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PLASMA-LEVELS OF PROGESTERONE AND ESTROGENS IN WOMEN TREATED WITH AN ORAL-CONTRACEPTIVE OF LOW ESTROGEN CONTENT (OVOSTAT-1375)

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ACTA OBSTETRICIA ET GYNECOLOGICA SCANDINAVICA 1975年第3期54卷 217-221页

作者： JOHANSSON, EDB UNIV HOSP UPPSALA DEPT OBSTET & GYNAECOL75014 UPPSALASWEDEN

The plasma levels of progesterone and oestrogens were measured during treatment with an oral contraceptive containing 37.5 mug of ethinyl oestradiol and 1 mg of lynestrenol (= 3-desoxy-17alpha-ethinyl-19-nortestosterone) (Ovostat 1375, Organon, Oss, Holland). Blood samples were taken every day during 9 complete cycles in 5 healthy women. The plasma levels of progesterone were in the range of those found during the early follicular phase of the normal women. No ovulation seemed to have occurred. The mean plasma levels of oestrogens (oestradiol and oestrone) during treatment were below those found during early follicular phase of 34 normal cycles although overlapping of values occurred. The ratio between oestradiol and oestrone during treatment was 1:2 vs. 1:1 during the early follicular phase of the normal cycles. In two cycles treatment was started during the midcyclic rise of oestrogens. No rise of progesterone indicating corpus luteum formation was found. Despite the low amount of oestrogen in the drug the ovaries appeared to secrete minimal amounts of sex steroids. The lynestrenol content is likely to be partly responsible for the inhibition of ovulation and the additional suppression of steroidogenesis.

关键词：抑制化学性雌二醇/血液雌激素类/血液雌酮/血液炔雌醇/投药和剂量利奈孕醇/投药和剂量月经/药物作用卵巢/药物作用孕酮/血液成年人女(雌)性人类

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COMPARATIVE STUDIES OF ETHYNYL ESTROGENS USED IN ORAL-CONTRACEPTIVES .2. ANTIOVULATORY POTENCY

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AMERICAN JOURNAL OF OBSTETRICS AND GYNECOLOGY 1975年第5期122卷 619-624页

作者： GOLDZIEHER, JW DELAPENA, A CHENAULT, CB WOUTERSZ, TB SW FDN RES & EDUC POB 281478848 W COMMERCE STST ANTONIOTX 78284

The occurrence or inhibition of ovulation was inferred from the plasma progestin level measured in the last week of 430 control cycles and of 4,638 cycles from fertile women receiving various antiovulatory steroids, singly and in combination. The substances tested included: mestranol and ethynylestradiol (EE) of homogeneous bioavailability, used alone in a range from 50 to 100 μg per day; these same dose levels combined with various progestins; and finally various proprietary combination and sequential low-dose regimens undergoing clinical trials. Statistical analysis showed ethynylestradiol and mestranol alone to be equipotent over the tested range, although at 50 μg per day superiority of mestranol over EE was suggested. Two preparations of EE at 50 μg per day, one of them a sequential with dimethisterone, showed different potency. At 50 μg per day no estrogen, alone or with a sequential progestin, reached a satisfactory level of effectiveness. However, very small amounts in the range of 20 to 40 μg per day were highly effective when combined with quantities of various 19-nor progestins which by themselves are well below the antiovulatory level. This indicates that a synergism exists between these two classes of compounds insofar as their antiovulatory effect is concerned, thus explaining the high contraceptive effectiveness observed with very-low-dose combination regimens.

