• 【含去氧孕烯和孕酮的口服避孕药与含左炔诺孕酮的口服避孕药对止血变量的影响: 综述。】 复制标题 收藏 收藏
    DOI:10.1053/ob.1998.v179.a92633 复制DOI
    作者列表:Winkler UH
    BACKGROUND & AIMS: In some studies third-generation oral contraceptives have been reported to be associated with a higher risk of venous thromboembolism than are second-generation oral contraceptives, whereas recent, more refined studies have not confirmed this. The reasons for the alleged differences are under discussion, and differential effects on hemostasis have been proposed. Eighteen studies comparing second- and third-generation oral contraceptives with respect to their effects on hemostasis were analyzed. Significant changes from baseline were reported for many variables with both second- and third-generation oral contraceptives without significant between-group differences. Also, in a combined analysis of nonsignificant changes, no consistent pattern of change emerged for any marker, with the exception of higher factor VII levels associated with third-generation oral contraceptives. However, factor VII is not related to venous thromboembolism risk. In addition, 1 cross-sectional study with an unvalidated assay reported a higher ratio of activated protein C sensitivity with third-generation oral contraceptives. Only 2 components of the hemostatic system (factor VII and activated protein C sensitivity ratio) emerged as potentially differentially affected by second- and third-generation oral contraceptives; the association with venous thromboembolism risk is questionable in the former case and unknown in the latter.

    The initial finding of an increased risk of venous thromboembolism in users of third-generation oral contraceptives (OCs) has not been confirmed in recent, more methodologically refined studies. This article reviews 17 prospective studies with healthy volunteers and one cross-sectional study that compared second- and third-generation OCs in terms of their effects on markers of hemostasis. Significant changes from baseline were reported for many variables with both second- and third-generation OCs. For example, activated partial prothrombin clotting time, protein S, and tissue plasminogen activator and its inhibitor were reduced during OC treatment. However, none of the studies reported statistically significant differences between treatment groups for any of these markers. In a combined analysis of nonsignificant changes, no consistent pattern emerged for any coagulation or fibrinolysis parameter with the exception of higher factor VII levels (not related to venous thromboembolism risk) associated with third-generation formulations. The cross-sectional study with an unvalidated assay found a higher ratio of activated C protein sensitivity with third-generation OCs. Only two components of the hemostatic system--factor VII and activated protein C sensitivity ratio--emerged as potentially differentially affected by second- and third-generation OCs. The association with venous thromboembolism risk is questionable in the former cases and unknown in the latter.

    背景与目标: 在一些研究中,据报道第三代口服避孕药比第二代口服避孕药具有更高的静脉血栓栓塞风险,而最近更精细的研究尚未证实这一点。正在讨论所谓差异的原因,并提出了对止血的不同作用。分析了18项比较第二代和第三代口服避孕药对止血作用的研究。据报道,第二代和第三代口服避孕药的许多变量与基线相比发生了显着变化,而组间没有显着差异。此外,在对非显著变化的综合分析中,除了与第三代口服避孕药相关的较高因子VII水平外,任何标志物都没有出现一致的变化模式。然而,因子VII与静脉血栓栓塞风险无关。此外,一项未经验证的横断面研究报告了第三代口服避孕药对活化蛋白C敏感性的比率更高。止血系统中只有2种成分 (因子VII和活化蛋白C敏感性比) 被第二代和第三代口服避孕药潜在地影响; 在前一种情况下,与静脉血栓栓塞风险的关联值得怀疑,而在后一种情况下则未知。
    在第三代口服避孕药 (OCs) 使用者中,静脉血栓栓塞风险增加的最初发现尚未在最近的方法学上得到证实。本文回顾了17项针对健康志愿者的前瞻性研究,以及一项横断面研究,该研究比较了第二代和第三代oc对止血标志物的影响。据报道,第二代和第三代oc的许多变量均与基线发生了显着变化。例如,在OC治疗期间,活化的部分凝血酶原凝血时间,蛋白质S和组织纤溶酶原激活剂及其抑制剂减少。然而,没有一项研究报告了治疗组之间任何这些标记物的统计学差异。在一项非显著变化的综合分析中,除了与第三代制剂相关的较高因子VII水平 (与静脉血栓栓塞风险无关) 外,任何凝血或纤溶参数均没有出现一致的模式。未经验证的分析的横断面研究发现,第三代oc的活化C蛋白敏感性更高。止血系统中只有两个组成部分-因子VII和活化的蛋白C敏感性比-可能受到第二代和第三代oc的差异影响。前者与静脉血栓栓塞风险的关联值得怀疑,后者则未知。
  • 【两种含炔雌醇和醋酸环丙孕酮或去氧孕烯的口服避孕药对骨量的影响: 为期2年的随访结果。】 复制标题 收藏 收藏
    DOI:10.3109/13625189809051408 复制DOI
    作者列表:Castelo-Branco C,Martínez de Osaba MJ,Pons F,Vanrell JA
    BACKGROUND & AIMS: BACKGROUND:There are conflicting data about the effects of oral contraceptives on bone mass in young women. Moreover, amenorrheic women may also be affected to varying degrees by osteopenia. Both conditions (oral contraceptive use and amenorrhea) are not infrequent in women during their reproductive years.

    AIM:To evaluate the safety for bone mass of two oral contraceptives, one containing cyproterone acetate and the other containing desogestrel.

