Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two contragestational agents, Mifepristone and Epostane, were compared in 78 pregnancy terminations at 49 days or less gestation. Mifepristone (RU 486, Roussel Uclaf, Romainville, France) is a steroid that antagonizes progesterone receptor binding in the decidua. It was taken twice daily at 25 or 50 mg for 7 days. Epostane (WIN 32,729, Sterling-Winthrop, Guildford, United Kingdom) is a progesterone synthesis inhibitor at 3B-hydroxy steroid dehydrogenase level acting on the endometrium. Women took 200 mg 4 times daily for 7 days. The criteria for complete abortion were bleeding and cervical dilatation with passage of products of gestation by Day 7, return to normal uterine size by Day 14 with hCG less than 10% of initial level. 61% of both Mifepristone groups aborted completely, and 83% of the women who completed the Epostane schedule did so. 3 women abandoned the Epostane regimen because of nausea. Only 2 incomplete abortions occurred in the Mifepristone group; the rest failed to abort and had vacuum aspiration on Day 7. Variations in blood chemistries and analysis of progesterone, hCG, estradiol and cortisol are discussed. The week-long treatment with Epostane is probably necessary, but dose and length of treatment with Mifepristone could be manipulated to get a more rapid response. Although the patients were satisfied with these regimens, they were not as efficient as vacuum aspiration or prostaglandin suppositories. Possibly both antiprogestins and even prostaglandins could be combined for better results.
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PMID:Early pregnancy termination with antiprogestins: a comparative clinical study of RU 486 given in two dose regimens and Epostane. 365 15

Postcoital contraceptives are available for adolescent use in the US. They include combination oral contraceptives (OCs), high dose estrogens, danazol, and IUDs. Mifepristone (RU-486) is currently not available in the US but is used in France, the UK, and Sweden. Postcoital contraception is especially important for adolescents who have a very high pregnancy rate due to poor contraceptive use. Administration of 2-5 mg ethinyl estradiol (EE) for 5 days beginning within 72 hours of unprotected intercourse yields pregnancy rates ranging from 0-0.92%. EE-related side effects include nausea, vomiting, sore breasts, and irregular menstrual bleeding. DES should not be used, since it is associated with reproductive tract anomalies and vaginal cancers in exposed offspring. Conjugated estrogens have not been used in adolescents for postcoital contraception. The Yuzpe regimen consists of 2 tablets of a combined OC with 200 mg EE and 2 mg dl-norgestrel administered within 72 hours of unprotected intercourse followed by the same dose 12 hours later. Common side effects are nausea and vomiting. Its pregnancy rate is 1.8%. Levonorgestrel-containing OCs can also be used. Administration of 800-1200 mg danazol up to 120 hours after unprotected intercourse protects against pregnancy in about 98% of cases. Copper IUDs have a high efficacy rate when used as postcoital contraception (99.9%), but public opinion, medicolegal considerations, financial costs, and potential for infection impede IUD as a postcoital contraceptive in the US. RU-486 is best known as an abortifacient. It is also a potential postcoital contraceptive. Two UK studies find that RU-486 used as a postcoital contraceptive has a very low pregnancy rate and fewer side effects than the Yuzpe regimen and danazol. It is much more costly than currently used postcoital contraceptives (600 mg of RU-486 cost US$ 68, while Ovral costs US$ 0.48-2.24). Nevertheless, RU-486 may replace the higher doses of OCs as a postcoital contraceptive method.
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PMID:Postcoital contraception: present and future options. 774 40

