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At least 163 records · Page 9Linked to original sources
PubMed1986

Use of oral contraceptives by women with epilepsy.

Oral contraceptives have not been associated with exacerbation of epilepsy despite warnings in package inserts. No clinical study has provided scientific evidence of worsening of seizures in epileptic women who use oral contraceptives, and improvement in seizure control has occurred in some cases. The main concern about use of oral contraceptives in this population is their effectiveness in preventing conception. Failure rates are higher in groups of women taking enzyme-inducing antiepileptic drugs. The degree of increased metabolism of estrogen and progestin components is highly variable and unpredictable among individuals. Use of higher doses increases protection against conception but also increases the risk of side effects, particularly in patients in whom no enzyme induction occurs. The strength of hormones in the pill should be selected individually when initiating use. Some women may require higher doses for full contraceptive effect.

Animals↗
PubMedDate not supplied

[Sex hormone regulation of progesterone and estradiol receptors in the cytosol of human endometrium in normal and pathologic pregnancy].

Hormonal control of progesterone and estradiol receptors was studied in the cytozol of short-lived culture of human endometrium in normal and undeveloping pregnancy. Endometrium was cultivated in the presence of estradiol or progesterone for 16 hours. In cultivation of normal endometrium with estradiol the content of estradiol receptors increased 4-fold in comparison with unstimulated tissue, and of progesteron receptors--3-fold. In cultivation of normal endometrium with progesterone the content of estradiol receptors rose 4--5-fold, and of progesterone receptors--3-fold. In cultivation of pathological endometrium with estradiol or progesterone the number of estradiol receptors was only doubled, and of progesterone receptors--increased only 1 1/2 times, this pointing to a diminished sensitivity of pathological endometrium to the regulating action of sex hormones.

Cells, Cultured↗
PubMedDate not supplied

[Effects of progestogens on the metabolism of lipids and carbohydrates. Practical consequences (author's transl)].

Estrogens which are one of the components of contraceptive less than pills greater than are incriminated in many cardiovascular accidents. These occur as a result of metabolic disorders (involving lipids and carbohydrates), of modifications in coagulation factors, etc. The possible influence of progestogens was ignored for a long time. The widespread use of these compounds, prescribed for contraception as well as during hormonal replacement therapy for absolute or relative luteinic insufficiency, makes careful monitoring of lipid and carbohydrate metabolism imperative. This position is strengthened by a preliminary review of the literature which leads to several conclusions concerning lipid and carbohydrate metabolism.

Carbohydrate Metabolism↗
PubMed1981

[The benefit of the classification of oral contraceptives. Studies of 525 women taking oral contraceptives (author's transl)].

The multiplicity of oral contraceptives suggests a classification for clinical routine. From the dosage of estrogens and gestagens in oral contraceptives, aberration indices were calculated from consideration of proliferation and transformation aspects. According to these a classification of oral contraceptives into 3 "estrogen" groups and 4 "gestagen" groups was made. Such a classification was made in 525 women taking oral contraceptives which took into consideration the following parameters: age, length of time during which oral contraceptives had been taken, subjective side-effects, sexual medical and psychometric aspects.

Adult↗
PubMed1980

[Effects of oral contraceptives on the vascular wall (author's transl)].

The vascular complications of oral contraceptive treatment affect both arteries and veins, and vessels of all calibres in the systemic, pulmonary and portal circulations may be involved. In most cases thrombophlebitis develops under the combined influence of drug-induced blood changes and alterations in the vascular wall. Thickening of the connective and muscular fibers of the intima is commonly found, either isolated or associated with proliferation of the endothelium and/or thickening of the tunica media. These lesions are unrelated to those of atherosclerosis. Systematic investigations being impossible, the true incidence and extent of vascular wall alterations are necessarily under-estimated. The physiopathology of these non-specific lesions is unknown, but synthetic oestrogens seem to be mainly responsible for their occurence. Oestrogens might act on the vascular wall either directly or through changes in blood composition. Such lesions unquestionably have clinical repercussions.

Blood Vessels↗
PubMed1982

Estrogen receptors in ovarian epithelial carcinoma.

