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Results for “Ethinyl Estradiol”

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At least 19 recordsLinked to original sources

PubMed1978

Serum alkaline phosphatase elevation in female rats treated with ethinyl estradiol.

Ethinyl estradiol treatment to female rats resulted in increased levels of serum alkaline phosphatase, but was not associated with any other manifestation of toxicity such as increased serum transaminases or toxic lesions. Elevated serum alkaline phosphatase seen in rats treated with chloroform was associated with frank hepatotoxicity. Induction of hepatic drug metabolising enzymes in rats by phenobarbitone treatment did not result in raised serum alkaline phosphatase levels. Estradiol benzoate treatment to rats also did not increase serum alkaline phosphatase levels. Ethinyl estradiol also resulted in increased alkaline phosphatase content in the liver, intestine and bone. The raised intestinal alkaline phosphatase content of rats treated with phenobarbitone or estradiol benzoate was not associated with an increase in the serum levels. There was histochemical evidence of induction of canalicular alkaline phosphatase in the liver in Ethinyl Estradiol treatment. The study of the electrophoretic separation of serum alkaline phosphatase of ethinyl estradiol treated rats revealed the presence of a new fast moving fraction, similar to those seen in bile duct ligated rats. It is concluded that the serum alkaline phosphatase increase during ethinyl estradiol treatment at least in part is from the liver, due to new synthesis.

Alkaline Phosphatase↗

PubMed1977

Effect of prenatal treatment with ethinyl estradiol on the mouse uterus and ovary.

Oral ethinyl estradiol (0.01 or 0.02 mg. per kilogram) administered prenatally to ICR-JCL strain mice before the development of the uterine and ovarian blastemata induced cystic glandular hyperplasia with epidermization in the endometrium and excessive formation of degenerating follicles in the ovaries at 10 to 14 weeks of age. To the evidence for the production by estrogen of malignant uterine neoplasms in rodents and the clinical data showing that cystic glandular hyperplasia develops after prolonged estrogen administration in postmenopausal women and adenocarcinoma in premenopausal or menopausal women using oral contraceptives including ethinyl estradiol, we add the present results which suggest that ethinyl estradiol administered transplacentally can cause malignant transformation of the uterine endometrium in mice.

Animals↗

PubMed1978

Ethinyl estradiol in peripheral plasma after oral administration of 30 microgram and 50 microgram to women.

Plasma levels of ethinyl estradiol were measured by radioimmunoassay in five women after oral administration of 30 microgram and of 50 microgram of ethinyl estradiol. Peak levels of ethinyl estradiol were mostly observed within two hours after the tablet intake. The peak concentrations found were 50--90 pg and 95--135 pg for the two doses administered. Twenty-four hours after the administration of the tablets, the plasma concentration of ethinyl estradiol did not exceed the plasma blank values (25 pg/ml) in most women.

Administration, Oral↗

PubMed1979

Plasma lipids and high density lipoproteins during oral contraception with different combinations of ethinyl estradiol and levonorgestrel.

Seventy-five menstruating women seeking contraceptive advice were randomly allocated to treatment with combined oral contraceptives containing either ethinyl estradiol 50 micrograms + levonorgestrel 250 micrograms (50/250), ethinyl estradiol 30 micrograms + levonorgestrel 150 micrograms (30/150) or ethinyl estradiol 50 micrograms + levonorgestrel 125 micrograms (50/125). The concentrations of cholesterol, triglycerides, phospholipids, high density lipoprotein (HDL)-cholesterol and HDL-phospholipids were determined after one, three and six months and compared to the mean of two determinations of the same parameters before medication. Triglycerides increased by 18--42 per cent after 1--6 months of treatment with 50/125. The HDL-cholesterol and HDL-phospholipids were reduced by 10 per cent during 50/250 treatment. No other parameters showed any consistent alteration in any of the treatment groups. Raised triglyceride concentration and/or decreased HDL concentration increases the risk for cardiovascular disease. It is therefore suggested that in order not to alter the HDL concentration a combined oral contraceptive agent should not contain more gestagen-androgen than corresponding to 125--150 micrograms of levonorgestrel. To avoid a rise of the triglyceride level the weight relation between levonorgestrel and ethinyl estradiol should be about 5:1.

