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At least 19 recordsLinked to original sources
PubMed1991

The use of antiprogestin (RU 486) for termination of second trimester pregnancy.

Pretreatment with laminaria tent is often used in prostaglandin-induced second-trimester abortion to increase efficacy and shorten induction-to-abortion time. In the present study, two alternatives to soften the cervix and dilate the cervical canal, the antiprogestin RU 486 and intra-cervical application of PGE2, were studied. The study included 71 women requesting legal abortion in the 15th to 23rd week of pregnancy who were treated with repeated vaginal applications of 9-methylene PGE2 in a hydrophilic gel (5 mg every 4th hour) following pretreatment with 200 mg of RU 486 and/or intracervical administration of 0.5 mg of PGE2 gel. The mean interval from start of vaginal prostaglandin treatment to abortion was 13.2 h after intracervical PG-treatment, 10.0 h after antiprogestin and 6.6 h after the combined pretreatment. Patients who received pretreatment with RU 486 alone or in combination with intracervical PGE2 experienced the lowest frequency of episodes of vomiting. Of these two pretreatment alternatives, RU 486 alone has the advantage of a shorter hospital stay. It can be concluded that vaginal administration of 9-methylene PGE2 after pretreatment with RU 486 was a highly effective, safe and rapid procedure for termination of mid-trimester pregnancy, was well tolerated by the patients and was associated with few side effects.

16,16-Dimethylprostaglandin E2↗
PubMed1991

Effects of mifepristone in vivo on decidual prostaglandin synthesis and metabolism.

Mifepristone is an effective abortifacient in combination with an exogenous prostaglandin but its mechanism of action is unknown. Mifepristone stimulates prostaglandin production from decidua in tissue culture. To determine whether this effect also operates in vivo, we treated women with mifepristone 24, 36 and 48 hours prior to surgical termination. Decidua was removed at operation and the ability of the tissue to generate prostaglandin in culture subsequently assessed. Pretreatment with mifepristone 36 hours prior to termination of pregnancy resulted in an increased production of PGF2 alpha in tissue culture (p less than 0.01). A significant decrease in PGFM production was seen 24 hours after pretreatment with mifepristone in vivo (p less than 0.01). These results suggest that the increased uterine activity observed after administration of mifepristone may be due to stimulation of endogenous prostaglandin production and inhibition of prostaglandin metabolism.

Culture Techniques↗
PubMed1990

Progesterone receptor antagonists and prostaglandins in human fertility regulation: a clinical review.

Progesterone receptor antagonists have been developed by substitutions at the 11-beta and 17 side-chain positions of the progestagen norethisterone. The most studied progesterone receptor antagonists are mifepristone (Mifegyne; Roussel-UCLAF; RU486) and ZK98734 and ZK98299 (Schering AG). These compounds bind avidly to the progesterone receptor and glucocorticoid receptor but have essentially no binding to the mineralocortocoid, oestrogen or androgen receptors. Mifepristone also binds avidly to albumin, resulting in a half-life of approximately 24 h after oral administration. Progesterone receptor antagonists can induce menstruation by a direct action upon the endometrium. They have also been shown to exert weak progesterone agonist actions in certain circumstances and to modulate pituitary hormone secretion by antagonizing the feedback actions of progesterone. Moreover, they release prostaglandin F2 alpha and E2 from human endometrium or early pregnancy decidua and reduce the metabolism of these eicosanoids. Clinically, progesterone receptor antagonists have been used in trials of menstrual regulation, abortion and induction of labour, and during treatment of breast or ovarian cancer, some forms of hypertension and meningioma. Progesterone receptor antagonists have been administered to approximately 70,000 women in 18 countries as medical abortifacients. They have been proven, especially when combined with prostaglandin analogues, to be as effective as surgical methods of termination of pregnancy. Progesterone receptor antagonists have focussed international attention on menstrual regulation, abortion and the rights of women to regulate their fertility.

Abortifacient Agents, Steroidal↗
PubMed1992

Conditions for choosing between drug-induced and surgical abortions.

