caused by EE is time dependent, beginning at 8 h and reaching a plateau at 18 h. This increased EGF binding was accompanied by a comparable increase in the amount of total EGF receptor protein. In vivo, EE treatment also increased the number of EGF binding sites. EE treatment did not increase the rate of [35S]methionine incorporation into immunoprecipitated EGF receptor protein, nor did it appear to affect the steady-state levels of EGF receptor mRNA compared to that found in controls. However, EE treatment did cause an increase in the half-life of EGF receptor protein from 4.5 +/- 0.5 h in control hepatocytes to 10.4 +/- 1.8 h. Taken together, these results indicate that the EE-induced 2-fold increase in EGF receptor levels, which is associated with the potentiation of responsiveness to EGF, was brought about by stabilization of receptor protein.

Animals↗