Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “PROGESTATIONAL HORMONES”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 649 records · Page 36Linked to original sources

Estrogen replacement therapy II: a prospective study in the relationship to carcinoma and cardiovascular and metabolic problems.

A 10-year double-blind prospective study was undertaken to evaluate the effects of estrogen replacement therapy (ERT). The sample population consisted of 84 pairs of randomly chosen postmenopausal in-patients, matched for age and diagnosis. The treatment group received high-dose conjugated estrogens, cyclically with progesterone. The controls recieved placebos. Results revealed no statistically significant difference in that incidence of thrombophlebitis, myocardial infarction (MI), or uterine cancer. There was a lower incidence of breast cancer in the treated group. Estrogen-treated patients showed a higher incidence of cholelithiasis. Those in the treated group who began the study with elevated beta/alpha lipoprotein ratios showed a reduction in that ratio over the course of the study, while the controls either maintained or increased their ratios. The low number of cases precludes drawing any real significance from the data on diseases of low frequency. The study excludes only a high incidence of complications from estrogens.

Adult↗

Inhibition of 3-beta-hydroxy steroid dehydrogenase activity in first trimester human pregnancy with trilostane and WIN 32729.

The effects of equivalent doses of two inhibitors of the 3-beta-hydroxy steroid dehydrogenase enzyme system--WIN 24540 (trilostane) and WIN 32729--on the secretion of progesterone in early human pregnancy are described. Patients and controls less than 12 weeks pregnant were given a single dose of either drug and the resultant hormonal changes monitored for 7 1/2 h. A consistent fall in plasma progesterone concentrations occurred at all doses and, at the highest dose, they fell to less than 50% of pre-treatment levels. However, whilst with trilostane the associated increase in plasma concentrations of pregnenolone was always accompanied by a rise in plasma DHA concentrations, with WIN 32729 there appeared to be no adrenal effect at the lower dosage levels. These data demonstrate inhibition of progesterone secretion in human pregnancy using non-hormonally active steroids. The pattern of steroid precursors indicates that while both drugs inhibit 3-beta-hydroxy steroid dehydrogenase activity, WIN 32729 is more selective and only interferes with adrenal steroid biosynthesis at high doses.

3-Hydroxysteroid Dehydrogenases↗

Serum levels of progesterone and some of its metabolites including deoxycorticosterone after oral and parenteral administration.

Single 100-mg doses of progesterone were given orally and as intramuscular injections to four women during the follicular phase of the menstrual cycle. After oral administration serum levels of progesterone increased rapidly to reach luteal phase values (mean maximum level 55.6 nM) within 1-4 h and were still elevated after 12 h. The serum concentrations of 20 alpha-hydroxy-4-pregnen-3-one showed a similar pattern while there were only minor transient changes in 17 alpha-hydroxyprogesterone concentrations. The serum levels of cortisol and 4-androstene-3,17-dione were unaffected. In comparison, after intramuscular administration values two to three times higher than by the oral route were achieved. A significant increase in serum deoxycorticosterone was recorded in all women. The mean ratio between the change in deoxycorticosterone and progesterone was increased after oral administration. Oral treatment with natural progesterone may develop into an attractive alternative to synthetic progestogens but the conversion of progesterone into a potent mineralocorticoid may be a potential disadvantage.

17-alpha-Hydroxyprogesterone↗

The effect of the antiprogestin RU 486 on uterine contractility and sensitivity to prostaglandin and oxytocin.

The effect of RU 486, a steroid acting as an antiprogestin at the receptor level, on uterine contractility and sensitivity to the prostaglandin analogue, 16-phenoxy-PGE2 methyl sulfonylamide (16-phenoxy-PGE2) and to oxytocin was studied in 29 women in early pregnancy. Seven untreated women at the same stage of pregnancy served as controls. In the untreated women no spontaneous uterine contractility was recorded and the response to 0.25 mg 16-phenoxy-PGE2 was characterized by an increase in uterine tonus with superimposed irregular contractions of low amplitude. Treatment with 25 mg RU 486 twice daily resulted in the appearance of regular uterine contractions at 24 h in two out of five patients and in all patients at 36, 48 and 72 h after the start of RU 486 treatment. The withdrawal of progesterone influence changed the inactive early pregnant uterus into an active organ. Administration of 16-phenoxy-PGE2 caused an obvious stimulation of both frequency and amplitude of the contractions. In addition, the significantly increased sensitivity to the prostaglandin analogue, but not to oxytocin, was already apparent 24 h after the start of RU 486 treatment. We have previously shown that the addition of one intramuscular injection of 16-phenoxy-PGE2 on the fourth day of treatment with RU 486 (25 mg twice daily) significantly increased the abortifacient effect of the antiprogestin during early pregnancy. The present study suggests that a shorter treatment may be possible.