In France, pregnant women with amenorrhoea of no more than 49 days intending to terminate pregnancy can choose between a surgical abortion via vacuum aspiration under local or general anesthesia and a drug method combining Mifepristone orally administered (RU 486 degrees), with a prostaglandin analogue. This prospective survey was conducted to study the conditions under which women choose their abortion method, and to evaluate the acceptability of each method after the abortion. The data gathered from 488 women were analyzed according to their initial decision, and then according to the method actually used. The majority (62%) chose RU 486. The women's choice was found to be linked to sociodemographic characteristics such as age, education, occupation, geographic origin, and certain attitudes towards pregnancy, as well as to the individual criteria of each method. The women who chose the drug protocol had most often already made their decision before going to the family planning center (68%), having been advised by their doctor (20%). They were slightly less satisfied with the abortion experience than they had expected: 12.4% were unsatisfied in the RU group and 3.6% in the aspiration group. They needed more rest and quiet afterwards (50%) than the other women. They were distinguished by their desire to verify the expulsion (63%). The length of pregnancy is therefore not the only criterion to be considered when recommending one or other of these methods: the women concerned have different requirements and should have several possibilities to choose from.

Abortion, Induced↗
PubMed1992

Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception.

BACKGROUND: Mifepristone (RU 486) is a synthetic steroid with potent antiprogestational and antiglucocorticoid properties that provides an effective medical method of inducing abortion in early pregnancy. Since progesterone is essential for implantation, we tested the use of mifepristone for emergency postcoital contraception. METHODS: We studied 800 women and adolescents requesting emergency postcoital contraception who had had unprotected intercourse within the preceding 72 hours. A total of 398 women and adolescents were randomly assigned to treatment with 100 micrograms of ethinyl estradiol and 1 mg of norgestrel, each given twice 12 hours apart (standard therapy), and 402 women and adolescents were randomly assigned to receive 600 mg of mifepristone. RESULTS: None of the women and adolescents who received mifepristone became pregnant, as compared with four of those who received standard therapy; the difference in failure rates between the two regimens was not statistically significant. The number of pregnancies in each group was significantly lower than the number expected according to calculations based on the day of the cycle during which intercourse had taken place (P less than 0.001). In many subjects the stage of the cycle as calculated by menstrual history was inconsistent with measurements of plasma progesterone or urinary pregnanediol excretion. The subjects treated with mifepristone reported less nausea (40 percent vs. 60 percent) and vomiting (3 percent vs. 17 percent) on the day of treatment, as well as lower rates of other side effects, than the subjects treated with the standard regimen, but they were more likely to have a delay in the onset of the next menstrual period (42 percent vs. 13 percent). CONCLUSIONS: Mifepristone is a highly effective postcoital contraceptive agent that, if used more widely, could help reduce the number of unplanned and unwanted pregnancies.

Adolescent↗
PubMed1991

A pilot study of acceptability of RU486 and ONO 802 in a Chinese population.

RU486 and ONO 802 in combination have been shown to be effective in early termination of pregnancy. Anecdotal information suggests that Chinese women have been using herbs to induce abortion, believing that such medication and means of abortion is less harmful to the body than surgery. Hence, a medical means of abortion using RU486 and ONO 802 may be the method of choice for some Chinese women. A pilot study involving 42 Chinese women in Hong Kong was conducted to explore the reasons for acceptance or refusal of RU486 and ONO 802 as abortifacient agents. It was found that more single women chose the medical method for abortion, the main reasons being fear of trauma to the body due to surgery and the feeling of having undergone menstrual regulation rather than having had an abortion with the medical method. Those who refused the treatment were worried about the efficacy and side effects of the new drugs and the long induction-abortion interval. There were 3 failures in the medical group of 23 women. All these 23 women were gland they had chosen the medical abortion method. Twenty-one out of the 23 women said they would choose the same abortion method again. The practice of the use of Chinese herbs was not more common in this group of women as compared to women who did not choose this method of abortion.

Abortifacient Agents, Nonsteroidal↗
PubMed1992

A study of gemeprost alone, dilapan or mifepristone in combination with gemeprost for the termination of second trimester pregnancy.

It is well established that abortion can be induced successfully in midtrimester of pregnancy by gemeprost vaginal pessaries. A randomised study was carried out to determine the efficacy of mifepristone and dilapan in combination with gemeprost for second trimester termination between 12-18 weeks' gestation. A contemporary group of women treated with gemeprost alone was used as a control group. A single course of 4 x 1 mg gemeprost pessaries was administered every six hours. If abortion had not occurred after 24 hours, a further course of 5 x 1 mg pessaries was administered every three hours over the next 24 hours. In the first twenty hours after administration of gemeprost, 95%, 85% and 72% of women aborted in the mifepristone, dilapan and the control group, respectively. The median induction-abortion interval in the mifepristone group (6.6h) was significantly shorter than the other two groups and fewer pessaries were required to induce abortion. The incidence of diarrhoea and vomiting was lower in the mifepristone than the other two study groups. This study demonstrated the efficacy of mifepristone in combination with gemeprost and this regimen is associated with fewer gastrointestinal side effects.

