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At least 703 records · Page 39Linked to original sources
PubMed1993

Anordiol is more potent than anordrin for terminating pregnancy when administered with RU 486.

In view of the unexpected ability of anordrin to synergize with RU 486 in terminating pregnancy, it was pertinent to examine the actions of the dihydroxylated metabolite of anordrin, anordiol, alone and in combination with RU 486. Does of RU 486 (1 mg/kg/day) and anordiol (0.6 mg/kg/day) that were ineffective when given alone terminated pregnancy with complete resorption of embryos when administered together. A smaller dose of anordiol than anordrin is required to achieve this synergistic effect with RU 486. This anordrin metabolite increased uterine weight in the ovariectomized rat similar to estradiol. The estrogenicity of anordiol in the uterine weight assay was about 1/120 of that of estradiol. Anordiol does not exert antiestrogenic activity in the uterine weight assay when administered at doses that terminate pregnancy. Administration of anordiol at doses that do not terminate pregnancy resulted in a significant suppression of serum progesterone concentrations during the period of medication; these observations suggest that anordiol has an inhibitory effect on progesterone biosynthesis. When the same dose of anordiol was given concomitantly with sufficient RU 486 (e.g., 1 mg/kg/day) to terminate pregnancy, the progesterone levels were reduced to low levels throughout the experiment. These observations support the postulate that the actions of anordrin are mediated by its metabolite, anordiol. The administration of anordiol plus RU 486 results in a more dramatic change in the functional progesterone:estradiol ratio than when either agent is administered alone.

Abortifacient Agents, Steroidal↗
PubMed1995

Effect of levonorgestrel-releasing intrauterine device on hormonal profile and menstrual pattern after long-term use.

In the present study 14 women after 6 years' use of levonorgestrel-releasing IUD were investigated for the changes of LH, progesterone (P), estradiol (E2), prolactin (PRL) and serum binding globulin (SHBG) in relation to the levonorgestrel levels throughout a segment of 26-40 days with the aim of comparing the hormonal profiles with those during the first year of use of Lng-IUD. Ultrasound scanning was used to follow the development of follicles along with the RIA measurement of hormones. The results of serum LH, P and E2 showed ovulation in 11 cases with either normal menstrual cycles (5 cases), prolonged or irregular cycles (4 cases) or with amenorrhea for 2-3 years (2 cases). One case showed insufficiency of luteal function and 2 cases showed anovulation but with follicular hyperactivity. Higher percentages of ovulatory cycles (78.5%) were found after 6 years of use. No case of complete suppression of ovulation was found. Anovulatory cycles only constituted 14.3%. Clinically, the development of follicles followed by ultrasound scanning further confirmed the hormonal findings. The persistent enlargement of follicles coincided with high levels of E2. After 6 years of use, the serum levels of levonorgestrel were still maintained at mean levels of 314.26 pmol/L and 470.63 pmol/L in the ovulatory and anovulatory groups, respectively. It is concluded that over two-thirds of the cases have ovulatory cycles after long-term use of Lng-IUD; the contraceptive effect is mainly due to its local action on the endometrium, with much less effect on the ovarian function.

Adult↗
PubMed1977

Effect of 15(s)15-methyl-PGF2alpha-methyl ester vaginal suppositories on circulating hormone levels in early pregnancy.

Intravaginal administration of 15-methyl-PGF2alpha-methyl ester in the form of suppositories terminated pregnancy in 70 percent of the cases whose last menstrual periods ranged from 35 to 56 days. The use of these suppositories in 49 patients, between 57 to 80 days of gestation, dilated the cervix by 10 mm or more, in one hundred percent of the cases. A decrease in circulating levels of estradiol-17beta and progesterone was observed following 15-methyl-PGF2alpha administration. The mean estradiol-17beta levels declined by about 55.9 percent at 9 hours whereas, the corresponding fall in progesterone was 32.7 percent. This was indicative of a direct action of 15-methyl-PGF2alpha on the corpus luteum. The vaginal use of 15-methyl-PGF2-alpha-methyl ester suppositories thus appears to be a promising method for the termination of early pregnancy and for pre-operative cervical dilatation. The termination of early pregnancy appears to be partly due to the luteolytic effect of 15-methyl-PGF2alpha besides stimulating uterine contractions.

Abortion, Induced↗
PubMed1982

Metabolic effects of progesterone.

Progesterone has important effects on carbohydrate, lipid and protein metabolism. This steroid induces hyperinsulinemia, possibly by direct action on pancreatic islets, while promoting glycogen storage in the liver. Paradoxically, it antagonizes the effects of insulin on glucose metabolism in adipose tissue and skeletal muscle. Progesterone stimulates deposition of body fat but had catabolic effects on protein metabolism. Provisional evidence is offered that the steroid may influence ketone body production by the liver as well. When these steroid actions are considered together, their most relevant expression appears to be the physiologic changes observed during normal pregnancy.