Specimens from 53% (16 of 30) of patients with untreated ovarian epithelial cancers between October 1976 and February 1979 had estrogen binding levels greater than 30 fmoles/mg of cytosol protein (receptor rich). The likelihood of a specimen being receptor rich appeared to be independent of patient age, histologic grade of tumor, clinical stage, and amount of residual tumor left after surgery. For 20 patients with previously untreated advanced disease a life-table analysis showed no significant difference when receptor-rich and -poor groups were compared in terms of either survival or time to first progression of disease. Analysis of more recent specimens (predominantly obtained after February 1979) indicates high-affinity binding of the estrogen consistent with receptor; occasional substantial heterogeneity in estrogen binding results between different sites of tumor involvement; and progestin-specific binding in some specimens. In an analogy to breast cancer, patients whose tumors are cytosol estrogen receptor rich might theoretically be responsive to the administration of antiestrogens.

Aged↗
PubMed1980

Incidence of hyperprolactinemia during oral contraceptive therapy.

A study was undertaken to determine the incidence of increased serum levels of human prolactin (hPRL) in women during oral contraceptive therapy, and to correlate this with both the dose of oral contraceptive medication and the duration of its use. The 123 patients in this study were divided into 3 groups according to the dosage of estrogenic component of the combined oral contraceptives. Thirty percent of these women had hyperprolactinemia of varying degree. Neither the dosage of steroids within our range nor the duration of therapy correlated with the presence or degree of hyperprolactinemia. The actions of estrogen-progestin compounds on hPRL are discussed.

Adolescent↗
PubMed1994

[Pharmacokinetics of RU 486 and its active metabolites in humans].

The pharmacokinetics of RU 486 and its active metabolites were studied in 31 women who received a single oral dose of 200 mg (n = 9), 400 mg (n = 10) or 600 mg (n = 12) of RU 486 for termination of an early unwanted pregnancy. The serum levels were measured within 48 hours after the intake by radioligand binding assay using human myometrial cytosolic progesterone receptor as binding protein. The assay is based on the competitive replacement of 3H-ORG-2058 by the active molecular fraction of RU 486 present in the serum. The results were expressed as RU 486 equivalent. It was found that pharmacokinetics of the RU 486 equivalent followed two-compartment open model. The pharmacokinetic parameters were calculated by MEDUSA computer programme. Rapid absorption and distribution was followed by relatively slow elimination. The elimination half-life ranged between 80-90 hours. No significant difference was found between the parameters of the absorption distribution and elimination processes of three different doses. Thus, the RU 486 equivalent followed first-order kinetic. Peak serum concentrations were reached within 1-2 hours after the ingestion of the drug. Significant differences were found between 200 and 600 mg doses in the peak plasma values (p < 0.05) and in the areas under the curve (p < 0.01). However, these differences were not directly proportional to the increase of the dose.

Female↗
PubMed1977

Characterization and assay of progesterone receptor in human mammary carcinoma.

[3H]Pregn-4-ene-3,20-dione ([3H]progesterone)-receptor complexes from human mammary carcinoma were found to be stabilized in the presence of glycerol. The dissociation rate constant was lowered and the equilibrium dissociation constant was decreased (KD=3 nM in the absence of glycerol and 1.1 nM in the presence of 30% glycerol), whereas no clear-cut effect on the association rate was observed and no change occurred in the concentration of binding sites. Cortisol was found to compete with [3H]progesterone only at concentrations higher than 1 muM. This made it possible to distinguish [3H]progesterone binding to the receptor from binding to corticosteroid-binding globulin. Synthetic progestins [6-chloro-17-acetoxypregna-4,6-diene-3,20-dione (chlromadinone acetate), 17alpha-ethinyl, 17-hydroxyestr-4-en-3-one (norethisterone), and 17,21-dimethyl-19-norpregna-4,9-diene-3,20-dione (R5020)] were found to have a high affinity for the receptor, whereas 5alpha-pregnane-3,20-dione had an affinity about one-half that of progesterone itself 5beta-Pregnane-3,20-dione, 17alpha-hydroxypregn-4-ene-3,20-dione (estradiol), 11beta,21-dihydroxy-pregn-4-ene-3,20-dione (corticosterone), estra-1,3,5(10)-triene-3,17beta-diol, and 17beta-hydroxyandrost-4-en-3-one (testosterone) were weak inhibitors of [3H]progesterone binding. Sedimentation on glycerol gradients showed different patterns in different tumors; i.e., [3H]progesterone specific binding having the characteristics of receptor was found either in the 8 S region, in the 4.5 S region, or in both. Activated progesterone-receptor complex from human mammary carcinoma cytosol was shown to bind to human DNA. An assay of the receptor based on these binding properties is described. This assay measures the total concentration of cytosol receptor since it makes possible the exchange of endogenous hormone for excess added [3H]progesterone. Of 55 biopsies examined by this method, 35 (64%) had a concentration of progesterone receptor-binding sites higher than 10 fmoles/mg protein. There was a positive correlation between the amounts of estrogen and progesterone receptors.

