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PubMed1986

[Inhibition of ovulation with 35 micrograms of ethinyl estradiol and 2 mg of cyproterone acetate (Diane 35)].

In the study reported here the ovulation inhibition dose for cyproterone acetate was determined. Experiments showed that the ovulation inhibition dose is 1 mg of cyproterone acetate, administered daily. Results proved that the cyproterone acetate dose cannot be reduced when cyproterone acetate is combined with ethinyl estradiol. However, the objective of this study was to determine whether it is possible to reduce the estrogen dose to 35 micrograms when the common combination of 2 mg cyproterone acetate and ethinyl estradiol is being used. After a control menstruation cycle, 2 mg cyproterone acetate and 35 micrograms ethinyl estradiol were administered daily to six women with normal menstruation. Drug administration began on Day 5 and ended on Day 25. During the control cycle, the first treatment cycle, and the third treatment cycle, LH, FSH, 17 beta estradiol, progesterone, testosterone, prolactin, and SHGB were examined daily. Cervix score and karyopyknosis index were determined at the same time. In addition, antithrombin III was examined during the control cycle and during the third treatment cycle. Present results show that ovulation inhibition is possible with dose reduction of ethinyl estradiol to 35 micrograms, combined with 2 mg of cyproterone acetate. Increase in SHBG and reduction in testosterone serum level point to an additional antiandrogenic effect of cyproterone acetate, aside from its cellular effect. The combined preparation discussed here does not bring about any changes in antithrombin III values. Results permit the conclusion that ovulation inhibition is insured with a reduction of the daily estrogen dose from 50 micrograms to 35 micrograms.

Adult↗
PubMed1979

Plasma levels of active ingredients after single and repeated administration of a new oral contraceptive containing 2 mg of cyproterone acetate and 50 micrograms of ethinyl estradiol (DIANE) to five young women.

Peripheral plasma from five young women was analyzed for cyproterone acetate and ethinyl estradiol during a period of 96 hours duration after single oral intake of a coated tablet of DIANE (2 mg of cyproterone acetate + 50 micrograms of ethinyl estradiol), and during a treatment cycle of 21 days during which the formulation was given daily. Radioimmunoassays were utilized for quantifications. A maximum concentration of 11.0 +/- 3.4 ng of cyproterone acetate/ml plasma was found 1.6 +/- 0.6 hours after a single administration of DIANE. Postmaximal disposition took place in two phases with half-lives of 1.9 +/- 0.6 hours and 2.2 +/- 0.2 days. The maximum level of 0.08 +/- 0.03 ng of ethinyl estradiol/ml plasma was found 1.6 +/- 0.6 hours after such single administration. Following commencement of a daily oral intake of DIANE a steady state was reached by the 5th to 8th days, during which 24 hours after each dose cyproterone acetate concentrations were found to be 2.4 +/- 0.7 times higher than at the corresponding time after a single administration. Accordingly, after the first third of the 21 day treatment cycle an almost constant plasma level was reached indicating an equilibrium of intake and elimination. Except for a change in the mean terminal half life after multiple dosing, there was evidently no change in the kinetics of cyproterone acetate. No pointers to an accumulation of ethinyl estradiol upon daily administration of DIANE could be found.

Adult↗
PubMed1999

Effects of low-dose monophasic levonorgestrel with ethinyl estradiol preparation on serum lipid levels: A twenty-four month clinical trial.

OBJECTIVE: The aim of this 24-cycle study was to evaluate the effects on serum lipid concentrations of an oral contraceptive preparation containing 100 microg levonorgestrel and 20 microg ethinyl estradiol. STUDY DESIGN: Forty-two healthy women were enrolled in a study designed to evaluate the effects on serum lipid concentrations of an oral contraceptive containing 100 microg levonorgestrel and 20 microg ethinyl estradiol. Lipid data were evaluated for 28 women who completed 24 cycles of treatment with a preparation of 100 microg levonorgestrel with 20 microg ethinyl estradiol for 21 days followed by placebo for 7 days. Concentrations of triglycerides, total cholesterol, high-density lipoprotein cholesterol, high-density lipoprotein cholesterol subfractions 2 and 3, low-density lipoprotein cholesterol, and apolipoproteins A-I and B were analyzed. Mean percentage changes from baseline were tested for significance by means of paired Student t tests. RESULTS: Total cholesterol, high-density lipoprotein cholesterol, high-density lipoprotein subfraction 2, and apolipoprotein A-I concentrations were not significantly changed from baseline. Neither was the ratio of high-density lipoprotein subfraction 2 to high-density lipoprotein subfraction 3. Mean percentage increases in concentrations of triglyceride, high-density lipoprotein subfraction 3, apolipoprotein B, and low-density lipoprotein cholesterol and increases in the ratios of total cholesterol to high-density lipoprotein cholesterol, low-density lipoprotein cholesterol to high-density lipoprotein cholesterol, and apolipoprotein B to apolipoprotein A-I were significant (P <.05) at >/=1 cycle. By cycle 24, however, only the concentration of high-density lipoprotein subfraction 3 remained significantly elevated. CONCLUSION: Changes in the plasma lipid profiles among women receiving monophasic 100 microg levonorgestrel with 20 microg ethinyl estradiol were similar to those seen with other low-dose oral contraceptives, but by cycle 24 only 1 of 7 mean values remained significantly different from baseline.