Adult↗

PubMed1977

Effects of ethinyl estradiol on hepatic microsomal proteins and the turnover of cytochrome P-450.

The effect of ethinyl estradiol, a steroid commonly used in birth control pills and possibly associated with impaired drug metabolism in humans, on the activity of and turnover of components of the hepatic microsomal mixed-function oxidase system was studied in male rats. After 5 days of ethinyl estradiol, 5 mg/kg/day, there was a significant decrease in the activity of ethylmorphine-N-demethylase and in cytochrome P-450, cytochrome b2, and NADPH cytochrome c reductase. Cytochrome P-450 apoproteins were identified within an SDS-polyacrylamide gel system, and the rate of turnover of cytochrome P-450 apoproteins was studied by double-isotope labeling techniques. After 5 days of ethinyl estradiol administration, the rate of degradation of cytochrome P-450 apoprotein was reduced (half-life of 50 hr compared to 24 hr in control), and their relative rate of synthesis was likewise reduced, indicating that a new steady state of protein turnover associated with reduced synthesis rate had been reached. This was confirmed by studies of the effect of ethinyl estradiol on the level of microsomal cytochrome P-450 over a 10-day period.

Animals↗

PubMed1979

Effects of three different combinations of ethinyl estradiol and levonorgestrel on plasma lipids and high density lipoproteins.

Seventy-five menstruating women seeking contraceptive advice were randomly allocated to treatment with combined oral contraceptives containing either ethinyl estradiol 30 micrograms + levonorgestrel 150 micrograms (30/150), ethinyl estradiol 50 micrograms + levonorgestrel 125 micrograms (50/125) or ethinyl estradiol 50 micrograms + levonorgestrel 250 micrograms (50/250). The concentrations of cholesterol, phospholipids, high density lipoprotein (HDL)-cholesterol, HDL-phospholipids and triglycerides were determined prior to treatment and after one, three and six months of medication. Triglycerides increased by 18--42 per cent after one to six months of treatment with 50/125. The HDL-cholesterol and HDL-phospholipids were reduced by 10 per cent during 50/250 medication. No other parameters showed any consistent alteration in any of the treatment groups. Raised triglyceride concentration and/or decreased HDL concentration may increase the risk for cardiovascular disease. It is therefore suggested that in order not to alter the HDL concentration a combined oral contraceptive agent should probably not contain more 19-nortestosterone type of progestogen than corresponding to 125--150 micrograms of levonorgestrel. To avoid a rise of the triglyceride level the weight relation between levonorgestrel and ethinyl estradiol should be about 5:1.

Cholesterol↗

PubMed1977

Responsiveness to various dipsogenic stimuli in rats treated chronically with norethynodrel, ethinyl estradiol and both combined.

Administration of the estrogen, ethinyl estradiol (36 microng/kg/day), alone, and in combination with the progestogen, norethynodrel (165 microng/kg/day), significantly attenuated the dipsogenic response characteristically induced by acute s.c. administration of the beta adrenergic agonist, dl-iosproterenol (50 microng/kg). Attenuation was apparent within 1 week of steroid treatment, and remained during the 4 weeks of testing. After 16 weeks of steroid treatment, the drinking response to acute i.p. administration of renin (2 and 4 Goldblatt units/rat) was tested. The groups receiving ethinyl estradiol alone, and in combination with norethynodrel, but not norethynodrel alone, showed a reduced water intake compared with untreated controls. Drinking induced by administration of hypertonic saline (1% of body weight of 1 M NaCl solution, i.p.) was also reduced in rats treated with the estrogenic, but not the progestational, agent. However, estrogen treatment did not affect drinking after a 24-hour period of dehydration. Although the reduced dipsogenic response to isoproterenol observed in estrogen-treated rats may reflect a reduced renin secretion, drinking could not be induced in these animals by administration of renin. In addition, the reduced dipsogenic response to hypertonic NaCl loading suggests that estrogens may inhibit thirst mechanisms centrally. Dehydration, which combines hypovolemic and osmotic thirst situmul was, however, sufficient to overcome the reduced dipsogenic responsiveness of estrogen-treated rats.

Animals↗

PubMed1978

Determination of ethinyl estradiol in human urine by radiochemical GLC.

