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At least 253 records · Page 14Linked to original sources

Factors affecting pituitary gonadotropin function in users of oral contraceptive steroids.

In order to determine whether certain factors influence the direct pituitary suppressive effect of contraceptive steroid, 50 subjects who had used various formulations of oral contraceptive steroids for periods of time ranging from one to nine years were stimulated with 50 microgram of gonadotropin-releasing hormone (GnRH) during the last week of oral contraceptive ingestion. The response of lutinizing hormone (LH) and follicle-stimulating hormone (FSH) was compared to the results obtained in nine control subjects with regard to: (1) age of subject. (2) type of contraceptive formulation used, and (3) length of use. Prestimulation levels of LH and FSH, respectively, were significantly decreased in 37 (74 per cent) and 42 (84 per cent) of the subjects. Following GnRH stimulation, peak responses of serum LH and FSH, respectively, were also significantly lower than those in the control subjects in 40 (80 per cent) and 45 (90 per cent of the subjects. The degree of suppression of pituitary gonadotropins, both before and after GnRH administration was significantly correlated with the type of steroid formulation used, being greatest with a combination of d-norgestrel and ethinyl estradiol. No correlation was found with length of use of oral contraceptives or age of the subjects.

Adult↗

Synthetic progestins: in vitro potency on human endometrium and specific binding to cytosol receptor.

The relative potency of six commonly used synthetic progestins has been evaluated in an organ culture system for human endometrium. The affinities of these progestins for endometrial progesterone receptor were also evaluated after removing the CBG-like protein by spheroidal hydroxylapatite chromatography. All six progestins induced an increase in tissue glycogen during culture at lower concentrations than did progesterone; only one (medroxyprogesterone acetate) had a relative affinity greater than progesterone. The relative potencies and affinities of the synthetic progestins were found to have the same relative order but to differ in relative magnitude.

Chromatography↗

The varying effects of progestins on lipid levels and cardiovascular disease.

A recent study at George Washington University Lipid Research Clinic compared three oral contraceptives containing different progestins and found that increases in total cholesterol, triglycerides, and apoprotein. All were not progestin related. Other effects, however, were apparently dependent on the type of progestin, with the androgenically potent agent dl-norgestrel causing dramatic increases in low-density lipoprotein (LDL)-cholesterol and the ratio of low-density to high-density lipoprotein (HDL) and decreases in HDL, particularly HDL2, and apoprotein Al. Reductions in HDL2 and increases in the LDL/HDL ratio are strongly associated with the development of atherosclerosis. In a study of postmenopausal women receiving hormone replacement therapy, estrogen alone was compared with estrogen plus dl-norgestrel. In contrast to the findings of the previous study, norgestrel lowered LDL and produced less substantial decreases in HDL and HDL2. Thus, although an antiestrogenic effect was evident, it cannot be assumed that the changes associated with progestin-containing oral contraceptives will automatically occur when lower doses of progestin are used in hormone replacement therapy.

Adolescent↗

Effects of desogestrel on carbohydrate metabolism.

Associated with progesterone and the synthetic progestins used in oral contraceptives is a dose-dependent impairment of carbohydrate metabolism. It is well known that in the general population hyperinsulinemia and alterations in glucose metabolism are significant risk factors for the development of cardiovascular disease. Studies that use curve analysis of glucose tolerance tests have demonstrated insulin resistance, rises in plasma insulin, and relative glucose intolerance in women using oral contraceptives. Desogestrel, a new progestin, has been demonstrated to have generally less pronounced effects on these parameters of carbohydrate metabolism.

Animals↗

Studies on dopamine turnover in ovariectomized or hypophysectomized female rats. Effects of 17 beta-estradiol benzoate, ethynodioldiacetate and ovine prolactin.

The effects of 17 beta-estradiol benzoate (EB), ethynodioldiacetate and ovine prolactin on dopamine (DA) turnover have been studied. As an index for a change in turnover, differences in DA depletion following tyrosine hydroxylase inhibition with alpha-methyl-tyrosine methylester were observed. DA was measured by means of mass fragmentographical analysis in the rat median eminence, the olfactory tubercle and the striatum. The actions of ethynodioldiacetate and ovine prolactin on DA turnover in various subregions of the rat median eminence were analysed by quantitative microfluorimetry. Repeated injections of EB to ovariectomized rats resulted in a significant increase of DA turnover in the median eminence. Administration of ethynodioldiacetate to ovariectomized rats almost significantly increased DA turnover in the olfactory tubercle. In the median eminence DA turnover was significantly increased only in the lateral palisade zone. In male hypophysectomized rats ovine prolactin increased DA turnover in both the lateral and the medial palisade zone of the median eminence. The results support the involvement of DA neurons in the control of prolactin and luteinizing hormone secretion. It is suggested that the tubero-infundibular DA neurons are involved in mediating the central inhibitory feedback actions of prolactin and gonadal steroids on prolactin and LH secretion, respectively.

Animals↗

Application of 125I-labelled second antibody to the solid-phase immunoassay of norethisterone in plasma.

The concept of employing 125I-labelled second antibodies for making quantitative measurements of small molecules in biological fluids was evaluated. In a model system 125I-labelled second antibodies were used to monitor the binding of purified norethisterone antibodies to albumin-norethisterone complexes immobilised upon plastic tube surfaces. Conditions were established to provide an assay response similar to other immunoassays for norethisterone using the same primary antiserum. The specificity and accuracy of the assay were comparable to the conventional solid and liquid-phase assays, but precision tended to be less at low levels of norethisterone (less than 200 pg/tube). A reduction in assay variance may be achieved through more efficient tube-washing procedures.

Contraceptives, Oral, Combined↗

Steroid absorption and enterohepatic recycling.

A short review on steroid absorption and enterohepatic recycling in man with special emphasis on contraceptive and related steroids is presented. Some new experimental data on the intestinal metabolism of steroids is described and includes further observations on the effect of antimicrobial agents on steroid hormone metabolism. Evidence is presented that plasma levels of steroids may be influenced if the intestinal microflora is altered. Some formation of biologically active steroids, like estradiol, may occur in the intestinal tract and this may have both biological and pathological consequences and may be influenced by such factors as diet and sex. It is concluded that our knowledge of the intestinal and especially, the mucosal metabolism of steroids is scanty and further studies are needed to clarify the role of the intestine and enterohepatic circulation in determining the bioavailability of natural and synthetic steroids.

Absorption↗