关键词：避孕药口服/药理学避孕药口服合成/药理学抑制化学性剂量效应关系药物复方合剂药物协同作用炔雌醇/投药和剂量炔雌醇/药理学宫内避孕器月经美雌醇/投药和剂量美雌醇/药理学排卵/药物作用孕酮/血液成年人女(雌)性人类妊娠

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Treatment of chronic bleeding from gastric antral vascular ectasia (GAVE) with estrogen-progesterone in cirrhotic patients: An open pilot study

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AMERICAN JOURNAL OF GASTROENTEROLOGY 1999年第10期94卷 2909-2911页

作者： Tran, A Villeneuve, JP Bilodeau, M Willems, B Marleau, D Fenyves, D Parent, R Pomier-Layrargues, G Hop St Luc Liver Unit Montreal PQ Canada Hop St Luc Internal Med Unit Montreal PQ Canada

OBJECTIVE: Gastric antral vascular ectasia (GAVE) is a rare cause of chronic bleeding in cirrhotic patients. Treatment of GAVE with surgical or nonsurgical portal decompression, P-blockers, or endoscopic therapy provides disappointing results. In the present study, we evaluated the efficacy of estrogen-progesterone therapy, which has been reported to control chronic bleeding in gastrointestinal vascular malformations, such as Osler-Weber Rendu disease or angiodysplasia, in GAVE-related chronic bleeding. METHODS: Six cirrhotic patients who bled chronically from GAVE were included. Three had alcoholic cirrhosis, two cryptogenic cirrhosis, and one primary biliary cirrhosis. Grade 1 esophageal varices were noted in four patients. Bleeding could not be controlled by P-blockers, and endoscopic therapy was not considered given the extension of the antral vascular lesions. RESULTS: Before the start of therapy, transfusion requirements averaged 3.5 units/month over a 1.5-11 month period of observation. Patients were then treated with a combination of ethynil estradiol 30 mu g and noretisterone 1.5 mg daily. During follow-up (range 3-12 months), bleeding did not recur in four patients;in one patient, treatment with estrogen progesterone decreased the need for transfusions from 4 units/month to 1.4 unit/month;this patient stopped the treatment inadvertently after 6 months and severe anemia recurred with a need for 4 units of blood in the following month;reintroduction of the treatment resulted in an increase of hemoglobin levels without the need for blood transfusions during the following 4 months. In the last patient, a 5-month treatment did not improve chronic bleeding. CONCLUSIONS: The present study suggests that estrogen-progesterone therapy is useful in the treatment of chronic bleeding related to GAVE;however, these findings require confirmation by a controlled trial. (C) 1999 by Am. Cell. of Gastroenterology.

关键词：慢性病药物评价药物疗法联合雌二醇同源物/投药和剂量炔雌醇/投药和剂量胃窦血管扩张/并发症胃肠出血/药物疗法肝硬化/并发症炔诺酮/投药和剂量炔诺酮/类似物和衍生物试点项目孕酮同源物/投药和剂量复发老年人老年人 80以上人类中年人

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不同减痛方法用于绝经后妇女取出宫内节育器的临床观察

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医学临床研究 2014年第9期31卷 1814-1815页

作者：张小琳刘婷朱慧琴湖北省宜昌市夷陵区计划生育服务站湖北宜昌443100

[目的]观察炔雌醇联合宫术宁胶棒在绝经后妇女取出宫内节育器（IUD）时的应用效果.[方法]选取因绝经要求取出节育器的妇女126例根据不同的减痛方法分为三组：A组术前在宫颈管放置宫术宁胶棒5～10min;B组术前1周口服炔雌醇0.35 mg/d;C组... 详细信息

[目的]观察炔雌醇联合宫术宁胶棒在绝经后妇女取出宫内节育器（IUD）时的应用效果.[方法]选取因绝经要求取出节育器的妇女126例根据不同的减痛方法分为三组：A组术前在宫颈管放置宫术宁胶棒5～10min;B组术前1周口服炔雌醇0.35 mg/d;C组采用炔雌醇联合宫术宁胶棒.比较三组的宫颈软化情况、术中疼痛程度及取器成功率.[结果]C组的宫颈软化程度最佳,显著优于A、B两组（P＜0.01）,但A组与B组比较无统计学差异（P＞0.05）;A手术时间为（5.23±1.27） min,明显长于B、C（2.64±0.93、2.13±0.76）min（P＜0.05）;三组的疼痛程度由大到小为A组,B组,C组;C组顺利取出IUD百分率最高,显著高于A、B组（P＜0.05）.[结论]炔雌醇联合宫术宁胶棒应用于绝经后妇女取出IUD,软化宫颈,提高取出IUD的成功率,减轻患者痛苦.