20-alpha-Dihydroprogesterone↗
PubMed1997

Binding activity of 5alpha-reduced gestagens to the progestin receptor from African elephant (Loxodonta africana).

Recent findings in the African elephant (Loxodonta africana) indicate that the major progestins contained within and biosynthesized by corpora lutea are 5alpha-reduced metabolites and that progesterone is quantitatively of minor importance. The specific gestagenic action within the reproductive tract of elephants was determined by measurement of relative binding affinity of the respective progestins to the gestagen receptor extracted from elephant endometrium. The cytosol was incubated with 40 nmol/liter [3H]ORG-2058 and increasing concentrations of the tested progestin. Progesterone (P4), 5alpha-pregnane-3,20-dione (DHP), and 5alpha-pregnane-3alpha-ol-20-one (5alpha-P-3OH) were used. The competition for binding sites on the progestin receptor was shown by decreasing counts measured after extraction with scintillation fluid. The progestin concentration which induced a 50% reduction of measured counts was estimated (C50) and relative binding affinity of progesterone to other progestins was calculated (RBA = C50progestin/C50p4). The relative binding affinity of DHP to P4 at the gestagen receptor of elephant endometrium was equivalent. The other 5alpha-reduced progestin (5alpha-P-3OH) showed no competition to the [3H]ORG-2058 receptor binding. We conclude that the biological significance of P4 and DHP at the receptor level is very similar. The higher quantitative levels of DHP in corpus luteum and serum support the hypothesis that this progestin is the major gestagen in the elephants, whereas 5alpha-P-3OH is an inactive metabolite.

5-alpha-Dihydroprogesterone↗
PubMed1989

Progestin inhibition of estrogen-dependent proliferation in ZR-75-1 human breast cancer cells: antagonism by insulin.

The effect of R5020 [17,21-dimethyl-19-nor-4,9-pregnadiene-3,20-dione], a synthetic progestin, was studied in the hormone-responsive ZR-75-1 human breast cancer cell line. Following a 12-day incubation with increasing concentrations of R5020, the mitogenic effect of 17 beta-estradiol (E2, 1nM) was partially (60-80%) antagonized by the progestin, with a half-maximal effective concentration measured at about 30 pM. This effect of R5020 was completely reversed by the addition of physiological concentrations of bovine insulin, as well as by the potent antiprogestin RU486 [17 beta-hydroxy-11 beta-(4-dimethylaminophenyl)-17 alpha-(1-propynyl)-4, 9-estradien-3-one], but not by the antiandrogen hydroxyflutamide (alpha, alpha, alpha-trifluoro-2-methyl-4'-nitro-m-lactotoluidide). Moreover, the effect of R5020 required the presence of estrogens, thus further indicating a progesterone receptor (PgR)-mediated effect. Low (greater than 100 nM) concentrations of R5020 increased the specific binding of [125I]-insulin up to 2- to 2.5-fold in intact ZR-75-1 cells, an effect which was reversed by RU486. The effect was rapid, being nearly maximal after 24h of incubation with R5020. The PgR-mediated effect of R5020 on cell proliferation was abolished by the addition of a pure steroidal antiestrogen. The present results suggest a physiological role for progestins in increasing the responsiveness to insulin, which could, in turn, reverse the antiproliferative effect of progestins on estrogen action and thus decrease the efficacy of progestins in the treatment of breast cancer.

Animals↗
PubMed1976

Potencies of oral contraceptives.