    METHODS:A total of 67 women between 19 and 29 years of age were studied. Of these women, 35 were selected to receive an oral contraceptive containing 35 mg ethinylestradiol and 2 mg cyproterone acetate. A second group of 32 women received an oral contraceptive containing 30 mg ethinylestradiol and 150 mg desogestrel for 2 years. Immediately before and after the 12th and 24th months of therapy, bone mineral density was assessed by dual X-ray absorptiometry, and hormonal profiles and Ferriman-Gallwey scores were evaluated.

    RESULTS:After the 2-year follow-up, all subjects showed regular cycles, no pregnancies, and no changes in bone mass density. In addition, hirsute subjects showed a decrease of almost 42% in hirsutism scores.

    CONCLUSION:Oral contraceptives containing cyproterone acetate or desogestrel in the studied doses have no deleterious effects on bone marrow.

    背景与目标: 背景 : 关于口服避孕药对年轻女性骨量的影响的数据相互矛盾。此外,闭经妇女也可能受到骨质减少的不同程度影响。两种情况 (口服避孕药和闭经) 在女性生育期间并不少见。
    目的 : 为了评估两种口服避孕药对骨量的安全性,一种含有醋酸环丙孕酮,另一种含有去氧孕烯。
    方法 : 研究了67名19至29岁的女性。在这些妇女中,选择了35名接受口服避孕药,其中含有35 mg炔雌醇和2 mg醋酸环丙孕酮。第二组32名妇女接受含有30 mg炔雌醇和150 mg去氧孕烯的口服避孕药2年。在治疗的第12个月和第24个月之前和之后,通过双重x射线吸收法评估了骨矿物质密度,并评估了激素特征和Ferriman-Gallwey评分。
    结果 : 经过2年的随访,所有受试者均显示出规律的周期,没有怀孕,并且骨密度没有变化。此外,多毛受试者的多毛症评分几乎降低了42%。
    结论 : 研究剂量中含有醋酸环丙孕酮或去氧孕烯的口服避孕药对骨髓没有有害影响。
  • 【口服 (类固醇) 避孕药对低密度脂蛋白受体调节的研究: 去氧孕烯,左炔诺孕酮和乙炔雌二醇在JEG-3细胞系和胎盘组织中。】 复制标题 收藏 收藏
    DOI:10.1016/j.contraception.2007.06.011 复制DOI
    作者列表:Ramakrishnan G,Rana A,Das C,Chandra NC
    BACKGROUND & AIMS: BACKGROUND:The aim of this study was to compare in vitro the role of two oral contraceptives, desogestrel (a less androgenic derivative of levonorgestrel) and levonorgestrel--alone and in combination with ethinyl estradiol--on low-density lipoprotein (LDL) receptor regulation by assessing receptor protein expression and functional effectiveness. STUDY DESIGN:Placental tissue and cultured placental cells (JEG-3) were used to study the expression and endocytotic activity of LDL receptor protein. The expression of the receptor was assessed by immunocytochemistry and immunoblot assays with and without contraceptive challenge. Functioning activity of LDL receptor was studied by measuring the rate of uptake of LDL by placental cells. Quantification of LDL was based on the total cholesterol content of the lipoprotein. RESULTS:A combination of desogestrel (20 ng/mL of incubation medium) and ethinyl estradiol (10 ng/mL of incubation medium) maintained the LDL receptor at high level of expression and functioning mode. In contrast, the double-blind preparation of levonorgestrel (20 ng/mL) and ethinyl estradiol (10 ng/mL) had shown much lower expression as well as receptor-mediated LDL uptake. The concentration of contraceptives used in this study was similar to the prevailing concentration of oral contraceptives in clinical use. CONCLUSION:Higher expression of LDL receptor and enhanced rate of LDL uptake by the receptor protein projects the possibility that there might be less atherosclerosis-related disorders from the combination of desogestrol and ethinyl estradiol.
    背景与目标:
  • 【炔雌醇联合孕二烯酮和去氧孕烯对年轻女性寻常痤疮的临床和激素作用。】 复制标题 收藏 收藏
    DOI:10.1016/0010-7824(96)00005-4 复制DOI
    作者列表:Mango D,Ricci S,Manna P,Miggiano GA,Serra GB
    BACKGROUND & AIMS: The effect of gestodene 75 micrograms (GTD) versus desogestrel 150 micrograms (DSG) combined with 30 micrograms of ethinylestradiol (EE) on acne lesions and plasma androstenedione (A), total testosterone (T), sex hormone binding globulin (SHBG) and "free androgen index" (FAI) was evaluated in an open study on 19 patients aged 18-35 years affected with postpubertal or persistent non-severe acne vulgaris. The patients were randomly allocated into two groups receiving EE-GTD (n = 8) and EE-DSG (n = 11), 21 tablets per cycle for 9 consecutive cycles. Clinical and hormonal evaluations were made between days 17-21 in the cycle before treatment and between days 17-21 of the cycle 3, 6 and 9 of treatment. During treatment, acne improved in most patients, reaching at cycle 9 a low score (absent or minimal) in 62% of the cases in the GTD group (mean acne score = 1.25) and in 90% of the cases in the DSG group (mean acne score = 0.90). Before treatment, about 75% of the patients showed one or more signs of biochemical hyperandrogenism, including elevated FAI (57%), elevated A (15%), elevated total T (15%) and decreased SHBG (21%), and there was evidence of inverse correlation between SHBG and acne scores (p < 0.05). The echogenic texture of the ovaries was multifollicular in 55% of the cases. By the end of the third cycle of treatment, the hormonal changes observed in both groups included significant decreases, with normalization of individual elevated levels of T, and a 3-fold rise of the initial values of plasma SHBG, which showed a further gradual increase at cycle 9 of EE-DSG administration. At cycle 9, normalization of the echogenic ovarian texture was observed. Acne improvement under treatments with estrogen and progestin (EP) could be significantly correlated with the normalization of biochemical hyperandrogenism. In conclusion, the biochemical and clinical efficacy of EE-GTD and EE-DSG indicate that both these preparations can be a good choice in the therapy of acne vulgaris, with a non-significant better clinical result with EE-DSG.

