去氧孕烯/孕二烯酮避孕药有致静脉血栓栓塞危险

EMEA药品专利委员会(CPMP)依据1995年～2001年9月的资料,公布了关于所谓“第三代”复方口服避孕药(COC,含孕激素去氧孕烯desogestrel或孕二烯酮gestodene)与诱发静脉血栓栓塞(VTE)危险性关联的评价结果,结论如下:服用含去氧孕烯或孕二烯酮的口服避孕药(与含左炔诺孕酮的避孕药比较,相对危险度是1.5～2.0)出现VTE的危险性有所增加,特别是在开始服用复方口服避     

复方口服避孕药在妇科疾病治疗中的应用

复方口服避孕药的活性成分为雌激素(主要是炔雌醇)和孕激素,通过抑制垂体促性腺激素的周期性合成和释放,进而抑制卵巢内卵泡的发育、成熟和排卵,最终起到避孕作用.复方口服避孕药中的孕激素成分有所不同,在妇科内分泌失调性疾病中的作用亦不同.本文综述复方口服避孕药这一特殊的雌、孕激素联合疗法在功能失调性子宫出血、原发性痛经、子宫...     

避孕药的多样化选择

由女性使用的甾体避孕药,主要为人工合成的雌激素、孕激素。采用合成的甾体激素作为口服避孕药已有30余年的历史,如前所述,1956年美国平卡斯等人首次合成异炔诺酮并进行了临床试验。1960年美国食品药物管理局批准的第一种口服避孕药异炔诺酮-10是含有雌激素的复方制剂。由于口服避孕药效果满意,很快在世界范围推广使用,至80年代,估计约有6000万妇女采用口服避孕药。     

复方短效口服避孕药的非避孕作用临床应用及体会

复方短效口服避孕药主要是由人工合成的甾体避孕药,是雌孕激素配伍合成的,少数是单纯孕激素制剂,避孕效果已得到证实。但目前将其用于与避孕无关的其他妇科疾病的治疗也取得了较好疗效,现将其临床应用与体会报道如下。     

新药

新剂型拜耳含叶酸避孕药Beyaz获批近日,拜耳公司复方避孕药Beyaz获美国FDA批准上市。该药物是雌激素（戊酸雌二醇）和孕激素（地诺孕素）及叶酸（添加左甲基四氢叶酸钙0.451mg）的复方药物。     

口服避孕药治疗青春期功能失调性子宫出血的效果分析

目的探讨口服避孕药治疗青春期功能失调性子宫出血(功血)的止血效果。方法回顾性分析我院诊治的62例青春期功能失调性子宫出血患者临床资料。根据用药的不同分为3组:雌激素组(21例)、孕激素组(19例)及口服避孕药组(22例)。对3组控制出血时间、完全止血时间、不良反应、减量后出血情况进行记录和评价。结果口服避孕药组、孕激素组控制出血时间和完全止血时间低于雌激素组,口服避孕药组不良反应及减量后出血少于雌、孕激素两组。口服避孕药组内去氧孕烯炔雌醇与炔雌醇醋酸环丙孕酮疗效相近,差异无统计学意义。结论在青春期功能失调性子宫出血止血效果方面,口服避孕药优于雌激素、孕激素。     

长效注射避孕药

概述 Siegel于1963年首先报道用孕激素缓慢释放注射剂作为女用避孕药,单用己酸孕酮或与戊酸雌醇合用。目前,注射避孕药仍限于使用甾体激素,即单独孕激素或孕激素与雌激素的复方。其作用类似于口服避孕药,     

复方口服避孕药与血脂异常

复方口服避孕药(COC)为最常用的避孕制剂,其含有2种性激素:孕激素和雌激素.COC 可致心血管疾病.流行病调查显示COC引起的心血管疾病与血脂异常有关.其机制尚不完全清楚;三酰甘油水平的升高可能与肝脏分解脂肪和清除三酰甘油能力降低及血液中胰岛素水平增高有关.育龄期妇女长期使用时应尽可能交替使用不同种类的COC,用药期间进行血脂监测.     