关键词：绝经后期宫内避孕器排出炔雌醇/投药和剂量镇痛/方法

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Low-dose contraceptive estrogen-progestin and coronary artery atherosclerosis of monkeys

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OBSTETRICS AND GYNECOLOGY 2000年第2期96卷 250-255页

作者： Adams, MR Anthony, MS Manning, JM Golden, DL Parks, JS Wake Forest Univ Sch Med Dept Pathol Comparat Med Winston Salem NC 27157 USA William Paterson Univ Dept Exercise & Movement Sci Wayne NJ USA

Objective: To determine the separate and combined effects of the estrogen and progestin components of a modern triphasic oral contraceptive (OC) formulation on extent of coronary artery atherosclerosis. Methods: Female cynomolgus monkeys (n = 81) were fed atherogenic diets for 32 months. After the first 7 months, they were randomized to four groups and treated triphasically for 21 of each 28 days with ethinyl estradiol (E2) (monkey equivalent of 30-40 pg), levonorgestrel (monkey equivalent of 50-125 mu g), a combination of the two steroids, or placebo. Results: Treatment with estrogen alone reduced coronary artery atherosclerosis extent 67% compared with untreated controls (P < .05). Treatment with progestin alone had no effect (P > .20). While atherosclerosis extent in monkeys treated with the combined OC was reduced 28%, this did not differ statistically from the other groups (P > .20). Conclusion: In doses used for oral contraception, E2, like all other estrogens studied to date, has a marked inhibitory effect on atherosclerosis progression. Levonorgestrel, at doses used in modern OC formulations, antagonizes this effect. When considered with other experimental evidence, these findings support the concept that progestins used in OCs and hormone replacement therapy can antagonize estrogen's atheroinhibitory effects. Whether this occurs seems to depend on a relative balance between estrogen and progestin with respect to dose, potency, route, and pattern of administration. However, when considered with evidence from previous studies, the findings also indicate a modest atheroinhibitory influence of combination (estrogen-progestin) OCs. ((C) 2000 by The American College of Obstetricians and Gynecologists.).

关键词：避孕药口服复合/投药和剂量避孕药口服复合/治疗应用冠状动脉疾病/预防和控制疾病模型动物用药计划表雌二醇同源物/投药和剂量雌二醇同源物/治疗应用炔雌醇/投药和剂量炔雌醇/治疗应用左炔诺孕酮/投药和剂量左炔诺孕酮/治疗应用脂蛋白类/血液成束猴孕酮同源物/投药和剂量孕酮同源物/治疗应用随机分配动物女(雌)性

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Changes in fat cell size and in vitro lipolytic activity of abdominal and gluteal adipocytes after a one-year cross-sex hormone administration in transsexuals

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METABOLISM-CLINICAL AND EXPERIMENTAL 1999年第11期48卷 1371-1377页

作者： Elbers, JMH de Jong, S Teerlink, T Asscheman, H Seidell, JC Gooren, LJG Free Univ Amsterdam Hosp Dept Endocrinol & Androl Res Inst Endocrinol Reproduct & Metab NL-1007 MB Amsterdam Netherlands Free Univ Amsterdam Hosp Dept Clin Chem Res Inst Endocrinol Reproduct & Metab NL-1007 MB Amsterdam Netherlands