    At the Sacred Heart Catholic University in Rome, Italy, health researchers randomly allocated 19 nulligravidae aged 18-35 with either postpubertal or persistent non-severe acne vulgaris to receive either the combined oral contraceptive (OC) containing 30 mcg ethinyl estradiol (EE) and 75 mcg gestodene (GTD) (Minulet) or 30 mcg EE and 150 mcg desogestrel (DSG) (Marvelon). They aimed to evaluate the effect of GTD and DSG combined with low doses of EE on acne lesions and on hormone levels. The women used the OCs (21 tablets/cycle) for nine consecutive cycles. At baseline, about 75% of all patients had at least one sign of biochemical hyperandrogenism (57% for elevated free androgen index, 15% for elevated androstenedione, 15% for elevated total testosterone, and 21% for reduced sex hormone binding globulin [SHBG]). At baseline, the higher the acne score was, the lower the SHBG level was (p 0.05). The ovaries of 55% of the women had multiple follicles. Acne improved significantly in both groups (mean acne score, 2.9-0.9 for EE/DSG and 2.87-1.25 for EE/GTD; p 0.05). In fact, 62% of cases in the EE/GTD group and 90% of those in the EE/DSG group had either minimal or no acne lesions. Acne improvement during treatment was significantly associated with normalization of biochemical hyperandrogenism. At completion of the third cycle of treatment, both groups experienced significant decreases in hormones. Individual elevated levels of testosterone normalized. The initial values of plasma SHBG had increased 3-fold. SHBG increased gradually to cycle 9 of EE-DSG OC use. At completion of cycle 9, the echogenic ovarian texture returned to normal. These findings suggest that, since both OCs are biochemically and clinically effective, these OCs may be a good treatment for acne vulgaris.