Abortion, Therapeutic↗

Oral contraceptives: relations to mammary cancer, benign breast lesions, and cervical cancer.

The results of experimental studies on the relationship of estrogens and oral contraceptives to mammary lesions demonstrate that the type of response obtained depends largely on the species and strain of animal that is employed. A variety of clinical studies has failed to demonstrate that estrogen can cause mammary cancer, this lack of effort correlates with the results obtained in various studies in animals. Similar relationships exist for oral contraceptives, and the clinical data show good agreement in demonstrating that the contraceptive steroids do not have a tumorigenic effect on the human mammary gland. Estrogen can increase the occurrence of cervical cancer in certain strains of mice, but apparently this effect is not observed in other species of animals, including man. The preponderance of data shows that oral contraceptives do not adversely affect the occurence of abnormal Papanicolaou smears, cervical dysplasia, cervical cancer in situ, or invasive cervical cancer.

Breast Diseases↗

[Mechanism of action of progestins in the treatment of hormone-dependent breast cancer (author's transl)].

The in vitro interference of some gestagens with the binding of 3H-17-beta-oestradiol to cytosol specific receptors was investigated with a view to elucidating the mechanism of action of progestins in the treatment of human hormone-dependent breast cancer. A decrease (up to 85%) of oestradiol binding capacity was observed with high concentrations of progesterone, clogestone and medrogestone. These findings are in good agreement with those previously obtained by the same progestins in our laboratory on rat uterine estrogen receptors in vitro or in vivo. These results provide the support for the hypothesis that the mode of action of progestins in the therapy of mammary and perhaps uterine carcinomas is to some extent related to the inhibition of oestradiol binding to cytosol specific receptors.

Breast Neoplasms↗

Pregnancy-specific beta 1-glycoprotein and chorionic gonadotropin-like immunoreactivity during the latter half of the cycle in women using intrauterine contraception.

In a cross-sectional study, the serum levels of pregnancy-specific beta 1-glycoprotein (PSBG), hCG, human LH, and progesterone were measured by RIAs during 94 mid or late luteal phases of 69 women using oral contraceptives. Subsequent spontaneous menstruation took place in every cycle. None of the women using oral contraceptives had any PSBG or hCG-like immunoreactivity in serum. In women with intrauterine devices, PSBG was found in six cycles (6.4%) and hCG-like immunoreactivity was demonstrated in one cycle only, where PSBG also was present. In two out of six PSBG-positive cycles, menstruation was delayed by 5 and 16 days. Although rare, the transient occurrence of trophoblastic antigens in women using intrauterine contraception is taken as evidence for an occult pregnancy in these apparently infertile cycles.

Chorionic Gonadotropin↗

[Electron microscopic observations of the rat endometrium during the implantation period, with special reference to its sex steroid hormone regulation (author's transl)].

