epostane and Nausea

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.

Topics: Abortifacient Agents; Abortifacient Agents, Steroidal; Androstenols; Chorionic Gonadotropin; Clinical Trials as Topic; Contraceptives, Oral, Synthetic; Female; Humans; Nausea; Pregnancy; Progesterone

The role of epostane (Sterling Winthrop, Guildford, UK), a competitive inhibitor of the 3 beta hydroxysteroid dehydrogenase enzyme system (3 beta-HSD), as an abortifacient agent in early human pregnancy has been studied in 54 women. All were less than 49 days from their last menstrual period. Thirty were treated with 200 mg of epostane every 8 h for 7 days and 24 were given 200 mg every 6 h for 7 days. This caused a sustained reduction in circulating progesterone concentrations, a smaller fall in 17 beta-oestradiol and no effect on serum cortisol. Abortion occurred in 21 women (70%) in the lower dosage group and in 20 women (87%) in the higher dosage group. Abortion was incomplete in 6 of these 41 women. A worsening of pregnancy nausea and vomiting was noted by 66% of women in the first group and 84% in the second. There was no delay in the resumption of normal menstruation following abortion. This study confirms the potential of epostane as an effective inhibitor of ovarian and placental steroidogenesis and as a potent abortifacient agent in early human pregnancy.. 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.

Topics: Abortifacient Agents; Abortifacient Agents, Steroidal; Abortion, Incomplete; Abortion, Induced; Adult; Androstenols; Consumer Behavior; Dose-Response Relationship, Drug; Estradiol; Female; Humans; Hydrocortisone; Nausea; Pregnancy; Pregnancy Trimester, First; Progesterone; Time Factors; Uterine Hemorrhage

Fifty-six healthy women, with a gestational length of less than 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 seven days. Physical examination, routine laboratory screening and determination of hCG, progesterone, estradiol and cortisol was performed on days 0, 7 and 14. The treatment resulted in 84% complete abortions (90% among women completing therapy). Two 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.. 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.

Topics: Abdomen; Abortion, Induced; Adult; Androstenols; Chorionic Gonadotropin; Estradiol; Female; Humans; Hydrocortisone; Nausea; Pain; Pregnancy; Progesterone; Uterine Hemorrhage; Vomiting