    背景与目标: 孕二烯酮75微克 (GTD) 与去氧孕烯150微克 (DSG) 联合30微克乙炔雌二醇 (EE) 对痤疮皮损及血浆雄烯二酮 (A) 、总睾酮 (T) 、性激素结合球蛋白 (SHBG) 和 “游离雄激素指数” (FAI) 在一项开放研究中评估了19例年龄在18-35岁之间的患有青春期后或持续性非严重寻常痤疮的患者。将患者随机分为两组,分别接受ee-gtd (n = 8) 和ee-dsg (n = 11),每周期21片,连续9个周期。在治疗前周期的第17-21天以及治疗周期的第3、6和9天的第17-21天之间进行了临床和激素评估。在治疗期间,大多数患者的痤疮得到改善,在第9周期,GTD组的62% 病例 (平均痤疮评分 = 1.25) 和DSG组的90% 病例 (平均痤疮评分 = 0.90) 达到低分 (不存在或最小)。治疗前,约75% 的患者表现出一种或多种生化高雄激素血症的迹象,包括FAI升高 (57%),A升高 (15%),总T升高 (15%) 和SHBG降低 (21%),SHBG与痤疮评分呈负相关 (p <0.05)。在55% 情况下,卵巢的回声质地是多卵泡的。到第三个治疗周期结束时,两组中观察到的激素变化均显着降低,个体T水平升高,血浆SHBG初始值升高3倍,这表明在第9周期EE-DSG给药时进一步逐渐增加。在第9周期,观察到回声卵巢质地正常化。雌激素和孕激素 (EP) 治疗下痤疮的改善可能与生化高雄激素血症的正常化显着相关。总之,EE-GTD和EE-DSG的生化和临床疗效表明,这两种制剂都可以作为治疗寻常痤疮的良好选择。EE-DSG的临床效果无明显改善。
    在意大利罗马的圣心天主教大学,健康研究人员随机分配了19例18-35岁患有青春期后或持续性非严重寻常痤疮的nulliravidae,以接受含有30 mcg乙炔雌二醇 (EE) 和75 mcg孕二烯酮 (GTD) (Minulet) 或30 mcg EE和150 mcg去氧孕酮 (DSG) 的联合口服避孕药 (OC) (妈富隆)。他们旨在评估GTD和DSG联合低剂量EE对痤疮病变和激素水平的影响。妇女连续9个周期使用OCs (21片/周期)。在基线时,约75% 的所有患者至少有一个生化高雄激素血症的征象 (57% 游离雄激素指数升高,15% 雄烯二酮升高,15% 总睾酮升高,21% 性激素结合球蛋白降低 [SHBG])。基线时,痤疮评分越高,SHBG水平越低 (p 0.05)。55% 妇女的卵巢有多个卵泡。两组的痤疮均显着改善 (平均痤疮评分,EE/DSG为2.9-0.9,EE/GTD为2.87-1.25; p 0.05)。事实上,EE/GTD组62% 的病例和EE/DSG组90% 的病例具有最小或无痤疮损伤。治疗期间痤疮的改善与生化雄激素过多症的正常化显着相关。在第三个治疗周期完成时,两组的激素均显着降低。个体睾酮水平升高正常化。血浆SHBG的初始值增加了3倍。SHBG逐渐增加到EE-DSG OC使用的第9周期。在第9周期完成时,回声卵巢质地恢复正常。这些发现表明,由于两种oc在生化和临床上都有效,因此这些oc可能是治疗寻常痤疮的好方法。
  • 【含去氧孕烯的双相口服避孕药治疗期间的炔雌醇,3-酮-去孕甾酮,SHBG,CBG和促性腺激素的血清浓度。】 复制标题 收藏 收藏
    DOI:10.1159/000182537 复制DOI
    作者列表:Jung-Hoffmann C,Storch A,Kuhl H
    BACKGROUND & AIMS: :During a cross-over study, the pharmacokinetics of ethinylestradiol (EE) and 3-keto-desogestrel (KDG) were investigated on days 7 and 22 of one cycle of treatment with two biphasic formulations containing 50 micrograms EE (7 tablets) and 50 micrograms EE + 125 micrograms desogestrel (DG) (15 tablets) (50/50 EE) or 40 micrograms EE + 25 micrograms DG (7 tablets) and 30 micrograms EE + 125 micrograms DG (15 tablets) (40/30 EE). Peak serum levels and areas under the curve of EE increased significantly by 50% between days 7 and 22 of those taking 50/50 EE, while during treatment with 40/30 EE, no difference was found between days 7 and 22. Both formulations caused identical KDG levels on day 22. There were only slight differences in the effects of both preparations on sex-hormone-binding globulin (SHBG; +150 to +160%) and on corticosteroid-binding globulin (CBG; +130 to +150%) on day 7. On day 22, the changes were more pronounced with 50/50 EE (SHBG, +310%; CBG, +240%) than with 40/30 EE (SHBG, +250%; CBG, +180%). On day 22 after discontinuation of treatment, the SHBG and CBG levels were still significantly above the control values. Using both formulations, LH and FSH levels were significantly suppressed on day 22, while on day 7 no significant reduction was observed. The rise in the EE levels between days 7 and 22 of 50/50 EE intake and the time course of the EE concentrations during treatment with 40/30 EE appear to be due to an inhibition of hepatic metabolism by the contraceptive steroids, as EE is nearly exclusively bound to albumin which does not change.
    背景与目标: :在交叉研究中,在一个疗程的第7天和第22天研究了乙炔雌二醇(EE)和3-酮-去氧孕烯(KDG)的药代动力学,其中两种双相制剂分别含有50毫克EE(7片)和50毫克微克EE 125微克去氧孕烯(15片)(50/50 EE)或40微克EE 25微克DG(7片)和30微克EE 125微克DG(15片)(40/30 EE)。在服用50/50 EE的患者的7至22天之间,血清峰值水平和EE曲线下的面积显着增加了50%,而在使用40/30 EE的患者中,在7和22天之间没有发现差异。第22天的KDG水平相同。在第7天,两种制剂对性激素结合球蛋白(SHBG; 150%至160%)和对皮质类固醇结合球蛋白(CBG; 130%至150%)的作用仅有微小差异。在第22天,与使用40/30 EE(SHBG,250%; CBG,180%)相比,使用50/50 EE(SHBG,310%; CBG,240%)的变化更为明显。在停药后第22天,SHBG和CBG水平仍显着高于对照值。使用这两种配方,LH和FSH水平在第22天被显着抑制,而在第7天未观察到显着降低。在50/50 EE摄入量的第7天到22天之间,EE水平升高以及在用40/30 EE治疗期间EE浓度随时间变化的过程似乎是由于避孕类固醇抑制了肝代谢,因为EE是几乎只与不变的白蛋白结合。
  • 【孕二烯/乙炔雌二醇和去氧孕烯/乙炔雌二醇的单相口服避孕药的临床比较。拉丁美洲口服避孕药研究组。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:
    BACKGROUND & AIMS: The efficacy, cycle control, subjective complaints, and safety of monophasic preparations of the oral contraceptives containing gestodene 75 mcg plus ethinyl estradiol 30 mcg versus desogestrel 150 mcg plus ethinyl estradiol 30 mcg were compared in a 6-cycle, open-label, parallel, randomized, multicenter phase IV clinical study in Latin America. Of a total of 176 women in each group, 163 in the gestodene group and 160 in the desogestrel group completed 6 cycles, providing data for 1,015 and 1,006 cycles, respectively. Subject compliance was excellent; pills were missed during only 6.9% of the cycles in each group. No woman became pregnant during the study. Gestodene group exhibited significantly better cycle control as evidenced by the lower incidence of breakthrough bleeding and spotting. Spotting in some cycles was reported by 11.9% of women taking the gestodene-combination compared with 21% of women taking the desogestrel-combination. Based on number of women, 86.4% of the gestodene group reported all cycles were normal (no BTB) compared with 76.7% of the desogestrel group. Also, the women in the gestodene group reported a significantly lower incidence of nuisance side effects during treatment cycles. No amenorrhea was observed for either group. There were no clinically significant differences between groups with respect to body weight, blood pressure, or laboratory evaluations. Seven women withdrew from the gestodene group and 8 women withdrew from the desogestrel group because of adverse reactions. The results of this study indicate that, although both OCs provided effective contraception, in comparison to the desogestrel-combination, the gestodene-containing OC is associated with better cycle control, less bleeding, and fewer subjective complaints.