Abortifacient Agents, Nonsteroidal↗
PubMed1991

Mifepristone or vacuum aspiration in termination of early pregnancy.

This trial compared the termination of early pregnancy (amenorrhoea less than 43 days) by 600 mg orally of the antiprogesteron Mifepristone to the traditional method of vacuum aspiration. Fifty women were randomly assigned to either of the treatments. All the patients treated with vacuum aspiration had a complete abortion. Three of these patients developed pelvic inflammatory diseasae (PID) after the aspiration. Another patient had the uterus perforated during the procedure, and an emergency laparotomy had to be performed. The patients in the evacuation group spent more days in bed and needed longer sick leave after the treatment than the patients in the Mifepristone group. In the Mifepristone group, six patients had incomplete abortions and all were treated by evacuation. Three of the patients developed PID after the evacuation. A decrease of 40% or more in beta hCG from the initial value to the value 1 week later were invariably associated with complete abortion. In both groups the changes in hemoglobin were insignificant and no patients needed blood transfusion or emergency evacuation. The Mifepristone treatment is a simple and safe alternative to vacuum aspiration for termination of early pregnancies.

Abortion, Incomplete↗
PubMed1992

Delayed endometrial maturation induced by daily administration of the antiprogestin RU 486: a potential new contraceptive strategy.

OBJECTIVE: Our objective was to determine if a progesterone antagonist might interdict the development of a secretory endometrium. STUDY DESIGN: Eleven normally cycling women not at risk for pregnancy received RU 486 (1 mg/day orally) or placebo throughout one menstrual cycle in a randomized, double-blind, crossover fashion. Estradiol, progesterone, and placental protein 14 were measured every 3 days; luteinizing hormone was measured until the midcycle surge was detected. An endometrial biopsy was performed on luteal phase day 7 to 9 and interpreted with Noyes' criteria. Differences between treatment groups were analyzed by the Student t test. RESULTS: RU 486 delayed ovulation, retarded endometrial maturation, and reduced peak levels of placental protein 14 without affecting gonadal steroid production. The abnormalities in endometrial morphology and function are similar to those seen in infertile women with luteal phase defects. CONCLUSION: We hypothesize that this regimen of antiprogestin administration may prevent implantation and offer a novel strategy for fertility control.

Adult↗
PubMed1991

The effects of the antiprogesterone RU486 (Mifepristone) on an endometrial secretory glycan: an immunocytochemical study.

OBJECTIVE: To examine the effects of progesterone (P) receptor blockade by RU486 (Mifepristone; Roussel-Uclaf, Paris, France) on a secretory endometrial glycan recognized by monoclonal antibody D9B1. DESIGN: Retrospective comparison of endometrial biopsies from treated and untreated women from 2 to 8 days after the luteinizing peak (LH) peak. SETTING: Infertility clinic, Jessop Hospital for Women, Sheffield. PATIENTS: Twenty-two normal fertile women received the RU486. A control group of 44 normal fertile women were also assessed. INTERVENTIONS: RU486 was administered to 22 normal women during the first half of the luteal phase and an endometrial biopsy examined 3 days later. MAIN OUTCOME MEASURES: Immunohistochemistry was used to assess the production and secretion of the D9B1 epitope. RESULTS: When the drug was given 2 days after the LH peak, it prevented appearance of the epitope. When RU486 was administered 5 days after the LH peak, epitope already present in gland cells was subsequently secreted. CONCLUSIONS: These data suggest that production of the sialo-oligosaccharide is P-dependent, but secretion through established intracellular pathways is P-independent.

Adult↗
PubMed1990

The effect of RU 486 administered during the early luteal phase on bleeding pattern, hormonal parameters and endometrium.

The purpose of the present study was to investigate the effect of a single dose of RU 486 administered very early in the secretory phase on endometrial development and levels of progesterone receptors, on plasma levels of gonadotrophins and ovarian hormones and on the pattern of menstrual bleeding. Twenty-four regularly menstruating subjects participated and were studied during a control, a treatment and a follow-up cycle. In the treatment cycle, a single dose of 200 mg RU 486 was given in the evening of the second day after the urinary LH peak. Plasma was collected from cycle day 10 until menstruation in both control and treatment cycles. The lengths of the control, treatment and follow-up cycles were equal. Three of the subjects had slight vaginal bleeding in association with RU 486 intake which, however, did not disturb their normal menstrual rhythm. Plasma levels of oestradiol, progesterone and FSH were not affected in the treatment cycle, whereas LH levels increased slightly. The elimination half-life of RU 486 was 28.6 h. An endometrial biopsy was taken 12, 36 or 84 h (LH + 3, LH + 4 and LH + 6) after drug intake (eight subjects in each group) and another biopsy was taken on the corresponding day in the control cycle. The specimens were assessed by morphometric analysis and for cytosolic progesterone receptor concentrations. Endometrial biopsies taken 12 h (on LH + 3) after RU 486 intake contained significantly (P less than 0.001) lower levels of cytosolic progesterone receptors than in the control cycle, but levels at 36 and 84 h were similar.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
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↗
PubMed1991

Pretreatment of the primigravid uterine cervix with mifepristone 30 h prior to termination of pregnancy: a double blind study.