Adipose Tissue↗
PubMed1989

Plasma levonorgestrel levels and ovarian function during the use of a levonorgestrel-releasing intracervical contraceptive device.

Levonorgestrel, estradiol and progesterone plasma concentrations were measured over four years of use of a 20 micrograms/day levonorgestrel-releasing intracervical device (LNG-ICD). The mean levonorgestrel concentration showed a slight decline, being 142 + 46 (SD) pg/ml in the third month and 81 +/- 22 pg/ml in the 48th month of LNG-ICD use. However, considerable interindividual variation in levonorgestrel plasma levels between study subjects was observed. In 77% of the monitored cycles, ovulation or a luteinized follicle was observed when judged by a plasma progesterone elevation of over 5 ng/ml. Some follicular function was also noted in anovulatory cycles. Inhibition of ovulatory ovarian function is not the mode of contraceptive action of the LNG-ICD.

Adult↗
PubMed1999

Preregistration study on the safety and contraceptive efficacy of a progesterone-releasing vaginal ring in Chilean nursing women.

The contraceptive efficacy and safety of a progesterone-releasing vaginal ring (PVR) manufactured in Chile were compared to that of the Copper T 380A IUD (T-Cu) in nursing women enrolled at three Chilean clinics. A total of 285 volunteers chose to use the PVR and 262 the T-Cu. Plasma progesterone levels attained with the ring decreased from 25 to 14 nmol/L from month 1 to month 3 of use. Ring replacement was scheduled every 3 months. Volunteers continued in the study until weaning or completing the continuous use of four PVRs. No pregnancies occurred in 2320 and 2183 woman-months of exposure with the PVR and the T-Cu, respectively. Lower continuation rates in the first 6 months because of problems with use and a longer lactational amenorrhea were observed in the PVR than in the T-Cu group. Breast-feeding performance and infant growth were similar in both groups. These results confirm the high efficacy and safety of the PVR for nursing women and have led to the registration of the PVR by Chilean health authorities.

Adult↗
PubMed1977

Embryo mortality and altered uterine luminal proteins in progesterone-treated rabbits.

This study was undertaken to elucidate the location, time, and nature of embryo mortality induced by preovulatory progesteron administration. Progesterone was injected into rabbits on days -2, -1, and 0 (the day of mating) at doses of 0.5, 1.0, and 1.0 mg, respectively. Normal fertilization rates resulted, but embryonic death occurred by day 4. Embryos residing in progesterone-treated does for up to 3 days survived normally when transferred to normal recipients, whereas day 4 embryos from treated does exhibited a reduced ability to implant. Uterine fluid (UF) protein pattern was examined on days 1 to 7 after mating. Total UF protein levels were significantly greater in treated animals on day 4 than in controls. Uteroglobin secretion was significantly advanced in the treated animals by day 3. Examination of the time of the arrival of embryos into the uterus revealed a delay in the progesterone-treated rabbits. This delay, coupled with the earlier secretion of uteroglobin in the treated rabbits, indicated a possible asynchrony of approximately 1 day between embryo arrival in the uterus and certain uterine proteins. To determine whether UF could be etiologically implicated in the progesterone-induced embryonic death, embryonic development in vitro and in vivo was examined after exposure to UF collected at different gestational stages. More normal day 3 morulae placed in UF from day 3 control and day 2 progesterone-treated rabbits developed than similar morulae placed in UF from day 2 controls and day 3 progesterone-treated does. Hence, partial physiologic synchrony was achieved. This was interpreted to mean that "asynchronous" UF can be embryotoxic. Infertility was transient. Ability of the does to produce young at a pregnancy immediately following a progesterone-treated pregnancy was not impaired.

Albumins↗
PubMed1978

Vaginal progesterone for contraception.

Silastic vaginal rings impregnated with progesterone (P) or progesterone and estradiol (E) were used in nine women for thirty 21-day cycles to study the effect on ovarian function. The average daily rates of release of P and E from the rings were 2.2 mg/day and 220 microgram/day, respectively. In anovulatory treatment cycles the mean plasma level of P was 0.9 ng/ml. E levels fluctuated in the range seen in normally cycling women due to endogenous E production. In a menopausal woman the E levels increased to 50 to 100 pg/ml during treatment and FSH levels declined. Ovulation occurred in 18 (60%) of the treated cycles, and resulted in one pregnancy. Although the results rule out the use of these rings for contraceptive purposes, they indicate that at higher dosages the Silastic vaginal ring offers a mode of administration of natural steroids to be used in hormonal contraception.