Adult↗
PubMed1980

Ethinyl estradiol and conjugated estrogens as postcoital contraceptives.

Five study centers enrolled 1,311 women seeking postcoital contraception methods. Ethinyl estradiol was administered at 5 mg/day and conjugated estrogens at 30 mg/day for five consecutive days starting within 72 hours of unprotected coitus. Eleven pregnancies occurred in the 976 women who had a single unprotected coitus at midcycle. Based on published information, 69 pregnancies would have been expected if no contraceptives were used. Although both treatments were effective in preventing pregnancy, ethinyl estradiol seemed to be more effective. At the two centers alternately prescribing both drugs, none of 137 women treated with ethinyl estradiol became pregnant, while six of the 132 given conjugated estrogens became pregnant. Women whose treatment commenced on the first postcoital day seemed to have lower pregnancy rates than those whose medication was delayed to the second or third postcoital day regardless of which drug was used. Side effects were mainly limited to nausea that occurred in 70% and vomiting that was experienced by 33% of all women treated.

Adolescent↗
PubMed1999

Oral contraceptives that contain ethinyl estradiol (0.035 mg) and cyproterone acetate (2 mg) inhibit leukocyte transmigration through endothelial cell monolayers.

OBJECTIVE: To investigate the influence of ethinyl estradiol and cyproterone acetate in oral contraceptives on leukocyte migration through endothelial cell monolayers. DESIGN: Experimental in vitro prospective study. SETTING: An academic research laboratory. INTERVENTION(S): Endothelial cells were cultured on microporous membranes to produce monolayers. Polymorphonuclear leukocytes were used in a previously described migration assay (n = 7). The amount of untreated polymorphonuclear leukocytes that migrated through untreated endothelial cell monolayers was used as a control and set at 100%. In addition, a leukocyte adhesion assay was used. MAIN OUTCOME MEASURE(S): Leukocyte adhesion to and transmigration through endothelial cell monolayers. RESULT(S): Ethinyl estradiol and cyproterone acetate inhibited the migration of polymorphonuclear leukocytes through endothelial cell monolayers significantly (67% +/- 6.4%) when both cell types were treated to simulate in vivo conditions. The adhesion assay produced similar results. CONCLUSION(S): Ethinyl estradiol and cyproterone acetate were identified as potent inhibitors of leukocyte migration through endothelial cell monolayers.

Cell Adhesion↗
PubMed2003

Oral feeding with ethinyl estradiol suppresses and treats experimental autoimmune encephalomyelitis in SJL mice and inhibits the recruitment of inflammatory cells into the central nervous system.

There is much interest in the possible ameliorating effects of estrogen on various autoimmune diseases. We previously established the protective effects of 17 beta-estradiol (E2) on experimental autoimmune encephalomyelitis (EAE). In the current study we investigated the effectiveness of oral treatment with ethinyl estradiol (EE) on EAE and the mechanisms involved. Ethinyl estradiol is a semisynthetic estrogen compound found in birth control pills, and its chemical structure allows this compound to retain activity when given orally. We found that oral EE, like E2, drastically suppressed EAE induced by proteolipid protein 139-151 peptide when given at initiation of EAE. However, unlike E2, EE reduced clinical severity when given after the onset of clinical signs. Treatment with EE significantly decreased the secretion of proinflammatory cytokines (IFN-gamma, TNF-alpha, and IL-6) by activated T cells as well as the expression of a key matrix metalloproteinase, disease-mediating chemokines/receptors, and IgG2a levels, but increased the expression of TGF-beta 3 in the CNS. The absence of infiltrating lymphocytes together with the suppression of cytokines, matrix metalloproteinase, and chemokines/receptors suggests that EE, like E2, protects mice from EAE by inhibiting the recruitment of T cells and macrophages into the CNS. These results suggest that oral ethinyl estradiol might be a successful candidate as therapy for multiple sclerosis.