More widespread availability of emergency contraceptive methods has the potential to drastically reduce unwanted pregnancy. At present, only 3% of women use such methods and only 10% know how to obtain them; another 25-30% are unaware of this option. Use of the regimens is indicated in cases of rape, unprotected intercourse, and contraceptive mishaps such as condom breakage or skipping more than two oral contraceptive pills. Currently available regimens include 200 mcg of ethinyl estradiol and 2 mg of levonorgestrel taken in a split dose within 72 hours of unprotected intercourse, 0.75 mg of levonorgestrel taken within 8 hours of intercourse and repeated in 24 hours, 2-3 doses of 800 mg of the synthetic androgen danazol started within 72 hours of unprotected sex, insertion of a copper IUD, and a single dose of 600 mg of RU-486 within 72 hours; high doses of estrogen are no longer recommended due to serious side effects. Pregnancy rates range from 0.2-2.3% in users of combined estrogen and progesterone to 0.0-0.1% for the copper IUD and RU-486. The main side effects associated with these methods include nausea, vomiting, breast tenderness, and disruption of the menstrual cycle. Given the safety, simplicity, and effectiveness of these postcoital methods, it is recommended that all family planning programs make emergency contraception available.
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PMID:Emergency contraception. 789 64

Many women in the Netherlands depend on a postcoital contraceptive (PCC) method in situations of unprotected intercourse. The incidence rate for abortions and for adolescent pregnancies in the Netherlands is the lowest worldwide. Dutch society matter-of-factly accepts adolescent sexuality and provides formal and informal sex education and readily accessible contraceptive services. Emergency contraception should be administered within 72 hours after unprotected intercourse (e.g., rape or incest) or mechanical contraceptive failure. Administration of 5 mg ethinyl estradiol (EE) for 5 days as a PCC first occurred in the Netherlands in 1964, and PCC usage peaked at 55,000 in 1975. Side effects of EE include, in order of frequency, nausea, vomiting, tender breasts, and menorrhagia. Possible modes of action for EE are more rapid transport of fertilized ova through the oviduct and slowed maturation of the endometrium, resulting in suppressed implantation. The Yuzpe PCC method involves 4 tablets of a combined oral contraceptive (each tablet with 50 mcg EE + 250 mcg levonorgestrel) administered within 72 hours followed by 2 tablets 12 hours later. Side effects are similar to those of EE alone, as is the effectiveness rate. A dose of 0.75 mg levonorgestrel alone is as effective at preventing pregnancy as the Yuzpe regimen. Side effects are considerably less common with the levonorgestrel regimen than the Yuzpe regimen. For women who present more than 72 hours after and less than 7 days after unprotected intercourse or for those with contraindications to estrogen, a copper-releasing IUD can serve as a PCC. A postcoital IUD can cause serious complications for women with a sexually transmitted disease, however. Taking RU-486 during the luteal phase of the menstrual cycle greatly drops plasma levels of progesterone and estradiol. Postovulatory administration of an antiprogestogen is the best PCC method because of minimal side effects and a high success rate.
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PMID:Emergency contraception: a review. 795 9

The authors present a review of the literature on the current methods of second trimester termination of pregnancy and labour induction for fetal death. Prostaglandins are efficient, but may cause side-effects (nausea, vomiting) and painful contractions. Natural PGs (PGF2 alpha and PGE2), induce fetal expulsion in about 80% of cases within 24 h. PG analogues (sulprostone and gemeprost), are, presently, more used, and lead to fetal expulsion in 90% of cases, with less side-effects. Mifepristone, an antiprogesterone steroid, increases uterine activity, sensitizes myometrium to PG action, and induces cervical priming. Several clinical trials point out the advantage of mifepristone use, 24 to 48 h before PG. So, the duration of termination, and the PG dosage are reduced by half. A clinical protocol for second trimester termination, with mifepristone, and PG analogues, is proposed. In case of fetal death, labour induction is now accepted. The expulsion of a dead fetus is easier than a live one. PG and analogues show a good efficacy: > 90% success within 24 h. Mifepristone, alone, leads to fetal expulsion in 2/3 of cases, within 72 h, without side-effects. A clinical protocol of induction with mifepristone and PG in case of fetal death is proposed. In these two difficult clinical cases, mifepristone is of great interest, in reducing duration of termination, and increasing comfort and security for the patients.
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PMID:[Methods of second trimester pregnancy termination and evacuation of in utero dead fetuses. Value of mifepristone]. 799 6

