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PubMed2001

Pharmacokinetics of norelgestromin and ethinyl estradiol from two consecutive contraceptive patches.

The primary objective of this open-label study was to determine the pharmacokinetics of norelgestromin (NGMN) and ethinyl estradiol (EE)following two consecutive applications of a contraceptive patch (ORTHO EVRA/EVRA). Twelve healthy women wore the first patch on their abdomen for 7 days and, after removal at 168 hours (day 7), wore a second patch for 10 days (i.e., 3 days beyond the intended 7-day wear period). Blood samples were collected before and at various times up to 456 hours (day 19) after application of the first patch for analysis of NGMN and EE. Mean serum concentrations of NGMN and EE remained within the reference ranges, 0.6 to 1.2 ng/ml and 25 to 75 pg/ml, respectively, during the entire 7-day wear period after application of the first patch and for 10 days after application of the second patch; reference ranges are based on studies with ORTHO-CYCLEN/ Cilest. No patch detached spontaneously. No subject discontinued or experienced a serious adverse event.

Administration, Cutaneous↗

PubMed1983

Contraception with levonorgestrel, 0.15 mg, and ethinyl estradiol, 0.03 mg. Clinical studies in Latin America.

Levonorgestrel, 0.15 mg, and ethinyl estradiol, 0.03 mg, an ultra-low-dose oral contraceptive product, was studied in Latin America. In total, 1,206 sexually active, fertile women in their reproductive years were followed through 9,736 cycles. Only one of eight pregnancies was attributed to failure of the medication, resulting in a corrected Pearl index of 0.13. Very good cycle regulation was achieved, with an acceptably low rate of intermenstrual bleeding. The medication was discontinued for medical reasons in only 5% of the patients. Apart from a mild case of thrombophlebitis, there were no major side effects. These studies show that this combination oral contraceptive provides effective contraception with a very low incidence of side effects.

Clinical Trials as Topic↗

PubMed1975

Eight years of fertility control with norgestrel-ethinyl estradiol (Ovral): an updated clinical review.

Data on a combination norgestrel-ethinyl estradiol oral contraceptive (Ovral) were obtained from eight large family planning clinics. The safety and efficacy of the drug were evaluated for 6,806 mature, sexually active women who received a total of 127,872 cycles of the medication; this represents 9,836 woman-years of usage. No pregnancy attributable to medication failure occurred, but 19 women who omitted two or more consecutive tablets became pregnant. This produced an overall use-effectiveness pregnancy rate of 0.19/100 woman-years. Cycle control was excellent, and intermenstrual bleeding was rare. Adverse effects were minimal; laboratory values seldom deviated from pretreatment levels. Fertility returned promptly upon withdrawal of the contraceptive, and no infant abnormalities were attributed to its use.

Adrenal Glands↗

PubMed1986

Induction of prostate carcinoma in situ at high incidence in F344 rats by a combination of 3,2'-dimethyl-4-aminobiphenyl and ethinyl estradiol.

Male F344 rats were given a diet containing 0.75 ppm of ethinyl estradiol for 3 weeks and a basal diet for 2 weeks alternately 10 times, and 2 days after each change to basal diet (on the third day of feeding of the basal diet), a single s.c. injection of 50 mg/kg body weight of 3,2'-dimethyl-4-aminobiphenyl. Then they were given the basal diet until week 60 and sacrificed for histological examination. Prostatic carcinomas were found in 18 of 21 rats (85.7%) after this treatment but in only 1 of 19 rats (5.2%) maintained on normal diet throughout the experiment but given 3,2'-dimethyl-4-aminobiphenyl at the same times as the diet given to test rats. All the carcinomas were microscopic and developed in the ventral lobe of the prostate. This method may ultimately lead to a useful animal model of prostatic carcinoma.

Aminobiphenyl Compounds↗

PubMed1980

Differential lipemic and proteinemic response to oral ethinyl estradiol and parenteral estradiol cypionate.