Ultrastructural changes in the rat endometrium under several conditions including experiments of the inhibition of implantation were studied to clarify the sequential changes of the endometrium and their endocrinologic background during ovoimplantation. The following pertinent findings were noted. 1) Normal pregnancy. In the luminal surfaces, the microvilli were short and arranged rather irregularly and lost their so-called glycocalyx on L3. The large fungus-like protrusions appeared on L4. On L5, the luminal surfaces were completely covered with small serrated cytoplasmic protrusions. They formed the interdigitation btween the apposed surfaces and the uterine lumen was disappeared when the uterus was fixed in situ by the arterial perfusion method. High ATP-ase activity was demonstrated at the site of interdigitation. In the apical cytoplasm, many apical vesicles, well developed Golgi apparatuses, and dilated cisternae of the granular endoplasmic reticulum were observed on L3. On L5, however, these apical vesicles decreased in number and the Golgi apparatuses were small. On the contrary, the semilunar and coated vesicles were numerous, and the lysosomes increased both in number and size. Acid phosphatase activity was detected in these lysosomes. In the glandular epithelium, progressive increase in the number of small granules and the amount of amorphous substance were observed in the glandular lumen from L2, to L4. But on L4, some autophagosomes had already appeared in the cytoplasm. Swollen and degenerated mitochondria as well as many vacuoles were recognized on L5. In the stromal cells, the cytoplasm was enlarged, and contained many polyribosomes, granular endoplasmic reticulum with markedly dilated cisternae, lysosomes and lipid droplets on L5. The cytoplasmic protrusions on L5 were elongated and showed various features; one of them was situated very closely to the basement lamina of the luminal epithelium, and the other surrounded the lumen. Some of these protrusions were connected with the desmosomes. High ATP-ase activity was localized in these cytoplasmic protrusions, on the surfaces of the stromal cells, and in the stroma itself. 2) Delayed implantation and estrogenic transformation. In delayed implantation, the luminal surfaces were covered with regular microvilli and several fungus-like cytoplasmic protrusions. The cytoplasm contained many apical vesicles and large Golgi apparatuses that were observed both on L3 and L4 in normal pregnancy. At 48 hrs after the injection of estrogen, the interdigitation between the apposed luminal surfaces was also established. In the glandular epithelium, a slight enlargement of the glandular lumen and the appearance of small granules similar to those observed in normal pregnancy were noted at the 4th hr of estrogen treatment. In the stromal cells, two cells apposed each other very closely at the 4th hr and formed large cell masses at the 48th hr of estrogen treatment...

Animals↗

Effects of RMI 12,936, a synthetic antiprogestational steroid, in the rat.

The antifertility effect of RMI 12,936 in the rat is shown to be reversible. Luteal hypertrophy followed administration to pregnant, but not to pregnant hysterectomized rats. Similar hypertrophy followed administration to pseudopregnant, immature gonadotrophin-treated, and immature hysterectomized and gonadotrophin-treated rats, but the ovarian sensitivity to gonadotrophins was reduced or unchanged, suggesting that the ovarian hypertrophy is due to a direct ovarian action of RMI 12,936. Progesterone production on Day 15 of pregnancy by the enlarged ovaries following RMI 12,936 administration on Day 8 was not significantly different from control levels, but there was a highly significantly reduction on Day 9. An isomer of RMI 12,936, Tsomer 201, presumed to be 7alpha-methyltestosterone, was shown to have antifertility and uterotrophic activities in rats similar to those of RMI 12,936. Unlike RMI 12,936, however, Isomer 201 did show significant cross-reaction in the competitive protein-binding assay for progesterone and did not cause significant reduction in peripheral progesterone levels on Day 9 after administration on Day 8. From this and previous evidence it is concluded that RMI 12,936 inhibits progesterone synthesis, possibly by acting as an alternative substrate for ovarian delta(5)3-ketosteroid isomerase, and that the product is probably a competitive antagonist of progesterone at the receptor level.

Age Factors↗

Uterine and ovarian estrogen receptor levels in climacteric women.

High affinity cytoplasmic estrogen receptors in the endometrium, myometrium and ovary of 15 climacteric women were studied. In addition, the concurrent serum estradiol and progesterone level of each woman was estimated and the endometrium examined histologically. The cytoplasmic estrogen receptor level of the endometrium and myometrium had remained extremely high in some cases several years after the menopause and in the presence of a completely atrophied endometrium. The lowest endometrial and myometrial estrogen receptor levels in pre-menopausal women were measured towards the end of the menstrual cycle. The eodometrial estrogen receptor level was roughly 2--3 times the comparable myometrial level. Estrogen receptors were also encountered in all cases in the cervical myometrium. The estrogen receptor levels of the ovary were low in all cases.

Adult↗

[Steroid receptors and hormonal receptivity. New pharmacological and therapeutic approaches applicable to the control of fertility].

The definition and main characteristics of the steroid hormone receptors are given. One may note a relationship between hormonal receptivity and the physiological changes in the concentration of the receptors in the target organs. The distribution of the various receptors is given in detail showing the existence of (a) different receptors for the same hormone in different target cells; (b) different receptors for different hormones in the same cells; (c) different receptors for the same hormone in the same cell. A new pharmacological approach is proposed based on differentiation of receptivities from which there results a dissociation of the therapeutic effects.

Drug Interactions↗