Contraceptive Agents, Female↗
PubMed1981

The effect of a synthetic progestogen, ethylnorgestrienone, on hypothalamic-pituitary-ovarian function, cervical mucus, vaginal cytology, and endometrial morphology.

The antifertility mechanism of a new progestin preparation, ethylnorgestrienone (13 beta-ethyl-17 alpha-ethynyl-17-hydroxy-gona-4,9,11-triene-3-one) (R2323), was evaluated. The compound was administered orally in doses of 5 mg weekly to seven subjects for a total of nine treatment cycles. Each woman served as her own control and was studied during a normal menstrual cycle followed by a cycle in which she received R2323. Serum concentrations of luteinizing hormone (LH), follicle-stimulating hormone (FSH), estradiol, and progesterone, as well as cervical mucus properties, were studied serially during the control and treatment cycles. Results indicated that all control cycles were ovulatory. Ovulatory gonadotropin patterns were observed in four treated cycles, but preovulatory FSH and LH peaks and progesterone production during the luteal phase were suppressed significantly. Estradiol levels showed an early increase during the follicular phase and a significantly decreased preovulatory peak. Cervical mucus properties were altered and sperm penetration in cervical mucus was inhibited in all treatment cycles. These findings suggest that at least two different factors might be involved in the contraceptive mechanism of R2323: (1) alteration of the ovulatory process and progesterone production, and (2) cervical mucus changes leading to inhibition of sperm migration.

Adult↗
PubMed1985

Oestrogen deficiency after tubal ligation.

4 of 7 women who had undergone tubal ligation within the past seven years were found to have oestrogen excretion concentrations at ovulation below the tenth percentile. A disturbance in the oestrogen/progesterone ratio as a consequence of localised hypertension at the ovary, when the utero-ovarian arterial loop is occluded at tubal ligation, is proposed as a possible cause of oestrogen deficiency syndrome, dysfunctional uterine bleeding, and menorrhagia after tubal ligation. Similar pathophysiology may occur after hysterectomy with ovarian conservation.

Adult↗
PubMed1973

Effects of time and duration of progesterone administration on mammary tumours induced by 7,12-dimethylbenz(a)anthracene in Sprague-Dawley rats.

A reduction in tumour yield was apparent when progesterone administration was begun 25 days before feeding 7,12-dimethylbenz(a)anthracene (DMBA). This effect was most obvious when the duration of hormone administration was brief. Continuation of progesterone for some time after feeding DMBA caused a progressive diminution of the inhibitory effect, and 135 days of continuous hormone treatment entirely abolished the effects of 25 days pretreatment with the hormone.In contrast, when progesterone injections were begun 2 days after feeding DMBA, there was a trend towards enhancement of tumour yield. Continuous hormone administration appeared more effective than shorter treatment regimens.

Animals↗
PubMed1983

Comparison of the frequency of muscle pain associated with suxamethonium in pre- and post-ovulatory women and in those taking a combined oral contraceptive pill.

The frequency of muscle pain following the use of suxamethonium was compared in pre- and post-ovulatory women and in those taking a combined oral contraceptive pill. There were no statistically significant differences between the groups. It is suggested that serum concentrations of progestogen were too low to produce the protection against suxamethonium pains reported in late pregnancy.

Adolescent↗
PubMed1992

Early changes of affinity and binding sites of progesterone and oestrogen receptors in decidua exposed to RU 486.

Sixty patients with 6-7 weeks of amenorrhoea were randomly allocated to three groups. The women in the first group (control) took a placebo 24 h before undergoing a vacuum aspiration. The patients in the second and third groups were given 200 mg of RU 486 orally, 12 or 24 h before surgical interruption of their pregnancy. Decidua were collected and frozen in liquid nitrogen. By Scatchard plot analysis, the number of cytosolic binding sites (1798 +/- 803 fmol/mg DNA) of progesterone in decidua in the control group was significantly reduced (P less than 0.01) to 696 +/- 408 or 626 +/- 179 fmol/mg DNA by RU 486 treatment for 12 or 24 h respectively. The dissociation constants of both cytosolic and nuclear progesterone receptors in RU 486-exposed decidua were increased (P less than 0.01). The number of nuclear binding sites of oestrogen receptor was significantly higher (P less than 0.05) in decidua with RU 486 treatment for 12 h (178 +/- 77 fmol/mg DNA) compared to the control (89 +/- 32 fmol/mg DNA). The results suggest that RU 486 might regulate progesterone and oestrogen receptors in the decidua of early human pregnancy, either directly or indirectly.

Binding Sites↗