Oral synthetic estrogen administration to normal women has been shown to result in both a lipemic and a proteinemic response. To determine whether parenteral estrogen administration would have similar results, the effects of intramuscular depo-estradiol cypionate on serum lipids and ceruloplasmin were examined. The oral and parenteral estrogens chosen for this study are frequently used therapeutically and varying doses in the range of those commonly employed clinically were given to the experimental subjects. Following oral ethinyl estradiol (20, 50, and 100 micrograms every 12 hr) comparable and significant increases in triglyceride (73 +/- 6 to 128 +/- 10 mg/dl, p < .001), ceruloplasmin (87 +/- 4 to 188 +/- 11 mg/dl, p < .001), and HDL-cholesterol (60 +/- 2 to 74 +/- 3 mg/dl, p < .001) were observed. In contrast, despite substantial increases in serum estrogens, parenteral estrogen administration (depo-estradiol cypionate, 5 and 10 mg) failed to result in alterations in any of the measured parameters. Thus, the route and/or type of estrogen administered may determine the proteinemic and lipemic effects of estrogen in man.

Administration, Oral↗

PubMed2006

Risk of nonfatal venous thromboembolism in women using a contraceptive transdermal patch and oral contraceptives containing norgestimate and 35 microg of ethinyl estradiol.

CONTEXT: There is concern that a new transdermal contraceptive patch containing ethinyl estradiol (EE) and the progestin norelgestromin increases the risk for venous thromboembolism (VTE) compared to previously marketed oral contraceptives (OCs). OBJECTIVE: Quantitative information was obtained on the risk of nonfatal VTE in women using the contraceptive patch in comparison to women using OCs, norgestimate (either monophasic or triphasic) and 35 microg EE (norgestimate-35), an OC that has been marketed for over a decade. DESIGN, SETTING AND PARTICIPANTS: Nested case-control design based on information from PharMetrics, a US-based company that collects and organizes information on claims paid by managed care plans. The study was nested among all women aged 15 to 44, who started either the contraceptive patch or norgestimate-35 after April 1, 2002. Cases were women with current use of one of these two study drugs and a documented diagnosis of VTE in the absence of identifiable clinical risk factors (idiopathic VTE). Up to four controls were matched to each case by age and calendar time. MAIN OUTCOME MEASURES: Odds ratios (ORs) comparing the risk of nonfatal VTE in new users of the two contraceptives and incidence rates of nonfatal VTE for new users of each of the study contraceptives. RESULTS: We identified 68 newly diagnosed, idiopathic cases of VTE in the study population. In the case-control analysis, the OR comparing the contraceptive patch to norgestimate-35 was 0.9 (95% CI 0.5-1.6). The overall incidence rate for VTE was 52.8 per 100,000 women-years (95% CI 35.8-74.9) among users of the contraceptive patch and 41.8 per 100,000 women-years among users of norgestimate-35 (95% CI 29.4-57.6), and the age-adjusted VTE incidence rate ratio (IRR) for current use of the contraceptive patch vs. norgestimate-35 was 1.1 (95% CI 0.7-1.8). CONCLUSIONS: The risk of nonfatal VTE for the contraceptive patch is similar to the risk for OCs containing 35 microg ethinylestradiol and norgestimate.

Administration, Cutaneous↗

PubMed2005

Idiopathic stuttering priapism treated successfully with low-dose ethinyl estradiol: a single case report.

INTRODUCTION: Chronic priapism represents a challenging therapeutic dilemma. Inadequate or deferred treatment can result in impaired quality of life and permanent erectile dysfunction. The etiology of stuttering priapism is speculated to be initially an ischemic injury that damages the neurologic and/or endothelial-mediated mechanisms that normally regulate detumescence and maintain penile flaccidity. AIM: We report a case of stuttering priapism successfully treated with low-dose ethinyl estradiol. METHODS: A 51-year-old man presented with idiopathic stuttering priapism. Treatment was given in the form of low-dose ethinyl estradiol for six consecutive weeks. RESULTS: Moderate lowering of testosterone level and effective prevention of priapism for at least 6 months with retaining of erectile function. CONCLUSION: The use of low-dose estrogen shows a potential to be an effective and relatively rapid treatment option for some cases of idiopathic stuttering priapism.