The synthesis of mifepristone (RU-486) in 1980 was a major step in the development of a simple, safe, and effective method for abortion that women can use themselves. RU-486 ends pregnancies by blocking the action of circulating progesterone at its receptor. Hormones must be able to fit into their uniquely-shaped receptors in order for the necessary series of biological events to occur. RU-486 is shaped very much like the progesterone molecule with 2 important changes: a very long side chain which permits it to bind tightly to progesterone receptors and a bulky side chain which makes it inactive as a progestin. A large dose of RU-486 saturates the progesterone receptors in the uterus and prevents progesterone from playing its sustaining role in the pregnancy. RU-486 also increases the production of prostaglandins (which stimulate uterine contraction) and the sensitivity of the uterus to prostaglandins. Early studies on the use of RU-486 for first-trimester abortions concentrated on finding the best dose and circumstances to increase the abortion rate. In 1985, Swedish investigators developed a procedure which capitalized on the drug's ability to enhance sensitivity to prostaglandins. After RU-486 establishes sensitivity, the abortion rate is improved by administration of the prostaglandin gemeprost as a vaginal suppository in doses a fraction of those necessary to induce abortion. This combination is currently used in France, the UK, and Sweden. In France the gestational age limit is 49 days of amenorrhea, in the UK and Sweden it is 63 days. This procedure involves an initial administration of RU-496 with a follow-up visit in 2 days. If the woman has not aborted, she is given a dose of prostaglandin and observed for about 4 hours, during which time most women abort. A return visit is scheduled in 2 weeks. The efficacy of this method has been measured at 94-96%. The procedure has recently been improved by the use of an oral pill, misoprostol, as the prostaglandin. RU-486 has also been used successfully to prepare cervixes for mechanical dilation, although a pretreatment interval of 36-48 hours is necessary. Second-trimester induction-of-labor abortion time and required doses of prostaglandins are also reduced with RU-486, making the procedure a less expensive, more comfortable, outpatient process. RU-486 has also shown promise as an emergency (postcoital) contraceptive, with 2 trials in the UK resulting in no pregnancies and fewer women experiencing nausea or vomiting. The work that remains to be done to improve the use of RU-486 in early abortions involves establishing the correct dosage and simplifying the provision of service without compromising safety to insure that women living in remote areas will have access to the procedure.
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PMID:Mifepristone (RU 486) for induced abortion. 827 73

Between June and October 1991 health workers administered 1 dose of 600 mg mifepristone (RU-486) and a single oral dose of 400 mcg misoprostol on day 3 to at least 488 women at 25 centers in France to terminate pregnancy of less than 50 days duration. Pregnancy termination occurred within 48 hours in 2.9% of all women. They had only received RU-486. 1% vomited after taking the first dose of misoprostol, necessitating a second dose. The overall success rate for this regimen was 96.9%. 12 hours was the mean time between taking misoprostol and expulsion of the conceptus. The median time was 3 hours. The types of failure were incomplete expulsion of the conceptus (1.8%), ongoing pregnancy (0.8%), and prolonged bleeding (0.4%). Mean duration of bleeding following the regimen was 9 days. A second study occurred between March 1991 and March 1992 among at least 385 women at 1 center in France. They received RU-486 and misoprostol in the same manner as the women in study 1, but those who did not experience pregnancy termination within 4 hours after the initial dose received another 200 mcg dose of misoprostol. 5/5% experienced pregnancy termination before administration of misoprostol. 69.1% experienced termination within 4 hours. Pregnancy termination occurred within the first 3 hours in almost 90% of them. 27 women who did not abort within 4 hours did not take the additional dose and 26 of them aborted completely. The sole woman with a continued pregnancy underwent vacuum aspiration. 67 of the 71 women who took the second dose completely expelled the conceptus within 48 hours. Thus, 79.2% of all women aborted while being monitored at the center. The overall success rate was 98.7% . The leading side effects in both studies in order of frequency were uterine cramps and nausea, vomiting, and diarrhea. These results showed that oral administration of misoprostol is as effective and well tolerated as other prostaglandins administered parenterally or vaginally.
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PMID:Early termination of pregnancy with mifepristone (RU 486) and the orally active prostaglandin misoprostol. 847 94