OBJECTIVE: To determine the effect of the antiprogestogen mifepristone (RU 486) on cervical resistance before first trimester termination of pregnancy. DESIGN: Prospective double blind randomized placebo controlled study. SETTING: Department of gynaecology in a university teaching hospital, Sheffield. SUBJECTS: 80 Primigravid women greater than 18 years of age, undergoing termination of pregnancy at between 7 and 13 weeks gestation. INTERVENTIONS: A single dose of 600 mg of mifepristone or placebo given orally 30 h before termination of pregnancy under general anaesthesia. MAIN OUTCOME MEASURES: Cervical resistance to dilatation. RESULTS: Pretreatment with mifepristone significantly reduced the amount of force required to dilate the cervix to 10 mm. In comparison with placebo, the mean sum of the peak forces obtained with dilators 4 to 10 mm was reduced from 84.3 N (SD 29.7) to 46.0 N (SD 26.7). Two women in the treated group had a cervical resistance of greater than 100 N compared with nine women in the placebo group (RR 0.18, 95% CI 0.04-0.89). The 8 mm dilator could be passed with less than 5 N force in 16 women (43%) in the treated group compared with none in the placebo group. Women in the active treatment group had more preoperative pelvic pain and vaginal bleeding but less postoperative pain. CONCLUSION: Mifepristone significantly reduces cervical resistance in the first trimester of pregnancy and produces minimal side effects.

Abortion, Therapeutic↗
PubMed1991

Pre-operative cervical preparation before first trimester vacuum aspiration: a randomized controlled comparison between gemeprost and mifepristone (RU 486).

OBJECTIVE: To compare the effectiveness of 200 mg mifepristone with 1 mg gemeprost vaginal pessary in achieving cervical dilatation and softening ('priming') before late first trimester pregnancy vacuum aspiration. DESIGN: A randomized, operator blind, placebo controlled trial. SETTING: UK teaching hospital. SUBJECTS: 90 primigravid women with 63-91 days amenorrhoea and ultrasonically confirmed single living fetus of correct size for gestational age. INTERVENTIONS: The women were allocated to receive 200 mg mifepristone orally or an identical oral placebo 36 h before operation or 1 mg gemeprost vaginal pessary 3-4 h preoperatively. MAIN OUTCOME MEASURES: Onset of new symptoms following drug administration, a proven objective measure of the force required to dilate the cervix, and estimated intraoperative blood loss. RESULTS: There were no significant differences in the baseline cervical dilatation, the force required to dilate the cervix or the volume of intraoperative blood loss between the active treatment groups. Both drugs were significantly more effective than placebo. Significantly fewer women in the mifepristone group had adverse side effects than in the gemeprost group. CONCLUSIONS: Mifepristone is a highly effective cervical priming agent, and has the advantages of being an oral preparation associated with few side effects.

Abortifacient Agents, Nonsteroidal↗
PubMed1990

The antiprogesterone steroid, RU 486 (mifepristone).

RU 486 (Mifepristone) represents a major development in the field of hormone antagonists as the first effective antiprogestogen. A number of therapeutic roles for the drug are envisaged. It is already being used extensively around the world for the procurement of first trimester abortion--particularly in combination with prostaglandins. It also has been shown to be effective as a cervical ripening agent and for the induction of labour. Initial human studies have involved nonviable pregnancies and more work is needed in animal models before the drug can be deemed safe for use in viable human pregnancies in the third trimester.

Abortion, Therapeutic↗
PubMed1992

Mifepristone (RU 486) treatment of meningiomas.