Administration, Oral↗
PubMed1987

Oral contraception with a triphasic combination of gestodene and ethinyl estradiol: results of a multicenter clinical study.

The clinical effects of a low-dose triphasic oral contraceptive containing the new progestogen gestodene and ethinyl estradiol were investigated in phase II and III multicenter studies. The phase II study compared the clinical effects in 377 women taking this new compound during 2123 cycles with the effects of a low-dose triphasic combination of levonorgestrel and ethinyl estradiol in 362 women treated in 2088 cycles. The discontinuation rates after 6 months were similar in the two groups, and no major differences in side effects were observed. Cycle control was better during intake of the gestodene-containing preparation, since spotting occurred less frequently (P less than .05). The phase III investigation comprised 1921 women representing a total of 27,308 cycles. The Pearl index was 0.05. During the 24-month trial, 243 women (12.7%) dropped out of the study because of side effects, mainly bleeding disturbances (6.0%), headache (2.2%), and breast tension (2.0%). The results of these studies indicate that the triphasic combination of gestodene and ethinyl estradiol is well tolerated and provides high contraceptive efficacy and good cycle control.

Clinical Trials as Topic↗
PubMed1999

The effects of a low-dose monophasic preparation of levonorgestrel and ethinyl estradiol on coagulation and other hemostatic factors.

OBJECTIVE: This study was undertaken to evaluate the effects on hemostatic factors of a low-dose preparation of levonorgestrel and ethinyl estradiol in a 12-cycle study. STUDY DESIGN: Thirty healthy women began taking 100 microg levonorgestrel and 20 microg ethinyl estradiol on the first day of the menstrual cycle, continued to take the preparation for the next 21 days, and then took placebo for 7 days. Mean changes in prothrombin time, partial thromboplastin time, and levels of factors VII and X, antithrombin, plasminogen, fibrinogen, protein S, thrombin-antithrombin complexes, and D-dimer were analyzed at baseline and at cycles 3, 6, and 12 with paired Student t tests. RESULTS: Factor X, plasminogen antigen and activity, and D-dimer levels were significantly increased (P </=.01) during all 3 cycle periods. Antithrombin antigen and protein S total antigen levels were significantly (P </=.001 ) decreased at cycles 3, 6, and 12, whereas factor VII and protein S activity levels were significantly (P </=.05) decreased at cycle 3 and at cycles 3 and 6, respectively. CONCLUSION: The effects on hemostatic factors in healthy women of a monophasic preparation of 100 microg levonorgestrel and 20 microg ethinyl estradiol were similar to those of other low-dose oral contraceptives.

Adult↗
PubMedDate not supplied

The duration of response to norgestimate and ethinyl estradiol in the treatment of acne vulgaris.

OBJECTIVE: This was a postmarketing, retrospective, exploratory analysis to investigate the duration of response to a triphasic combination oral contraceptive (OC) (Ortho Tri-Cyclen; Ortho-McNeil Pharmaceutical, Raritan, NJ) [norgestimate-ethinyl estradiol]) in the treatment of moderate acne vulgaris. PROCEDURES: Healthy women with moderate acne vulgaris were enrolled in two 6-month, multicenter, randomized, double-blind, placebo-controlled clinical trials. Subjects received either 3 weeks of active OC treatment (i.e., 0.035 mg ethinyl estradiol plus increasing doses of norgestimate [0.180 mg, 0.215 mg, 0.250 mg]) and 1 week of inactive tablets, or 4 weeks of color-matched placebo tablets. RESULTS: A total of 507 subjects were enrolled in the study. Duration of response was analyzed in subjects with at least slight improvement in global progress of treatment from the earliest cycle showing response (n = 305) and in subjects with at least slight improvement at or before cycle 3 (n = 276); the duration of response was statistically significant in favor of the norgestimate-ethinyl estradiol group in both cases (P < or = .001). The variability of mean percent change in lesions was also statistically significantly greater in the placebo group than in the OC group for total lesions (P < or = .001) and inflammatory lesions (P < or = .001). CONCLUSION: A triphasic combination of norgestimate and ethinyl estradiol lengthens the time interval to recurrence of acne lesions.

Acne Vulgaris↗
PubMed1997

Double-blind, randomized, placebo controlled study on the effects of the monophasic oral contraceptive containing 30 micrograms ethinyl estradiol and 2.00 mg dienogest on the hemostatic system.