    背景与目标: 在一个6周期,开放标签,平行,6周期,开放标签,平行,拉丁美洲的随机,多中心IV期临床研究。每组总共176名妇女中,孕二烯酮组中的163名妇女和地索孕酮组中的160名妇女完成了6个周期,分别提供了1,015和1,006个周期的数据。受试者的依从性极好;每组仅在6.9%的周期内漏服药丸。在研究期间,没有女人怀孕。孕二烯酮组表现出明显更好的周期控制,其表现为突破性出血和斑点的发生率较低。据报道,服用孕二烯酮的妇女中有11.9%在某些周期出现斑点,而服用去氧孕烯的妇女中有21%的妇女出现了斑点。根据女性人数,孕二烯酮组中86.4%的人报告所有周期均正常(无BTB),而地索孕酮组的这一比例为76.7%。此外,孕二烯酮组的妇女报告在治疗周期中滋扰性副作用的发生率显着降低。两组均未观察到闭经。两组之间在体重,血压或实验室评估方面没有临床上的显着差异。由于不良反应,有7名妇女从孕二烯酮组退出,有8名妇女从地索孕酮组退出。这项研究的结果表明,尽管两种OC都能提供有效的避孕方法,但与去氧孕烯联合使用相比,含孕二烯的OC具有更好的周期控制,更少的出血和更少的主观主诉。

  • 【含左炔诺孕酮和去氧孕烯的低剂量口服避孕药对凝血的影响:一项交叉研究。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Middeldorp S,Meijers JC,van den Ende AE,van Enk A,Bouma BN,Tans G,Rosing J,Prins MH,Büller HR
    BACKGROUND & AIMS: :Combined oral contraceptives (OC) are known to increase the risk of venous thromboembolism. The aim of this randomized, cycle-controlled, cross-over study in 28 healthy volunteers was to assess potential differences between the effects of an OC containing 150 microg levonorgestrel (as representative of the so-called second generation OC) and an OC containing 150 microg desogestrel (as representative of the third generation OC) in combination with 30 microg ethinylestradiol on several coagulation factors and markers of thrombin formation. All participants used each OC for two cycles, and were switched to the other OC after a washout period of two menstrual cycles. The plasma concentrations of factors II, VII, X, and fibrinogen significantly increased during use of both the levonorgestrel- and desogestrel-containing OC's. The plasma concentrations of factor VIII increased, and of factor V decreased, changes which only reached statistical significance during the use of the desogestrel-containing OC. During exposure to the desogestrel-containing OC, as compared with the levonorgestrel-containing OC, both factor VII and factor II showed a greater increase (FVII: 32% and 12% respectively; p <0.0001; FII: 16% and 12% respectively; p = 0.048), whereas factor V showed a greater decrease (-11% and -3% respectively; p = 0.010). Only one of the markers for ongoing coagulation (prothrombin fragment 1+2) showed a significant increase during OC use, whereas concentrations of thrombin-antithrombin complexes and soluble fibrin remained unchanged. For these markers, there was no difference between the tested OC's. We conclude that there are differences between the effects of levonorgestrel and desogestrel-containing OC's on some coagulation factors. Whether these changes provide a biological explanation for the reported differences in venous thromboembolic risk is as yet unclear. The real challenge now becomes to define a pattern of changes in the various systems which, if affected simultaneously, may tip the hemostatic balance towards a prethrombotic state and may lead to overt clinical venous thromboembolism.
    背景与目标: :已知联合口服避孕药(OC)会增加静脉血栓栓塞的风险。这项针对28位健康志愿者进行的随机,周期控制,交叉研究的目的是评估含150微克左炔诺孕酮的OC(代表所谓的第二代OC)与含150克左炔诺孕酮的OC的作用之间的潜在差异。微克去氧孕烯(代表第三代OC)与30微克乙炔雌二醇组合在一起,可用于多种凝血因子和凝血酶形成标记。所有参与者使用每个OC两个周期,并在两个月经周期的冲洗期后切换到另一个OC。在同时使用含左炔诺孕酮和去氧孕烯的OC的过程中,因子II,VII,X和纤维蛋白原的血浆浓度显着增加。血浆VIII因子浓度升高,而V因子浓度降低,这些变化仅在使用含去氧孕烯的OC期间达到统计学显着性。与含左炔诺孕酮的OC相比,暴露于含地索孕烯的OC期间,因子VII和II均显示出更大的增加(FVII:分别为32%和12%; p <0.0001; FII:分别为16%和12% ; p = 0.048),而因子V表现出更大的下降幅度(分别为-11%和-3%; p = 0.010)。持续使用的凝血中只有一种标记物(凝血酶原片段1 2)显示在使用OC期间显着增加,而凝血酶-抗凝血酶复合物和可溶性血纤蛋白的浓度保持不变。对于这些标记,测试的OC之间没有差异。我们得出结论,左炔诺孕酮和含去氧孕烯的OC对某些凝血因子的作用之间存在差异。这些变化是否为所报告的静脉血栓栓塞风险差异提供了生物学解释,目前尚不清楚。现在真正的挑战是确定各种系统的变化模式,如果同时受到影响,则可能使止血平衡趋于血栓前状态,并可能导致临床上明显的静脉血栓栓塞。
  • 【两种含有乙炔雌二醇和去氧孕烯或孕二烯酮的单相口服避孕药的功效和可接受性。】 复制标题 收藏 收藏
    DOI:10.3109/13625189809051413 复制DOI
    作者列表:Halbe HW,de Melo NR,Bahamondes L,Petracco A,Lemgruber M,de Andrade RP,da Cunha DC,Guazelli CA,Baracat EC
    BACKGROUND & AIMS: OBJECTIVE:To assess the contraceptive efficacy, cycle control and acceptability of two monophasic oral contraceptives containing either 30 micrograms ethinylestradiol plus 150 micrograms desogestrel or 30 micrograms ethinylestradiol plus 75 micrograms gestodene.