地诺孕素药学特性及其临床应用前景

<正> 孕激素是一类重要的化学药物,临床应用广泛且具不可替代性(表1)。孕激素依来源与结构大体分为三类,即:17α—羟基黄体酮及其它们的合成衍生物和19—失碳孕激素,其中后者因发现了普美孕酮(promegestone)、诺美孕醇(nomegestrol)、曲美孕酮(trimegestone)等所谓“混合孕激素”,现似已有再次形成一孕激素研究与开发“热”的趋势。所谓“混合孕激素”是指这些孕激素同时具有天然和合成孕激素的药理学优点,它已随着其第一个药物地诺孕素(dienogestril,17α—氰甲基—17β—羟基—4,9—雌甾二烯—3—酮。图1)的上市而正式走上了临床。本文介绍地诺孕素的药学特性及其临床应用潜力。     

加拿大批准地诺孕素片剂Visanne治疗子宫内膜异位相关骨盆疼痛

2011年11月,加拿大卫生部批准了Bayer HealthCare公司的地诺孕素(dienogest)2mg片剂Visanne,用于一日1次口服治疗妇女子宫内膜异位相关骨盆疼痛。地诺孕素属第三代孕激素,能经抑制雌二醇(estradiol)     

口服避孕药物的安全性问题及相关应用

以期口服避孕药的主要有效成分为雌激素和孕激素.随着口服避孕药使用的日益增多,其安全性问题也逐渐显露出来.本文综述了不同类型的口服避孕药已经发生和可能存在的不良反应及其机制,对口服避孕药与其它药物相互作用引起的不良反应以及使用注意事项做出阐述,同时评价了口服避孕药可能产生的非避孕益处.     

Evolution of the Hungarian oral contraceptives]

Author gives a review of the development of Hungarian oral contraceptives from the beginning to the present status. He describes the three main historical phases that means the high-dose combined pills, the low-dose compositions and the most modern two- and three-phasic preparations. Besides, he mentions the monohormonal mini-pills and the so-called postcoital pill, too. He refers to the fact that the Hungarian pharmaceutical research followed truly the international development in oral contraception, too.     

口服避孕药与静脉血栓栓塞

目前常用的避孕药为复方口服避孕药（COC）,由雌激素和孕激素配伍而成,仅供女性应用。COC可致一些严重不良反应,其中之一为静脉血栓栓塞（venous thromboembolism,VTE）。VTE一般发生在COC开始使用1~2年内,但不受使用持续时间的影响,停药后VTE消失。服用COC者发生VTE的风险约为未服用者的4倍。VTE的发生与COC中雌激素含量和孕激素类型有关。COC制剂中雌激素含量〈50μg时VTE发生率明显降低;第3代COC致VTE风险通常高于第2代COC。COC引致VTE的机制可能是与其所含雌激素促进纤维蛋白原活化、增高凝血因子水平、降低抗凝血酶原水平和增强凝血功能有关。COC致VTE的危险因素有心血管疾病、高龄、嗜烟、有VTE病史和（或）家族史及长期卧床。育龄期女性在服用COC前应进行危险因素筛查,以降低发生VTE的风险。     

Interactions between oral contraceptives and antifungals/antibacterials. Is contraceptive failure the result?