Drug Administration Schedule↗

PubMed1986

The relative bioavailability of levonorgestrel and ethinyl estradiol administered as a low-dose combination oral contraceptive.

The relative bioavailability of levonorgestrel (LNG) and ethinyl estradiol (EE) administered concomitantly both as an oral tablet and as a solution was assessed in a randomized two-period crossover study in 24 healthy women. Serum concentrations were monitored for 96 h after each administration. The relative bioavailability (Fr) of LNG in the tablet with respect to the solution was 107%; thus the two formulations were bioequivalent with respect to LNG. The relative bioavailability of EE, however, was significantly lower for the tablet (Fr 83%) compared to the solution. This difference may have been due to either decreased absorption or enhanced presystemic elimination of EE from the tablet formulation.

Adult↗

PubMed1991

Incidence of ovarian cyst formation in women taking ethynodiol diacetate, 1 mg, with ethinyl estradiol, 35 micrograms.

A total of 7,759 women were treated with ethynodiol diacetate, 1 mg, with ethinyl estradiol, 35 micrograms (EDA 1 mg with EE 35 micrograms) in a field study involving 983 obstetrician-gynecologists evaluating the incidence of ovarian cyst formation. Six thousand three hundred eighty-two patients were evaluable; 1,377 could not be evaluated because of failure to meet inclusion criteria or inconsistent or incomplete data collection. Cysts were detected in 80 patients at the time of the final visit. Follow-up questionnaires were received on 61% of patients and confirmed the presence of 12 newly formed ovarian cysts in patients taking EDA 1 mg with EE 35 micrograms. Only three women required an operation for ovarian cysts; two women had functional ovarian cysts (one follicular and one luteal), and one had a neoplastic cyst (cystadenoma). Thus, the incidence of ovarian cyst formation requiring surgical intervention was 0.05% in women taking EDA 1 mg with EE 35 micrograms.

Adult↗

PubMed2004

Urinary 6-sulfatoxymelatonin excretion in hyperandrogenic women: the effect of cyproterone acetate-ethinyl estradiol treatment.

Evidence for a relationship between melatonin and the reproductive hormones in humans is based on observations of abnormal melatonin secretion in clinical disorders of the pituitary-gonadal axis. The aim of this study was to investigate melatonin production in hyperandrogenic women before and during treatment with cyproterone acetate and ethinyl estradiol (Diane 35). Twelve women with polycystic ovary syndrome (PCOS), 10 women with idiopathic hirsutism (IH), and 10 women with late onset adrenal hyperplasia due to 21-hydroxylase deficiency (LOCAH) were studied. Patients were treated with Diane 35 for four months. Fasting blood samples for the determination of luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone and dihydroepiandrosterone sulfate (DHEAS) and 24-hour urine collections for the determination of 6-sulfatoxymelatonin (aMT6s) excretion were obtained from all patients at baseline and after 4 months of treatment. Results were compared with those obtained in 15 control women. At baseline, women with PCOS and LOCAH had significantly higher testosterone and aMT6s values than women with IH and controls. Diane 35 treatment significantly decreased testosterone, LH, FSH and aMT6s values in PCOS and LOCAH patients compared with pretreatment values. These results indicate that hyperandrogenic women with PCOS and LOCAH have increased melatonin production. The decrease in aMT6s excretion together with reduced serum LH, FSH, DHEAS and testosterone values during treatment with cyproterone acetate-ethinyl estradiol, suggest that sex steroids either directly or through the suppression of gonadotropins, modulate melatonin secretion in these patients.

Adrenal Hyperplasia, Congenital↗

PubMed1981

Lipid absorption in unanesthetized, unrestrained rats. Effects of 4-aminopyrazolopyrimidine and ethinyl estradiol.