    METHODS:In a randomized, open-label, six-cycle, group-comparative, multicenter study performed in Brazil, pregnancies, cycle-control parameters, incidence of side-effects and the presence and severity of acne vulgaris were assessed, and blood pressure and body weight were measured at pretreatment and after one, three and six cycles of oral contraceptive use.

    RESULTS:Of the 595 women enrolled, 274 (86.7%) in the desogestrel/ethinylestradiol group and 227 (81.4%) in the gestodene/ethinylestradiol group completed the six cycles, providing data for 1753 and 1487 treatment cycles, respectively. Two pregnancies occurred, one of which (in the desogestrel/ethinylestradiol group) was attributed to user failure, whilst the other (in the gestodene/ethinylestradiol group) was thought to result from method failure. Cycle control was observed to be excellent; the incidences of irregular bleeding and minor side-effects were low in both groups and decreased after an initial increase in the first cycle. Pre-existing acne improved in both groups, whereas blood pressure and body weight remained essentially unchanged.

    CONCLUSIONS:Both desogestrel/ethinylestradiol and gestodene/ethinylestradiol provide effective oral contraception with comparable cycle control and acceptability.

    背景与目标: 目标:评估两种单相口服避孕药的避孕效果,周期控制和可接受性,其中两种避孕药均含有30毫克乙炔雌二醇加150毫克去氧孕烯或30毫克乙炔雌二醇加75毫克雌二醇。

    >方法:在巴西进行的一项随机,开放标签,六周期,组比较的多中心研究中,妊娠,周期控制参数,副作用的发生率以及寻常痤疮的发生和严重程度是

    结果:在接受治疗的前,次,三和六个周期的口服避孕药评估后,测量血压和体重。

    结果:在纳入研究的595名妇女中,有274名(86.7%) )在去氧孕烯/炔雌醇组中为),而在孕二烯/炔雌醇组中为227(81.4%)完成了六个周期,分别提供了1753和1487个治疗周期的数据。发生了两次怀孕,其中一个(在去氧孕烯/乙炔雌二醇组中)归因于用户失败,而另一个(在孕二烯/乙炔雌二醇组中)则归因于方法失败。观察到循环控制非常好;两组的不规则出血和轻微副作用的发生率均较低,并且在第一个周期最初增加后有所下降。两组都已存在痤疮的情况有所改善,而血压和体重却基本保持不变。

    结论:去氧孕烯/乙炔雌二醇和孕二烯/乙炔雌二醇均能提供有效的口服避孕药,并且具有可比的周期控制能力和可接受性。

  • 【17种α-炔雌醇,左炔诺孕酮,3-酮-去孕甾烯和孕二烯对人主动脉平滑肌中通过电压门控钙通道的钙流入的影响。】 复制标题 收藏 收藏
    DOI:10.1016/s0010-7824(96)00188-6 复制DOI
    作者列表:Seeger H,Mück AO,Lorkowski G,Teichmann AT,Lippert TH
    BACKGROUND & AIMS: The effect of the synthetic estradiol, 17 alpha-ethinylestradiol, and three progestogens on calcium influx was investigated in cell cultures of human aortic smooth muscle. Neither the synthetic estrogen nor the progestogens levonorgestrel, 3-keto-desogestrel, and gestodene showed, in the concentration range of 10(-9) to 10(-6) M, a significant effect on calcium influx both alone or in equimolar estrogen-gestagen combinations. The results indicate that these substances, commonly used in contraceptive pills, do not change vasotonus interfering with calcium homeostasis.

    背景与目标: 在人主动脉平滑肌的细胞培养物中,研究了合成雌二醇,17α-炔雌醇和三种孕激素对钙内流的影响。在10(-9)至10(-6)M的浓度范围内,无论是合成雌激素还是孕激素,左炔诺孕酮,3-酮-去孕甾烯酮和孕二烯均未显示对钙流入量的显着影响,无论是单独的还是等摩尔的雌激素-孕激素组合。结果表明,这些常用于避孕药的物质不会改变影响钙稳态的血管紧张素。

