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)

54 healthy women 17-41 years of age participated in a study to investigate the role of epostane as an abortifacient in early pregnancy. Epostane is a competitive inhibitor of the 3-beta hydroxysteroid dehydrogenase enzyme system. 30 subjects were treated with 200 mg of epostane every 8 hours for 7 days, while the remaining 24 subjects received 200 mg every 6 hours for 7 days. All subjects were less than 49 days from their last menstrual period. In the 1st group (600 mg of epostane/day), 21 of the 30 women (70%) aborted and the abortion was complete in 17 (80%) of these women. In the 2nd group (800 mg of epostane/day), 20 of 23 patients (87%) aborted and abortion was complete in 148 (90%). 66% of the women in the 600 mg/day regimen complained of side effects, largely a worsening of pregnancy nausea, while side-effects were experienced by 87% of those in the higher-dose group. Nausea and vomiting were successfully reduced, however, by administration of an oral antiemetic. Serum progesterone concentrations fell after the beginning of epostane treatment to 5% of pretreatment values and remained low for the duration of the treatment. There was a smaller fall in estradiol values and no effect on serum cortisol. Hematology and biochemistry measurements remained within the normal range after treatment with epostane. The higher abortion rate recorded in the higher-dose group may be a dose-response effect; alternatively, it may be due to a more constant inhibition of the hydroxysteroid dehydrogenase enzyme system. Overall, this study confirms the potential of epostane as an effective inhibitor of ovarian and placental steroidogenesis and as a potent abortifacient agent in early pregnancy.
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PMID:Induction of abortion in early first trimester human pregnancy using epostane. 271 92

Epostane is a steroid which inhibits the synthesis of progesterone by inhibiting the enzyme 3-beta-hydroxysteroid dehydrogenase. Progesterone is produced during early pregnancy by the corpus luteum, but after the 7th week, production of progesterone is taken over by the placenta, which also secretes human chorionic gonadotropin. In a clinical trial 50 patients in early (5-8 weeks) pregnancy were given 800 mg of Epostane for 7 days. 84% aborted, including 90% of primigravidas and 76% of multigravidas. Side effects were mild and included nausea, cramps, and vaginal bleeding. In the 16% of patients who did not respond to Epostane there was an increase in cortisol levels. Since cortisol induces human chorionic gonadotropin synthesis and this increases the activity of 3-beta-hydroxysteroid dehydrogenase, it is evident that the nonresponders required a larger dose of Epostane to suppress progesterone synthesis. Epostane is thus a candidate for a "morning after" method to terminate early pregnancy and induce labor.
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PMID:Antiprogestins. 304 93

RU-486 (or mifepristone developed by Roussel-Uclaf, France) is an antiprogesterone drug. Similar compounds have been introduced by Schering AG, Germany: ZK 98.734 and ZK 98.299. Epostane (Sterling- Winthrop, UK) is a progesterone synthesis inhibitor blocking the 3- beta-hydroxysteroid dehydrogenase enzyme system. In a WHO study 37 women at amenorrhea of 42 days or less were given 25, 50 or 100 mg mifepristone twice/day for 4 days: 22 patients had a complete abortion and 11 had an incomplete abortion. Success rate varied between 82.4% and 88.5% with a daily dose of 100 or 150 mg; 83% with 100 or 200 mg daily; and complete abortion occurred in 39% with 200 mg. 400 mg daily for 2 days produced complete abortion in 85%. 200 mg epostane 4 times/day for 7 days terminated pregnancy in 73%. 30 mg of ZK 98.734 given sc for 2 days induced complete abortion in guinea-pigs vs. 7 of 9 and 4 of 9 animals with equal doses of ZK 98.299 and mifepristone, respectively. Sequential therapy with 25 mg mifepristone twice/day produced regular uterine contractions. In administration of sulprostone (16-phenoxy-tetranor PGE2 methyl sulphonylamide); 1 mg of gemeprost (16, 16-dimethyl-trans-delta2-PGE1 methyl ester) given vaginally after mifepristone treatment; and vaginal administration of 10 mg PGE2 following 300-600 mg epostane daily for 5 days showed similar effects. In a clinical trial 25 mg mifepristone twice/day for 4 days followed by .25 mg sulprostone in injection led to complete abortion in 32 (94%) of 34 patients. All 5 women treated with 300, 400 or 600 mg doses of epostane and PGE2 daily for 5 days had abortion. Bleeding lasted 1-2 weeks in successful cases after mifepristone with blood loss of 87 +or- 9 ml and excessive bleeding in 0-5.6% of cases. Side effects were mild. Nausea occurred more often with 800 mg/day epostane than with 50 or 100 mg mifepristone. In a recent study 20 patients with 16-18 weeks of pregnancy were given 200 mg mifepristone before extra-amniotic infusion of PGE2, and the time needed to induce abortion and the total PGE2 dose required was reduced significantly.
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PMID:Anti-progesterones for the interruption of pregnancy. 306 65

56 healthy women, with a gestational length of 49 days from the last menstrual period, who requested termination of pregnancy were treated with Epostane, a progesterone synthesis inhibitor. Epostane, which competitively inhibits the 3 beta-hydroxy steroid dehydrogenase enzyme system, was given in the dose 200 mg x 4 for 7 days. Physical examination, routine laboratory screening, and determination of hCG, progesterone, estriadol, and cortisol were performed on days 0, 7, and 14. The treatment resulted in 84% complete abortions (90% among women completing therapy). 2 women experienced vaginal bleeding only, while 7 were non-responders. Among subjective side effects nausea dominated totally and was also the reason for discontinuation in 4 cases. The average length of bleeding among women with complete abortions was 10.7 days and the decrease in hemoglobin and hematocrit was very slight. Routine laboratory values remained within the normal range. Cortisol levels were elevated on day 7 compared to days 0 and 14, but all single values were within the normal limits.
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PMID:Termination of early human pregnancy with epostane. 359 38

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