Emulsified triacylglycerol containing [14C]palmitate was infused intraduodenally in unanesthetized, unrestrained animals treated with 4-aminopyrazolopyrimidine or pharmacologic doses of ethinyl estradiol. 4-Aminopyrazolo-pyrimidine practically eliminated the appearance of radioactivity in plasma but in ethinyl estradiol-treated animals the peak of radioactivity and shape of the plasma curve were similar to control, although lower in amplitude. A delayed appearance of radioactivity was also observed in 48-h- compared to 15-h-fasted controls, suggesting a requirement for induction of lipoprotein production prior to fat absorption.

Adenine↗

PubMed2005

Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2.

BACKGROUND AND OBJECTIVE: Oral contraceptives (OCs) can inhibit drug metabolism, but their effect on various cytochrome P450 (CYP) enzymes and drugs can be different. Our objective was to study the effect of combined OCs, containing ethinyl estradiol (INN, ethinylestradiol) and gestodene, on CYP1A2 activity, as well as their interaction potential with tizanidine. METHODS: In a parallel-group study, 15 healthy women using OCs and 15 healthy women without OCs (control subjects) ingested a single dose of 4 mg tizanidine. Plasma and urine concentrations of tizanidine, as well as several of its metabolites (M-3, M-4, M-5, M-9, and M-10), and pharmacodynamic variables were measured until 24 hours after dosing. As a marker of CYP1A2 activity, an oral caffeine test was performed in both groups. RESULTS: The mean area under the plasma concentration-time curve from time 0 to infinity [AUC0-infinity] of tizanidine was 3.9 times greater (P<.001) and the mean peak plasma tizanidine concentration (Cmax) was 3.0 times higher (P<.001) in the OC users than in the control subjects. In 1 OC user the AUC0-infinity of tizanidine exceeded the mean AUC0-infinity of the control subjects by nearly 20 times. There were no significant differences in the elimination half-life or time to peak concentration in plasma of tizanidine between the groups. Tizanidine/metabolite ratios in plasma (M-3 and M-4) and urine (M-3, M-4, M-5, M-9, and M-10) were 2 to 10 times higher in the users of OCs than in the control subjects. In the OC group the excretion of unchanged tizanidine into urine was, on average, 3.8 times greater (P=.008) than in the control subjects. The plasma caffeine/paraxanthine ratio was 2.8 times higher (P<.001) in the OC users than in the control subjects. The caffeine/paraxanthine ratio correlated significantly with the AUC0-infinity and peak concentration of tizanidine in plasma, with its excretion into urine, and with, for example, the tizanidine/M-3 and tizanidine/M-4 area under the plasma concentration-time curve ratios. Both the systolic and diastolic blood pressures were lowered by tizanidine more in the OC users (-29+/- 10 mm Hg and -21+/- 8 mm Hg, respectively) than in the control subjects (-17+/- 9 mm Hg and -13+/- 5 mm Hg, respectively) (P < .01). CONCLUSIONS: OCs containing ethinyl estradiol and gestodene increase, to a clinically significant extent, the plasma concentrations and effects of tizanidine, probably mainly by inhibiting its CYP1A2-mediated presystemic metabolism. Care should be exercised when tizanidine is prescribed to OC users.

Adolescent↗

PubMed1991

Efficacy and safety of ethynodiol diacetate, 1 mg, with ethinyl estradiol, 35 micrograms, with an emphasis on contraceptive efficacy. A phase IV trial.