As a potent antagonist of glucocorticoid and progesterone receptors, mifepristone (RU-486) has potential use in the treatment of Cushing's syndrome. Initial research in this area has demonstrated that RU-486 acts as an anti-glucocorticoid by antagonizing the negative feedback on the pituitary of endogenous and exogenous glucocorticoids. Since 1985, the literature has reported four studies of the feasibility of RU-486 treatment in Cushing's syndrome patients. In the largest of these studies, 11 patients with inoperable adrenal cancer or ectopic adrenocorticotrophic hormone-secreting neoplasms received 5-22 mg/kg/day of RU-486 for 1-12 months. In seven of these patients, treatment resulted in marked improvement in the Cushingoid phenotype, psychiatric status, hypertension, and carbohydrate intolerance. Three patients discontinued RU-486 because of clinical manifestations of adrenal insufficiency. The most common side effect was nausea. Titration of RU-486 dosing remains imprecise due to the lack of an acceptable rapid biochemical measurement to monitor glucocorticoid action. Regrettably, further research in this area has been hindered by the political controversy regarding RU-486's use as an abortifacient agent.
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PMID:Mifepristone: treatment of Cushing's syndrome. 873 15

The antiprogesterone mifepristone (RU-486) and a prostaglandin preparation (misoprostol), in combination, have been documented to be effective for inducing abortion in France, Sweden, and Great Britain. They are effective up to 63 days of gestation with a slightly longer period of bleeding, pain requiring analgesia, diarrhea, and nausea. In Sweden, 70% of abortions are carried out by the use of drugs. In Norway, medically induced abortion has been introduced as an alternative to surgical intervention. The patient takes mifepristone in a hospital under the supervision of health personnel, then 48 hours later the prostaglandin is administered transvaginally in the hospital where the abortion also takes place. About 4 weeks later, a check-up follows with clinical examination and a pregnancy test. The political debate about medical abortion has also flared up in Norway as in many other countries, mainly in connection with the issue of abortion decided by the individual. In 1989 there was a motion introduced in the Parliament to ban medically induced abortion, but it failed to be adopted. The argument that abortion could be used for contraception is not supported, because there was almost the same rate of decline of abortions in Sweden, where this had been used for several years during the period of 1991-94, as in Denmark, Finland, and Norway, where it had not been. From an ethical point of view, abortion should be the simplest and least invasive, and it could also be less stigmatizing in a hospital because of the outpatient status. The better use of resources for other women waiting for operations also advocates this method as does its acceptability to women.
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PMID:[Should antiprogesterone be used in pregnancy termination?]. 948 12

The safety and effectiveness of oral methotrexate and vaginal misoprostol for early abortion were evaluated in a prospective study of 300 women who presented to the Cuidad de la Habana (Havana, Cuba) for termination of a pregnancy of a gestational age of 63 days or less. All women were given 50 mg of methotrexate at study entry and then were randomly allocated to receive 800 mcg of misoprostol either 3, 4, or 5 days later. If abortion did not occur, misoprostol was readministered 48 and 96 hours later. Complete abortion occurred in 273 women (91%); the success rate was 72% (216 cases) after just one dose of misoprostol. There were no significant differences in abortion rates based on the day on which misoprostol was administered. Vaginal bleeding lasted an average of 7.1 +or- 3.8 days, spotting continued for 4.1 +or- 2.5 days, and total bleeding persisted for 11.2 +or- 4.1 days. Side effects for methotrexate included nausea (9.7%), vomiting (6.7%), dizziness (10.3%), fatigue (6.3%), headache (5.3%), and chills (5.3%). For misoprostol, side effects included nausea (23.0%), vomiting (25.3%), diarrhea (51.7%), dizziness (18.3%), headache (18.0%), chills (60.0%), and pelvic pain (97.3%). All signs and symptoms were of low intensity and short duration, however. These results suggest that combined use of methotrexate and misoprostol represents a feasible alternative to the intramuscular use of methotrexate or of antiprogestins and prostaglandin for medical abortion. The efficacy and safety of this new regimen are very close to those of RU-486, but the cost is considerably less.
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PMID:Oral methotrexate and vaginal misoprostol for early abortion. 958 33


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