The effectiveness of oral contraceptives may be impaired by concomitant treatment with antimicrobials. This may occur because of reductions in plasma concentrations of ethinylestradiol by the induction of hepatic metabolism, as for rifampicin (rifampin) and possibly griseofulvin, or in a small percentage of women because of interference with enterohepatic recirculation. There are no scientific data to support the anecdotal evidence that the concomitant use of combined oral contraceptives and antimicrobials reduces contraceptive efficacy in the majority of women. It has been postulated that there is a subset of women in whom the enterohepatic recirculation of ethinylestradiol plays an important role. In these women the action of an antimicrobial may reduce the efficacy of oral contraceptives by interfering with this mechanism. Studies that have quantitatively examined these effects may have failed to include women from this subset because of the small numbers involved in the studies. On the other hand, there are no good prospective studies comparing contraceptive failure rates between compliant women who use combined oral contraceptives with and without antimicrobials. All women using combined oral contraceptives should be informed of the very low level of risk of interactions with antimicrobials (probably about 1%) and that it is not possible to identify who may be at risk. Women concerned about this low level of risk should be given information about the use of barrier methods or avoidance of intercourse during the first 7 days of concomitant antimicrobial therapy and for 7 subsequent days. Women who have had previous contraceptive failures or developed breakthrough bleeding during concomitant antimicrobial use should be strongly advised to follow these precautions, as they may be part of the subset of women at higher risk of contraceptive failure.     

Disposition of serum steroids in response to combined oral contraceptives and menstrual cycle phases: A double-blind,randomized, placebo-controlled study

To analyze doping control samples from female athletes demands understanding of non-doping factors that affect the steroid profile. These could be physiological factors such as exercise, alcohol consumption, hormonal changes during the menstrual cycle, or the effect of commonly used approved drugs like combined oral contraceptives. Urine samples have been the main way of doping testing, but serum samples are proposed as a complement. Testosterone, dihydrotestosterone, or the ratio of testosterone and androstenedione has been proposed as a biomarker for testosterone doping because it increases after transdermal testosterone administration. In this double-blind, randomized, placebo-controlled study of 340 healthy females, we analyzed the serum steroid levels, including glucuronide metabolites, before and after 3 months of combined oral contraceptives or placebo. At follow up, sample collection in the placebo group was randomly distributed between different menstrual cycle phases. This enabled to analyze changes in concentrations between the follicular, ovulation, and luteal phases. Combined oral contraceptives decreased all serum steroids including the glucuronide metabolites. As expected, serum testosterone levels increased during the ovulation phase, and also androstenedione and androstenediol, whereas the glucuronide metabolites remained unaffected. Neither combined oral contraceptives nor menstrual cycle phases did affect the ratio of testosterone and androstenedione in serum, and consequently this ratio seems promising as a marker of doping with endogenous anabolic androgenic steroids in women.     

Drospirenone: a novel progestin

Drospirenone is a novel progestin available in combined oral contraceptives and menopausal hormonal therapy. Similar to its parent compound spirolactone, an analog of spironolactone, drospirenone has antimineralocorticoid and antiandrogenic activity. Combined with ethinyl estradiol in oral contraceptive formulations, drospirenone-containing contraceptives have similar efficacy and safety profiles to other low-dose oral contraceptives, but seem to offer improved tolerability with regard to weight gain, mood changes, acne and treatment of a severe form of premenstrual syndrome called premenstrual dysphoric disorder. Combined with estradiol as a continuous hormone therapy regimen, the compound was shown to reduce vasomotor symptoms, maintain bone mass, have a beneficial effect on body weight and, more importantly, was shown to lower blood pressure in postmenopausal women.     

Drospirenone: high risk of venous thrombosis

Oral contraceptives increase the risk of venous thrombosis, with the extent depending on the dose of ethinylestradiol and the type of progestin: the risk is about 20 cases per 100,000 woman-years with norethisterone or levonorgestrel and less than 50 microgrammes of ethinylestradiol, and 30 to 40 cases per 100,000 woman-years with gestodene or desogestrel. Since the beginning of this decade, some oral contraceptives have combined ethinylestradiol with drospirenone, a spironolactone-derived progestin with antimineralocorticoid activity, which carries a risk of hyperkalaemia. A Danish cohort study was based on a registry containing 3.3 million woman-years of data on oral contraceptives, including more than 130,000 woman-years of drospirenone exposure. Compared with levonorgestrel, a statistically significant increase in the risk of venous thrombosis was observed in women using drospirenone (relative risk 1.64, 95% confidence interval 1.27-2.10). A case-control study conducted in the Netherlands that included 1524 patients and 1760 controls showed a statistically significant 6-fold increase in the risk of thrombosis among women using combinations containing drospirenone compared to women who did not use oral contraception, and a non-significant 1.7-fold increase compared to women using combinations based on levonorgestrel. In practice, the first-choice combined oral contraceptives are those containing ethinylestradiol plus either levonorgestrel or norethisterone.     