A phase IV trial evaluated the efficacy and safety of a monophasic oral contraceptive formulation, ethynodiol diacetate, 1 mg, plus ethinyl estradiol, 35 micrograms (EDA 1 mg with EE 35 micrograms) (Demulen 1/35). Nine hundred eighty-three community-based obstetrician-gynecologists treated a total of 7,759 patients with EDA 1 mg with EE 35 micrograms for one to eight months. Clinical evaluation forms on 6,382 patients were amenable to analysis for safety (including breakthrough bleeding, ovarian cyst formation and complexion changes); 5,412 patients were evaluable for efficacy (prevention of pregnancy), with a total of 21,440 cycles recorded. The study results were interpreted in terms of the impact on clinical management of oral contraceptive users and the methods, strengths and weaknesses of phase IV trials, particularly as they relate to confirmation of the results reported here.

Adolescent↗

PubMedDate not supplied

Systemic and histopathologic changes in Beagle dogs after chronic daily oral administration of synthetic (ethinyl estradiol) or natural (estradiol) estrogens, with special reference to the kidney and thyroid.

ABSTRACT Four groups of 3 male and 3 female sexually mature Beagle dogs were treated daily po with either ethinyl estradiol (EE) or estradiol (E2). A fifth group of 4 males and 4 females acted as a control group. Three groups of dogs were treated with EE: One group was treated at dose levels of 2.0, 1.5, and 1.0 mg/kg for 6 mo; the other 2 groups received either 0.5 mg/kg or 1.0 mg/kg for 1 yr. The fourth group was treated with 5.0 mg/kg E2 for 1 yr. Results obtained for the clinical, hematological, and biochemical parameters and the histopathologic findings of most organs and tissues in EE- and E2-treated dogs were essentially comparable to those documented in the literature for dogs treated with synthetic or natural estrogens. Chronic treatment with EE or E2 induced similar effects, with the exception of mesothelial proliferation of the genital serosa, which was observed in EE-treated dogs only. Additional new estrogen-related findings were observed in the kidneys and thyroid glands of EE- and E2-treated dogs. Increased interstitial fibrous tissue occurred at the corticomedullary junction and in the outer cortex of the kidney. It appeared to originate primarily from the perivascular fibrous tissue of branches of the renal arteries and veins. Extension of this lesion into the renal parenchyma resulted in secondary atrophic changes of tubules and glomeruli. The treatment relationship and specific characteristics of this renal alteration differentiated it from other chronic renal interstitial and vascular diseases. Squamous metaplasia of urogenital tract epithelia, including renal cortical tubule epithelium, occurred as expected in both EE- and E2-treated dogs. Unexpectedly, squamous metaplasia of thyroid follicular epithelium also occurred. It was present in scattered follicles of both EE- and E2-treated dogs. The renal and thyroid changes did not alter clinicopathological function tests for either of these organs. These 2 new findings extend the list of estrogen-related effects in the dog.

Administration, Oral↗

PubMed1992

Triphasic combination of ethinyl estradiol and gestodene. Long-term clinical trial.

A triphasic oral contraceptive containing ethinyl estradiol and gestodene was used by 1933 women for up to 36 cycles in order to evaluate contraceptive efficacy, general tolerance and cycle control. Altogether, 30,763 treatment cycles were recorded. Two pregnancies were seen, both of them classified as user failure. The rates of spotting and breakthrough bleeding fell below the rates of the pre-treatment cycle after the first three months of treatment. Adverse events were mostly minor with breast tension and headaches the most common complaints. After the first three cycles, the incidence of most complaints was the same as or even lower than in the pre-treatment cycle. Blood pressure and body weight remained practically unchanged. The trial preparation provided reliable contraception with good general tolerance and cycle control when taken for up to three years.

Adult↗

PubMed2000

Photoaffinity labeling identification of a specific binding protein for the anabolic steroids stanozolol and danazol: an oligomeric protein regulated by age, pituitary hormones, and ethinyl estradiol.