Forty healthy female volunteers aged between 19 and 35 years (27.3 +/- 4.1 years) with normal menstrual cycles were included in a double-blind, randomized, placebo-controlled study to investigate the influence on the hemostatic system of an oral contraceptive containing 30 micrograms ethinyl estradiol in combination with 2.00 mg dienogest, which is a 19-norprogestin without a 17 alpha-ethinyl group. At baseline and during one treatment cycle, 12 hemostatic parameters were measured on cycle days 7, 14, and 21. The hemostatic parameters were categorized as either procoagulatory, anticoagulatory and profibrinolytic, or antifibrinolytic and indicative of fibrin turnover. Differences between placebo and 30 micrograms ethinyl estradiol and 2.00 mg dienogest of plasma levels of hemostatic parameters on cycle days 21 of the precycle and treatment cycle were chosen as target variables. Prothrombin fragment 1 + 2 (F 1 + 2) was chosen as the main target variable. Equivalence of F 1 + 2 between placebo and active treatment was noted. Among the procoagulatory factors, only factor VII activity was found to be increased over placebo in the active treatment group, but decreased in the placebo group. Protein C activity increased during the treatment with 30 micrograms ethinyl estradiol and 2.00 mg dienogest, and was higher than that of the placebo group in which this parameter decreased during the treatment cycle. There was a corresponding increase in fibrinolytic activity being reflected by higher plasminogen levels in the active treatment group in comparison with placebo. An increase was noted for the fibrinolytic parameter D-dimer. Apart from isolated measurements, the parameters remained in their respective normal ranges. The data combine to suggest that 30 micrograms ethinyl estradiol and 2.00 mg dienogest has a balanced effect on the hemostatic system stimulating both procoagulatory and fibrinolytic activity.

Adult↗
PubMed1999

The effects on ovarian activity of a monophasic oral contraceptive with 100 microg levonorgestrel and 20 microg ethinyl estradiol.

An open-label, single-center, noncomparative study was conducted to determine the effects of a monophasic oral contraceptive containing 100 microg levonorgestrel and 20 microg ethinyl estradiol on ovarian activity. The subjects were 26 healthy women 20 to 35 years of age who had normal ovulatory cycles and were not at risk for becoming pregnant. For 3 treatment cycles, they took 1 tablet of active drug daily for 21 days followed by placebo tablets for 7 days. Follicle diameters and serum progesterone and 17beta-estradiol levels were measured before, during, and after treatment. In 2 (2.7%) of 73 cycles, luteinized unruptured follicles were present and in another 2 (2.7%) cycles, ovulation was confirmed by the disappearance of the enlarged follicle. Ovarian activity, as reflected by mean serum progesterone levels, was restored after treatment. The results of this study are in agreement with those of other studies that showed suppression of ovarian activity in women treated with a monophasic oral contraceptive containing 100 microg levonorgestrel and 20 microg ethinyl estradiol. These results indicate that low-dose 100 microg levonorgestrel and 20 microg ethinyl estradiol given for 21 days is effective in suppressing ovarian activity and they confirm the contraceptive efficacy observed in clinical trials (Pearl index of 0.8).

Adult↗
PubMed1997

Norgestimate and ethinyl estradiol in the treatment of acne vulgaris: a randomized, placebo-controlled trial.

OBJECTIVE: To evaluate the efficacy of a triphasic, combination oral contraceptive (OC), (norgestimate-ethinyl estradiol), in comparison with placebo in the treatment of moderate acne vulgaris. METHODS: Two hundred fifty women were enrolled in a multicenter, randomized, double-blind, placebo-controlled clinical trial to evaluate the effectiveness of norgestimate-ethinyl estradiol in the treatment of acne vulgaris. Subjects were 15-49 years old and had moderate acne vulgaris. Each month for 6 months, subjects received either 3 consecutive weeks of active OC treatment followed by 1 week of inactive drug, or 4 consecutive weeks of color-matched placebo tablets. Efficacy was assessed by facial acne lesion counts, the investigator's global assessment, and the subject's self-assessment. Hormone levels were also measured. RESULTS: Despite the large placebo effect inherent in an acne trial (due to, for example, careful skin care, frequent office visits, regression to the mean), of the 164 subjects who completed the study without major protocol deviations, the OC group was significantly better than the placebo group for all primary efficacy measures: inflammatory lesions (mean reduction, 51.4% compared to 34.6%; P = .01), total lesions (mean reduction, 46.4% compared to 33.9%; P = .001); investigator's global assessment (83.3% compared to 62.5%; P = .001). Free testosterone decreased significantly and sex hormone-binding globulin increased significantly in the OC group, but remained unchanged in the placebo group. CONCLUSION: A triphasic combination of norgestimate and ethinyl estradiol is an effective treatment for moderate acne vulgaris in women with no known contraindication to OC therapy.