Drospirenone: a novel progestin

Drospirenone is a novel progestin available in combined oral contraceptives and menopausal hormonal therapy. Similar to its parent compound spirolactone, an analog of spironolactone, drospirenone has antimineralocorticoid and antiandrogenic activity. Combined with ethinyl estradiol in oral contraceptive formulations, drospirenone-containing contraceptives have similar efficacy and safety profiles to other low-dose oral contraceptives, but seem to offer improved tolerability with regard to weight gain, mood changes, acne and treatment of a severe form of premenstrual syndrome called premenstrual dysphoric disorder. Combined with estradiol as a continuous hormone therapy regimen, the compound was shown to reduce vasomotor symptoms, maintain bone mass, have a beneficial effect on body weight and, more importantly, was shown to lower blood pressure in postmenopausal women.     

Economic analysis of long-term reversible contraceptives. Focus on Implanon

OBJECTIVE: To examine the economic impact of a new implantable contraceptive, Implanon, in comparison with other available contraceptive methods. DESIGN: This was a modelling study using cost data derived from national published sources and effectiveness data from either controlled clinical trials (Implanon) or reports in the literature (other contraceptives). In the baseline analysis, Implanon was compared with 2 long term reversible contraceptives, Norplant and Mirena. Further analyses were then carried out comparing Implanon with Depo-Provera and with combined oral contraceptives. SETTING: The study concentrated on the UK, but also made reference to several other European countries. MAIN OUTCOME MEASURES AND RESULTS: The baseline analysis showed that all 3 long term reversible contraceptives produce very good rates of return, with Implanon providing the best rate of return (both average and internal) of the 3 methods. The payback period for Implanon was calculated as 146 days, compared with 339 and 368 days for Norplant and Mirena, respectively. In terms of cost effectiveness, the cost per protected year for Implanon was 95 Pounds, compared with 146 Pounds and 168 Pounds for Norplant and Mirena, respectively. In comparison with Depo-Provera (an injectable contraceptive), Implanon was both less costly and more effective, the cost per protected year for Depo-Provera being 131 Pounds. The threshold beyond which Implanon delivers cost savings compared with combined oral contraceptives was at a failure rate of 4.9% for the combined pill. CONCLUSIONS: Reversible long term approaches to contraception provide an effective and efficient use of healthcare resources and generate an excellent return on public investment. Implanon produces better rates of return than both Norplant and Mirena, and is also more cost effective in terms of cost per pregnancy avoided and cost per protected year than Norplant, Mirena, Depo-Provera and oral contraceptives.     

雌孕激素复合剂、雌激素及孕激素三种方法治疗青春期功能失调性子宫出血的疗效比较

目的探讨简单、有效的治疗青春期功能失调性子宫出血的止血方法。方法100例青春期功血患者随机分为三组：雌孕激素复合组（妈富隆）、雌激素组、孕激素组。比较各组的出血控制时间及出血停止时间。结果雌孕激素复合剂组的出血控制和出血停止时间均明显小于雌激素组和孕激素组,差异有显著性意义（P〈0．05）,而雌激素组和孕激素组两组间的出血控制和出血停止时间比较,差异则无显著性意义（P〉0．05）。结论雌孕激素复合剂（妈富隆）治疗青春期功能失调性子宫出血,方法简单、经济、疗效确切。