  • 【含Desogestrel的分阶段口服避孕药对皮脂溢和痤疮的作用。】 复制标题 收藏 收藏
    DOI:10.1080/13625180500252638 复制DOI
    作者列表:Kränzlin HT,Nap MA
    BACKGROUND & AIMS: OBJECTIVE:To investigate the effect of an oral contraceptive (Novial) on facial seborrhea and moderate acne. METHODS:In this nonrandomized, group-comparative trial, women aged between 18 and 30 with seborrhea were enrolled. Women used either a phasic oral contraceptive containing ethinylestradiol (35/30/30 microg) and Desogestrel (50/100/150 microg (DSG-OC)) (n = 177) or no hormonal treatment (control group; n = 77) for four cycles. RESULTS:Overall, 161 subjects (90.9%) in the DSG-OC group and 73 subjects (94.4%) in the control group completed the study. In the DSG-OC group, the total score for sebum excretion decreased by 0.71 nL/cm(2) (95% CI 0.36-1.05). In the control group, sebum excretion increased by 0.05 nL/cm(2) (-0.55 to 0.46). The difference between groups (0.78 nL/cm(2) (0.19-1.36)) was statistically significant (P = 0.010). The number of active follicles/cm(2) decreased by 0.86 (0.44-1.28) and 0.08 (-0.53 to 0.69), respectively (P = 0.029). The difference in qualitative scores between the groups (0.93 (0.08-1.78)) was statistically significant ( P = 0.032). Overall, 19.3% of the subjects reported an AE (18.1% in the DSG-OC group, 22.1% in the control group). CONCLUSION:Novial effectively reduces seborrhea after only four cycles of treatment and may be a suitable oral contraceptive for women wishing to improve their facial skin condition.
    背景与目标: 目的:探讨口服避孕药(Novial)对面部皮脂溢出和中度痤疮的影响。
    方法:在这项非随机分组对照试验中,纳入了18至30岁患有皮脂溢出的女性。妇女使用含乙炔雌二醇(35/30/30微克)和地索孕酮(50/100/150微克(DSG-OC))(n = 177)的阶段性口服避孕药或未进行激素治疗(对照组; n = 77)四个周期。
    结果:总体而言,DSG-OC组中有161名受试者(90.9%),而对照组中有73名受试者(94.4%)完成了研究。在DSG-OC组中,皮脂排泄总分降低了0.71 nL / cm(2)(95%CI 0.36-1.05)。在对照组中,皮脂排泄增加了0.05 nL / cm(2)(-0.55至0.46)。组之间的差异(0.78 nL / cm(2)(0.19-1.36))具有统计学显着性(P = 0.010)。活动卵泡/ cm(2)的数量分别减少了0.86(0.44-1.28)和0.08(-0.53至0.69)(P = 0.029)。两组之间的定性得分差异(0.93(0.08-1.78))具有统计学意义(P = 0.032)。总体而言,有19.3%的受试者报告了AE(DSG-OC组为18.1%,对照组为22.1%)。
    结论:仅在四个疗程后,Novial即可有效减少皮脂溢,对于希望改善面部皮肤状况的女性而言,它可能是合适的口服避孕药。
  • 【地索孕酮/乙炔雌二醇加螺内酯与醋酸环丙孕酮/乙炔雌二醇治疗多囊卵巢综合征的比较:一项随机对照试验。】 复制标题 收藏 收藏
    DOI:10.1111/jog.12543 复制DOI
    作者列表:Leelaphiwat S,Jongwutiwes T,Lertvikool S,Tabcharoen C,Sukprasert M,Rattanasiri S,Weerakiet S
    BACKGROUND & AIMS: AIM:To compare the effects of ethinyl estradiol (EE) 30 mcg/desogestrel 150 mcg plus spironolactone 25 mg/day (group A) versus EE 35 mcg/cyproterone acetate 2 mg (group B) on hyperandrogenism and metabolism in PCOS. METHODS:This was a randomized clinical study. Eighteen women in groups A and B received medications for three cycles. Acne score, androgens and metabolic parameters were assessed before and after treatment. RESULTS:One and two women in groups A and B, respectively, were excluded from the study. Both groups had significantly decreased acne score and free androgen index, and increased sex hormone-binding globulin levels. Cholesterol and high-density lipoprotein were significantly increased in group B, and androstenedione was significantly decreased in group A. The regular withdrawal bleeding was obtained in both groups. CONCLUSION:Both regimens had quite similar efficacy on hyperandrogenism after three cycles of therapy and without any changes in metabolic parameters.
    背景与目标: 目的:比较乙炔雌二醇(EE)30 mcg /去氧孕烯150 mcg加螺内酯25 mg / day(A组)与EE 35 mcg /醋酸环丙孕酮2 mg(B组)对PCOS高雄激素血症和新陈代谢的影响。
    方法:这是一项随机临床研究。 A组和B组中的18名妇女接受了三个周期的药物治疗。治疗前后评估痤疮评分,雄激素和代谢参数。
    结果:A和B组分别有1名和2名妇女被排除在研究之外。两组痤疮评分和游离雄激素指数均显着降低,而性激素结合球蛋白水平升高。 B组胆固醇和高密度脂蛋白显着升高,A组雄烯二酮显着降低。两组均获得了常规戒断出血。
    结论:两种方案在三个疗程后对高雄激素血症的疗效均相似,且代谢参数没有任何变化。
  • 【口服给予去氧孕烯和3-酮-去氧孕烯后的血清3-酮-去氧孕烯的水平。】 复制标题 收藏 收藏
    DOI:10.1016/0010-7824(86)90047-8 复制DOI
    作者列表:Hasenack HG,Bosch AM,Käär K