We prospectively studied the effects of cross-sex hormone administration on fat cell size and in vitro lipolytic activity in subcutaneous abdominal and gluteal fat biopsies obtained from 19 male-to-female (M-F) transsexuals and 17 female-to-male (F-M) transsexuals. The amount of subcutaneous fat at the abdominal and gluteal levels was quantified with the use of magnetic resonance imaging (MRI). Before cross-sex hormone administration. M-F transsexuals had less subcutaneous fat with smaller fat cells compared with F-M transsexuals, with a higher baseline in vitro lipolytic activity expressed as glycerol release per milligram of triglyceride (TG) in the abdominal region (P < .05). Before cross-sex hormone treatment, no differences in lipolytic activity stimulated with arterenol (ART), isoproterenol (ISO), or ISO + insulin (INS) were observed between groups or regions. After a 1-year treatment with estrogens and antiandrogens in M-F transsexuals, subcutaneous fat areas on MRI and fat cell size were increased (P < .001) and reductions were observed in the basal lipolytic activity of gluteal and abdominal fat biopsies (P < .05). Following administration of testosterone to F-M transsexuals, subcutaneous fat and fat cell size at the gluteal and abdominal depots were decreased (P < .01) and basal lipolysis was increased significantly at the abdominal level (P < .05) but not at the gluteal level. In both M-F and F-M transsexuals, no effect of sex hormone administration was observed on stimulated lipolytic activities;In conclusion, regional sex differences in the amount of subcutaneous fat, adipocyte size, and in vitro basal lipolytic activity were demonstrated that could be largely reversed by cross-sex hormone treatment in adult subjects, providing evidence for their dependence on the sex steroid milieu. Copyright (C) 1999 by W.B. Saunders Company.

关键词：腹部脂细胞/代谢臀用药计划表雌二醇同源物/投药和剂量雌二醇同源物/药理学炔雌醇/投药和剂量炔雌醇/药理学性腺甾类激素/投药和剂量性腺甾类激素/药理学脂类代谢磁共振成像前瞻性研究睾酮/投药和剂量睾酮/药理学易性转化癖/代谢成年人女(雌)性人类男(雄)性

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Oral ethinyl estradiol, but not transdermal 17β-estradiol, increases plasma C-reactive protein levels in men

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THROMBOSIS AND HAEMOSTASIS 2000年第2期84卷 359-360页

作者： Giltay, EJ Gooren, LJG Emeis, JJ Kooistra, T Stehouwer, CDA Free Univ Amsterdam Hosp Dept Internal Med NL-1007 MB Amsterdam Netherlands Free Univ Amsterdam Hosp Res Inst Endocrinol Reprod & Metab NL-1007 MB Amsterdam Netherlands TNO PG Gaubius Lab Leiden Netherlands

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Effects of exogenous steroids on gonadotrophin secretion

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Clinics in Obstetrics and Gynaecology 1976年第3期3卷 579-590页

作者： Johansson, E.D.B. Sweden

Oestrogens inhibit ovulation by negative feedback on FSH and to a lesser extent on LH secretion, thereby hampering the development of follicles. Due to the rapid conversion to oestrone, it is necessary to administer large doses of oestradiol in order to inhibit FSH secretion. The positive feedback of oestrogen, which induces an LH peak at a critical level of oestrogens, may also inhibit ovulation by luteinising the available follicles before they reach maturation and ovulation. The gestagens inhibit ovulation mainly by blocking the positive feedback of oestradiol. When high doses are given the development of follicles is also inhibited. When ethinyl oestradiol is given together with a gestagen, as in combined oral contraceptives, a very reliable drug for ovulation inhibition is formed, due to its dual action. Both the development of follicles and the positive feedback of oestrogens are blocked.

关键词：避孕药口服/药理学避孕药口服复合避孕药口服序贯雌二醇/投药和剂量雌二醇/血液炔雌醇/投药和剂量炔雌醇/药理学反馈卵泡刺激素/血液卵泡刺激素/分泌性腺甾类激素/药理学黄体期/药物作用促黄体激素/血液促黄体激素/分泌卵泡/药物作用排卵/药物作用催乳素/血液甾类/药理学成年人女(雌)性人类妊娠

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