Meningiomas are common brain tumours which are generally benign, well circumscribed and slow growing. In a minority of patients complete surgical removal is not possible and re-growth of tumour tissue is a major clinical problem. Most meningiomas contain progesterone receptors. The anti-progestational drug mifepristone (RU 486) binds to these receptors. Ten patients were treated with 12 recurrent or primary "inoperable" meningiomas, all of whom had shown recent neuroradiological and/or ophthalmological evidence of tumour growth. They received 200 mg mifepristone daily for 12 months. Most patients initially had complaints of nausea, vomiting and/or tiredness. In four patients prednisone (7.5 mg/day) was given after which these side-effects subsided. CT scan analysis of tumour size, showed progression of growth of five meningiomas in four patients, stable disease in three patients with three tumours and regression of four tumours in three patients. A decrease in the complaints of headache and an improved general well being was observed in five patients. Two patients died during the treatment period from unrelated causes. Mifepristone treatment resulted in control of tumour growth (= stable disease) in six of 10 patients who had shown recent evidence of tumour growth. In three of these six patients consistent tumour shrinkage was observed.

Adult↗
PubMed1990

Effect of chronic treatment with the glucocorticoid antagonist RU 486 in man: toxicity, immunological, and hormonal aspects.

Suppression of immune function was traditionally thought to occur only with pharmacological levels of glucocorticoids. However, recent studies in rodents have suggested that glucocorticoids exert tonic antiinflammatory/immunosuppressive effects even at basal nonstress concentrations. To examine whether basal glucocorticoid secretion modulates immune function in man we employed the specific glucocorticoid receptor antagonist RU 486. If a tonic level of inhibition of the immune system by basal glucocorticoid levels was present, then a potentiation or enhancement of immune function might evolve in the absence of glucocorticoid action. To examine this hypothesis, we studied 11 healthy male normal volunteers who received RU 486 (10 mg/kg.day) or placebo vehicle, divided into 2 daily oral doses, for 7-14 days. Blood samples were collected every 2 days for measurement of plasma ACTH and cortisol concentrations along with 24-h urine samples for measurement of 17-hydroxysteroid and free cortisol excretion. Complete and differential blood counts, erythrocyte sedimentation rates, C-reactive protein, antinuclear antibodies, rheumatoid factor, and quantitative immunoglobulins were also determined at 2-day intervals. Leukocytes were obtained by leukopheresis for phenotypic characterization and functional analysis before and 7 days after the initiation of RU 486 or placebo therapy. Blockade of cortisol receptors with RU 486 was associated with marked compensatory elevations of plasma ACTH and cortisol and increases in 24-h urinary excretion of 17-hydroxysteroids and free cortisol. Unexpectedly, 8 of the 11 subjects developed generalized exanthem after 9 days of RU 486 treatment. One subject developed symptoms and signs consistent with the diagnosis of adrenal insufficiency. Total white blood cell counts, absolute lymphocyte, neutrophil and eosinophil counts, erythrocyte sedimentation rate, and quantitative immunoglobulins did not change with RU 486 therapy. Similarly, T-, B-, and natural killer cell subsets did not change during RU 486 treatment. Furthermore, functional evaluation of lymphocyte cytotoxicity and proliferation revealed no changes. We conclude that administration of high doses of RU 486 to normal volunteers does not result in measurable enhancement of immune function. This suggests that in man, glucocorticoids may not exert a tonic inhibitory effect on the immune system as they appear to do in rodents. Alternatively, the compensatory increase in endogenous cortisol may obviate any effect of the glucocorticoid antagonist on the immune system.(ABSTRACT TRUNCATED AT 400 WORDS)

Adrenal Insufficiency↗
PubMed1991

The endocrine effects of long-term treatment with mifepristone (RU 486).

Mifepristone (RU 486) is a compound with progesterone as well as cortisol-blocking activities. We investigated the endocrine effects of long-term therapy of 10 patients with meningiomas with 200 mg mifepristone daily for 1 yr. Most patients initially complained of nausea, vomiting, and/or tiredness. In four patients prednisone (7.5 mg/day) had to be given simultaneously in order to overcome these side-effects. In retrospect those patients who presented with the most severe side-effects showed the most rapidly occurring activation of the hypothalamo-pituitary-adrenal-axis, as measured by an increase of circulating cortisol levels as well as of urinary cortisol excretion. Therapy with RU 486 activated the hypothalamo-pituitary-adrenal axis, resulting in a resetting of this system at a higher level at which the diurnal rhythm and the responsiveness to CRH stimulation were maintained, whereas the sensitivity to dexamethasone had diminished. Secondarily the production of androstenedione and estradiol increased considerably. These endocrine changes were caused by the induction of partial cortisol receptor resistance during therapy with RU 486. The compensatory overproduction of androgens and consequently of estrogens during long-term RU 486 therapy might limit its use as a single treatment in the treatment of estrogen-dependent cancer.

Adrenocorticotropic Hormone↗