A radiochemical GLC analysis was developed for 3H-labeled ethinyl estradiol in human urine. The technique was applied to the unconjugated and aglycone fractions of urine collected from women who were dosed orally with: (a) single capsules containing 2.0 mg of 3H-quinestrol (900 muCi) and 2.5 mg of unlabeled quingestanol acetate dissolved in sesame oil and (b) single tablets containing 100 microgram of 3H-quinestrol (86 muCi). Unconjugated ethinyl estradiol in Day 1 urine collections represented means of 0.02% of the high quinestrol dose and 0.12% of the low dose. Ethinyl estradiol glucuronide in the same collections represented means of 0.55% of the high drug dose and 1.35% of the low dose. The method could detect 1-ng quantities of 3H-ethinyl estradiol and 3H-quinestrol.

Adult↗

PubMed1978

Ethinyl estradiol administration and plasma steroid concentrations in ovariectomized women.

The effect of ethinyl estradiol treatment on the plasma levels of cortisol, corticosterone, deoxycorticosterone, progesterone, testosterone, dehydroepiandrosterone sulfate, delta4-androstenedione, and estrone was studied in eight women. All the subjects had undergone ovariectomy and hysterectomy at least one year prior to this study. The systemic concentration of cortisol and the binding of cortisol were significantly increased, paralleling the increased transcortin concentration due to ethinyl estradiol treatment. Corticosterone concentration was also significantly increased after three days of estrogen administration and this level continued to be higher than normal as long as patients were treated with estrogens, but there was no change in the plasma concentration of deoxycorticosterone. The plasma levels of progesterone testosterone, dehydroepiandrosterone sulfate, delat4-androstenedione and estrone or the ratio of estrone to delta4-androstenedione did not change with ethinyl estradiol treatment. These observations suggest that the administered estrogen increased the transcortin concentration and had only a limited effect on adrenocortical steroidogenesis.

Adult↗

PubMed1975

Rapid, sensitive colorimetric method for determination of ethinyl estradiol.

A colorimetric procedure, based on the formation of an azo dye by condensation of diazotized 5-chloro-2,4-dinitroaniline with ethinyl estradiol, was developed. An alkaline solution of ethinyl estradiol is reacted with the reagent, and the resulting color is measured at 450 nm. Absorbance versus concentration is linear up to 10 mug/ml; the lower limit of detection is 1 mug/ml under the conditions studied. Replicate analysis showed good agreement, and an average recovery of 99.6 +/- 0.3% was obtained for analyses of synthetic mixtures. Vitamins and minerals likely to be present along with ethinyl estradiol in certain geriatric formulations, as well as ordinary tablet excipients and coating materials, do not interfere with the precision of the method or development of the color. The method is applicable to progestin-estrogen preparations. Assay results on various single-component as well as contraceptive commercial samples are reported.

Aniline Compounds↗

PubMed1979

Ovulation inhibition with a combined oral contraceptive containing 20 micrograms ethinyl estradiol and 250 micrograms levonorgestrel. Serum levels of the active ingredients and FSH, LH, estradiol 17-beta and progesterone.

In order to investigate the possible ovulation inhibitory effect of a new oral contraceptive containing a combination of 20 micrograms ethinyl estradiol and 250 micrograms levonorgestrel peripheral serum from five healthy women between 17 and 24 years were analysed for FSH, LH, estradiol 17-beta and progesterone. The measurements were carried out during a control cycle before the treatment, during two treatment cycles and during a subsequent control cycle. In addition, serum levels of ethinyl estradiol and norgestrel were determined during the treatment periods. Radioimmunological methods were utilized for all the measurements. In all five women studied there was a complete inhibition of ovulation during treatment as indicated by a lack of mid-cycle LH peaks and by suppression of normal luteal phase levels of progesterone. Four out of the five women showed no biphasic estradiol pattern. During treatment the serum levels of levonorgestrel varied between 1 and 10 nmol/l while the levels of ethinyl estradiol usually were below the limit of detection for the method used (below 85 pmol/l). Post-treatment control cycles revealed a re-establishment of the ovulatory pattern in four of the five subjects.

Adolescent↗

PubMed1979

Optimum dosage of an oral contraceptive. A report from the study of seven combinations of norgestimate and ethinyl estradiol.