Acne Vulgaris↗
PubMed1984

Enhancement of hepatocarcinogenesis in female rats by ethinyl estradiol and mestranol but not estradiol.

The effect of dietary exposure to synthetic estrogens on hepatocarcinogenesis was evaluated. Diethylnitrosamine-initiated and 0.85% NaCl solution-treated noninitiated female Sprague-Dawley rats were transferred to semisynthetic diets containing mestranol (0, 0.1, or 0.5 ppm), ethinyl estradiol (0.5 ppm), estradiol (0.6 ppm), or mestranol plus beta-methasone (0.5 and 0.2 ppm, respectively). gamma-Glutamyl transferase (GGT)-positive transections and hematoxylin and eosin-detectable nodules and carcinomas were scored at 9 and 12 months. Quantitative stereological calculations were performed to determine GGT lesion number and size. At 9 months, in diethylnitrosamine-initiated rats, ethinyl estradiol and mestranol caused 3.5- and 4.4-fold increases, respectively, in the number of GGT lesions per liver and an increased incidence of hepatocellular carcinomas while estradiol had no enhancing effect. Addition of beta-methasone to the mestranol-containing diet caused a significant decrease in GGT lesion number but not carcinoma incidence compared to mestranol alone. At 12 months, in diethylnitrosamine-initiated rats, mestranol caused a dose-dependent increase in GGT lesion number. The hepatocellular carcinoma incidence was significantly increased at the high mestranol dose. Small increases in the numbers of larger GGT lesions were also observed in noninitiated animals treated with mestranol and ethinyl estradiol and are most probably due to promotion of spontaneously initiated hepatocytes. These results indicated that the synthetic estrogens cause dramatic increases in the number of presumptive preneoplastic GGT lesions. Carcinoma incidence is also enhanced. Thus, these results confirm and extend our previous studies which together with the results of others have shown that synthetic estrogens can act as promoters of hepatocarcinogenesis.

Animals↗
PubMed1982

Determination of ethinyl estradiol in solid dosage forms by high-performance liquid chromatography.

A rapid, reproducible high-performance liquid chromatographic system for the determination of ethinyl estradiol in solid dosage forms consisting of a reversed-phase column with a mobile phase of 0.05 M aqueous KH2PO4-methyl alcohol (2:3) and fluorescence detection has been developed. This stability-indicating method is applicable to tablets containing ethinyl estradiol alone or in combination with methyltestosterone and progesterones. The procedure has been used for the determination of ethinyl estradiol in single tablets, stability samples, and dissolution medium. Recovery of drug substance added to placebo was from 97.3 to 101.5% in stability and single-tablet assays, and 95.4 to 102.2% in dissolution assays. Reproducibility studies gave relative standard deviations of 0.4-2.2%.

Chromatography, High Pressure Liquid↗
PubMed1984

Hepatocyte taurocholic acid uptake in the regression of ethinyl estradiol cholestasis. Preliminary results.

Taurocholic uptake in ethinyl estradiol cholestatic rats is significantly lower than in untreated rats. In the days following treatment withdrawal there is only a slow increase in uptake, which is still statistically lower than normal at the 11th day. Taurocholic acid uptake behaves in a different way from biliary flow and the amount of excreted bile acids. The diversity could be attributed to a different behaviour of bile acid carriers at the sinusoidal and biliary membranes in the hepatocyte or to a normalisation of bile acid carriers and Na+,K+,-ATPase activity at different times.

Animals↗
PubMed1977

Low-dose combination oral contraceptives: a controlled clinical study of three different norgestrel-ethinyl estradiol ratios.

Three doses of norgestrel-ethinyl estradiol in altered ratios were investigated in a double-blind, randomized study. The estrogen content was maintained at 20 microng or less, while the progestogen dose was increased in 100-microng increments. Two pregnancies were reported for the lowest dose. No pregnancies occurred in the two higher doses. Each dosage increase improved cycle control and lessened bleeding irregularities. The incidence of patients reporting intermenstrual bleeding was inversely proportional to the doses studied. Dropouts for cycle disturbances followed a similar pattern.

Adult↗
PubMedDate not supplied

[Effect of 17 alpha-ethinyl estradiol on the blood serum lipid indices of rats].

The administration of 17-ethinyl estradiol (0.25 mg/kg) to male Wistar rats caused on the 3rd day a decrease of the levels of free and esterified cholesterol, blood serum triglycerides and also a reduction of the content of esterified cholesterol with respect to total cholesterol while the lecithin-cholesterol-acyltransferase activity appeared to be unchanged. The effect of ethinyl estradiol on blood lipid parameters against the background of lipemia induced by triton WR 1339 was reduced.

Animals↗