We have demonstrated previously that both rat and human liver microsomes contain a highly specific binding protein for the anabolic steroids stanozolol (ST) and danazol (DA). In this study we solubilized the male rat liver ST-binding protein (STBP) and investigated the following parameters: 1) pharmacological properties, 2) hydrodynamic properties, 3) peptidic composition, 4) the effects of age and hypophysectomy, and 5) inducibility by 17alpha-ethinyl estradiol. We found that STBP is an integral protein bound to the endoplasmic reticulum. 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS) provided its optimal solubilization without changes in its pharmacological properties, i.e. high specificity for ST and danazol, between natural steroids and ligands of low affinity glucocorticoid-binding sites or of progesterone-binding sites. Hydrodynamic properties of the STBP showed that it has a molecular mass of at least 118 kDa. SDS-PAGE of covalently labeled STBP under nonreducing conditions showed that [3H]ST binds to a 110-kDa protein. The STBP was resolved under reducing conditions into three peptides of 55, 31, and 22 kDa, respectively. STBP increased from immature to adult rats, and it dramatically decreased after hypophysectomy. Unlike the 22-kDa peptide, both the 55- and 31-kDa peptides drastically decreased in both immature and hypophysectomized rats. 17alpha-Ethinyl estradiol administration to immature or hypophysectomized rats induced the 55- and 31-kDa [3H]STBP to a greater extent than the 22-kDa peptide. Thus, STBP appears as an oligomeric protein composed of hormone-regulated peptides. The availability of solubilized STBP and the fact that it can be induced in vivo represent major steps toward the purification and functional significance of this unique steroid-binding protein.

Aging↗

PubMed1997

A new low-dose monophasic combination oral contraceptive (Alesse) with levonorgestrel 100 micrograms and ethinyl estradiol 20 micrograms. North American Levonorgestrel Study Group (NALSG).

The efficacy and safety of a new, low-dose, 21-day combination oral contraceptive containing 100 micrograms of levonorgestrel and 20 micrograms of ethinyl estradiol were evaluated in an open-label, multicenter trial. A total of 1477 subjects were enrolled and had 7870 cycles of exposure as of the data cutoff of this interim report. Of these, 792 subjects had completed six cycles of treatment. A total of five pregnancies occurred during treatment during 7720 efficacy cycles, for a Pearl index of 0.84. To date, 415 (28%) subjects have been withdrawn from the study for any reason, including 131 (9%) due to adverse events. The cumulative life table pregnancy rate was 0.0041 per woman entering the sixth cycle. Breakthrough bleeding alone occurred in 4.3% of the cycles and breakthrough bleeding and spotting occurred together during 11% of the cycles. Of the cycles evaluable, 2.6% were amenorrheic. The most commonly reported adverse events in this trial considered at least possibly drug related were headache (14%) and metrorrhagia (8%). This formulation provides contraceptive efficacy similar to higher-dose oral contraceptives, while maintaining a safety and common OC side effect profile that is consistent with prior years of reported use with levonorgestrel-containing products.

Adolescent↗

PubMed1998

Contraceptive efficacy and acceptability of a monophasic oral contraceptive containing 30 microg ethinyl estradiol and 150 microg desogestrel in Latin-American women.

Contraceptive efficacy, subject acceptability (cycle control, side-effects, acne score and weight gain) and blood pressure of a monophasic oral contraceptive containing 30 microg ethinyl estradiol plus 150 microg desogestrel (Marvelon) were assessed in an open-label 6-cycle multicenter study in Argentina (7 centers) and Venezuela (5 centers). Of the 407 participating women, 389 (95.6%) completed six cycles of treatment, providing data for a total of 2383 cycles. No pregnancies occurred during the course of the study, confirming the high contraceptive reliability of Marvelon. Cycle control was excellent; the duration of withdrawal bleeding decreased during consecutive treatment cycles and the incidence of spotting and breakthrough bleeding was low. The desogestrel/ethinyl estradiol combination was well tolerated and the incidence of minor side-effects, which was already low in the first treatment cycle, in most cases decreased during the subsequent cycles. The preparation was effective in reducing pre-existing acne, whereas it did not induce clinically relevant changes in blood pressure and body weight. Marvelon was shown to provide effective oral contraception, with good tolerance and excellent cycle control in Latin-American women.

Acne Vulgaris↗