Oral contraceptives are combinations of estrogens and progestogens or, in the case of the mini-pills, progestogens alone. With specific test procedures in laboratory animals or human subjects, it is possible to assign potency evaluations to the components relative to the progestational, estrogenic, or antiestrogenic activities of the progestogen or to the estrogenic potencies of the estrogenic component. It might even be possible to quantify the synergistic effects of the estrogen on the progestational agent. Unfortunately, however, it is impossible now to amalgamate such assay results into single estimates of the potencies of the combinations (either the combination products per se or the combination tablets of sequential products). For example, an over-all estrogenic potency of a combination preparation would involve the integration of contributions form the estrogen itself plus the estrogenic products of metabolism of the progestogen minus the antagonistic effect of the progestational agent, if any. These factors cannot now be quantified independently, much less merged into a single figure of clinical significance. Further, even if it were possible to produce such an estimate, it is unlikely that the evaluation would be meaningful in relation to any putative side effect or adverse reaction, i.e., the alleged thrombogenic effects of oral contraceptives cannot currently be related directly to any measure of potency that will allow prediction of these clinical conditions from laboratory models. Any evaluation of the potential of a given contraceptive to produce a specific side effect will depend upon data generated with specific regard to that adverse reaction and the individual product in question.

Contraceptives, Oral↗
PubMed1982

The effect of oral contraceptives on antiaggregatory prostacyclin and proaggregatory thromboxane A2 in humans.

The effect of different types of oral contraceptives on the productions of antiaggregatory prostacyclin (PGI2) and proaggregatory thromboxane A2 (TxA2) was studied by measuring the stable metabolites of these prostanoids, that is, 6-ketoprostaglandin F1 alpha (6-keto-PGF1 alpha) and thromboxane B2 (TxB2), respectively, from plasma. In addition, the capacity of the platelets to produce TxB2 during spontaneous clotting was studied by measuring the TxB2 levels from the serum incubated at +37 degrees C for 60 minutes. The material consisted of 48 women who had used estrogen-containing oral contraceptives for 2.0 +/- 1.9 years (mean +/- SD), 24 women using progestogen-only pills for 3.7 +/- 2.0 years, and 42 women of the same age using no oral contraceptives or intrauterine contraceptive device. The plasma concentrations of 6-keto-PGF1 alpha in women with combined oral contraceptives (65.5 +/- 16.1 pg/ml, mean +/- SD) was lower (p less than 0.01) than that in the control subjects (77.4 +/- 26.4 pg/ml), whereas the use of combined oral contraceptives was associated with no changes in TxB2 levels in plasma or serum, in women with progestogen-only oral contraceptives, the plasma levels of 6-keto-PGF1 alpha and TxB2 were normal, but the capacity of the platelets to release TxB2 during spontaneous clotting was decreased (113.6 +/- 77.6 ng/ml versus 179.9 +/- 81.9 ng/ml, p less than 0.05). In a prospective trial on 11 women, who started using 30 microgram of ethinyl estradiol and 150 microgram of levonorgestrel, no changes in PGI2 or TxA2 were seen during the first 3 months of usage. The decrease in antiaggregatory PGI2 during the prolonged use of estrogen-containing oral contraceptives may be associated with the increased risk of thromboembolism.

6-Ketoprostaglandin F1 alpha↗
PubMed1993

Selectivity information on desogestrel.

Improvement in oral contraceptive formulations was originally achieved through dose reduction of the estrogen and progestogen components. Recently, further improvement was achieved by increasing the selectivity of contraceptive progestins. The ratio between the affinity for the progesterone receptor and the affinity for the androgen receptor is an indicator of progesterone (or androgen) selectivity of a progestin. This ratio (selectivity index) reflects the relative amount of androgenic or progestational effect at a given dose. Relative selectivity can be characterized with in vitro receptor-binding studies and animal pharmacologic experiments. In comparison with levonorgestrel, desogestrel displays markedly lower androgenicity and slightly increased relative progestational activity. In receptor-binding experiments and animal pharmacologic studies, 3-keto-desogestrel, the active metabolite of desogestrel, shows the highest selectivity index. The favorable effect of desogestrel-containing oral contraceptives on lipoprotein metabolism and preexisting androgen-dependent skin disorders and the absence of adverse effects on blood pressure and body weight are attributed to the increased progestin selectivity of desogestrel.

Animals↗