A statistically designed study was carried out to determine an optimum combination of norgestimate and ethinyl estradiol as an oral contraceptive, based on efficacy, safety, and side-effect patterns. A total of 1,991 patients were studied for more than two years while they were receiving various dosage combinations of these steroids. There were seven dosage combinations studied as part of a statistically orthogonal experimental design, augmented by three combinations near the center. The data arising from these studies were used to fit approximate functions relating the amount of norgestimate and ethinyl estradiol to the rate of spotting and breakthrough bleeding, gastrointestinal disturbance, and pregnancies. These functions, in turn, helped to identify an optimum dosage (0.125 mg. of norgestimate plus 0.035 mg. of ethinyl estradiol) in the entire range of combinations studied.

Adolescent↗

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↗

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↗

PubMed1978

Disposition of norgestimate in the presence and absence of ethinyl estradiol after oral administration to humans.

The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4 muCi, 0.50 mg) or in combination (73.5 muCi, 0.49 mg) with 3H-ethinyl estradiol (103 muCi, 0.14 mg) in polyethylene glycol 400. Peak levels of radioactivity due to carbon-14 and tritium in plasma occurred within 2 hr after drug administration, followed by distribution and elimination phases. The mean apparent elimination half-life and mean cumulative elimination of radioactivity in the urine and feces following 14C-norgestimate administration were not significantly different than those following administration of the combination dose. Approximately 50% of the administered radioactivity due to carbon-14 was excreted in the urine following administration of 14C-norgestimate both in the presence and absence of coadministered 3H-ethinyl estradiol.

Administration, Oral↗

PubMed1975

Mutual modification of glucose-stimulated serum insulin responses in female rhesus monkeys by ethinyl estradiol and nortestosterone derivatives.

Changes in iv glucose tolerance (IVGTT) and serum insulin responses to glucose infusion have been measured in intact female rhesus monkeys treated per os with norethindrone or medroxyprogesterone acetate (500 mug/day) both alone and in combination with mestranol or ethinyl estradiol (10 mug/day) orally for 3 weeks. When administered as the sole contraceptive steroid, neither norethindrone, medroxyprogesterone acetate, mestranol, or ethinyl estradiol produced consistent changes in fasting serum insulin or glucose concentration, mean intravenous serum glucose disappearance rates (K) or mean integrated serum insulin response to glucose (sigmal40). By contrast, concurrent administration of norethindrone with mestranol or ethinyl estradiol resulted in a significant increase in the fasting serum insulin concentration and the mean sigmal40. An increase in the mean K was also observed after norethindrone + mestranol. These results show that synthetic estrogens have the ability to potentiate the metabolic effects of norethindrone. However, the improvement in glucose tolerance produced in rhesus monkeys by concurrent mestranol + norethindrone treatment was marginal because of wide variation in glucose assimilation rates uncer control conditions. Thus, the IVGTT in the rhesus monkey appears to have limited use as a model for studying glucose homeostasis in man.

Administration, Oral↗

PubMed1978

Double-blind crossover clinical pharmacology study comparing moxestrol (R 2858) and ethinyl estradiol in postmenopausal women.

The potency of 5 migrogram moxestrol (R 2858). 11beta-methoxy-17alpha-ethinyl-estra-1,3,5-[10]-triene-3,17-diol, administered orally, was compared to that of 25 microgram ethinyl estradiol in a double-blind crossover clinical pharmacology study of six postmenopausal women. At these doses, both compounds increased the eosinophilic index and decreased serum LH and FSH levels. A marked effect on circulating prolactin was observed only during ethinyl estradiol treatment.

Aged↗

PubMed1978

Treatment of acne with cyproterone acetate and ethinyl estradiol.

Tablets containing 2 mg cyproterone acetate and 0.05 mg ethinyl estradiol in a calendar package of 21 days were used as an oral contraceptive to treat acne. The series comprised 20 patients. The women were 18--43 years of age, and all had acne which had previously been resistant to therapy. The treatment was continued for 6 months. Serum testosterone, 17-OHCS, 17-KS, serum ALAT and gamma-GT were recorded prior to the treatment at 3 and 6 months. Ten patients responded well to the treatment, 5 responded moderately well, 3 experienced no change, and 2 became worse. The serum testosterone level fell during the therapy and the ALAT level rose, though only one pathological ALAT value was recorded.

17-Hydroxycorticosteroids↗