    BACKGROUND & AIMS: :In a cross-over study with orally administered desogestrel (0.150 mg) plus ethinyloestradiol (0.030 mg) and 3-keto-desogestrel (0.150 mg) plus ethinyloestradiol (0.030 mg) in ten women under steady-state conditions, the serum levels of 3-keto-desogestrel were monitored by radioimmunoassay. No statistically significant differences between treatment groups were found with respect to the areas under the curve of the serum levels versus time (AUC), peak heights and peak times. The individual AUCs for 3-keto-desogestrel after dosing with desogestrel (plus EE) or 3-keto-desogestrel (plus EE) show a similar degree of variation. The biotransformation of desogestrel into 3-keto-desogestrel is rapid and appears not to be limited by the metabolic capacity of the normal liver.
    背景与目标: :在一项十项妇女在稳态条件下口服给予去氧孕烯(0.150 mg)加乙炔雌二醇(0.030 mg)和3-酮-去氧孕烯(0.150 mg)加乙炔雌二醇(0.030 mg)的交叉研究中,通过放射免疫测定法监测3-酮-去氧孕烯。关于血清水平对时间(AUC),峰高和峰时间的曲线下面积,在治疗组之间没有发现统计学上的显着差异。用去氧孕烯(加EE)或3-酮去氧孕烯(加EE)给药后,3-酮去氧孕烯的单个AUC表现出相似的变化程度。去氧孕烯到3-酮-去氧孕烯的生物转化是迅速的,并且似乎不受正常肝脏代谢能力的限制。
  • 【在稳态和交叉时,接受含地索孕酮联合口服避孕药(COC)的妇女的蛋白S水平低于接受含左炔诺孕酮的COC的妇女。】 复制标题 收藏 收藏
    DOI:10.1046/j.1365-2141.2001.02853.x 复制DOI
    作者列表:Mackie IJ,Piegsa K,Furs SA,Johnson J,Bounds W,Machin SJ,Guillebaud J
    BACKGROUND & AIMS: :This study aimed to identify specific haemostatic changes that might account for previous observations of higher venous thromboembolic risk among users of combined oral contraceptives (COCs) containing desogestrel (DSG) than levonorgestrel (LNG). Sixty-three current users of monophasic 30 microg oestrogen COCs containing either LNG or DSG omitted one pill-free interval (PFI), switching immediately either to the opposite formulation for one cycle or continuing with the same pill. Venesection followed the initial PFI after one cycle (21 tablets) and two cycles (42 tablets) of continuous pill taking, and after the following PFI. Protein S was lower in users of DSG than LNG formulations after the first PFI (mean +/- SD, 0.67 +/- 0.09 vs 0.76 +/- 0.10, P < 0.001) and after one cycle (0.61 +/- 0.09 vs 0.76 +/- 0.09, P < 0.0001). Protein S decreased when switching from LNG to DSG pills (0.77 +/- 0.07-0.65 +/- 0.06, P < 0.0001), mirrored by an increase at switching from DSG to LNG formulations (0.61 +/- 0.08-0.73 +/- 0.10, P < 0.005). Mean protein S levels remained within the normal range. Three different markers of thrombin generation remained unaltered. Potential explanations for COC-related thrombotic events are 'acquired resistance to activated protein C' or inhibition of fibrinolysis. A potential role has been described for protein S deficiency in both. A further triggering factor is a probable prerequisite for actual thrombosis, but pill-takers whose levels of protein S were in the lowest percentiles may be at greatest risk.
    背景与目标: :本研究旨在确定特定的止血变化,这些变化可能解释了先前观察到的患者中,使用去氧孕烯(DSG)联合左炔诺孕酮(LNG)的联合口服避孕药(COC)使用者的静脉血栓栓塞风险更高。目前有63位使用LNG或DSG的单相30微克雌激素COC使用者省略了一个无丸间隔(PFI),立即切换到相反的配方进行一个周期或继续使用同一丸。在连续服药一个周期(21片)和两个周期(42片)之后,以及随后的PFI之后,Venesection遵循最初的PFI。 DSG使用者在第一次PFI之后的蛋白S低于LNG制剂(平均值/-SD,0.67 /-0.09 vs 0.76 /-0.10,P <0.001),并且在一个周期后(0.61 // 0.09 vs 0.76 /-0.09, P <0.0001)。从LNG换成DSG药丸时,蛋白质S减少(0.77 /-0.07-0.65 /-0.06,P <0.0001),这反映了从DSG换成LNG制剂时的增加(0.61 /-0.08-0.73 /-0.10,P < 0.005)。平均蛋白S水平保持在正常范围内。凝血酶生成的三个不同标记保持不变。 COC相关血栓形成事件的潜在解释是“获得的对活化蛋白C的抗性”或纤维蛋白溶解的抑制。已经描述了两者中蛋白质S缺乏症的潜在作用。另一个触发因素是实际血栓形成的可能先决条件,但蛋白质S水平最低的服用避孕药者风险最高。
  • 【含乙炔雌二醇联合屈螺酮或去氧孕烯的口服避孕药在13个周期内对脂质和脂蛋白代谢影响的随机研究。】 复制标题 收藏 收藏
    DOI:10.1016/j.contraception.2003.11.003 复制DOI
    作者列表:Gaspard U,Endrikat J,Desager JP,Buicu C,Gerlinger C,Heithecker R
    BACKGROUND & AIMS: :In this open-label, randomized study we compared the influence of a new oral contraceptive containing 30 microg ethinylestradiol and 3 mg drospirenone (EE + DRSP = Yasmin), with a reference preparation containing 30 microg ethinylestradiol and 150 microg desogestrel (EE + DSG = Marvelon) on the lipid profile. The primary target variables were total high-density lipoprotein (HDL) cholesterol, HDL2 cholesterol and low-density lipoprotein (LDL) cholesterol. These and additional lipid and lipoprotein fractions were measured at baseline and in the 3rd, 6th and 13th treatment cycles in a total of 50 volunteers, and also assessed after density gradient ultracentrifugation. A slight increase in mean total HDL cholesterol vs. baseline was found for the DRSP group (+12.8%) and the DSG group (+11.8%) after 13 treatment cycles. HDL2 cholesterol did not change remarkably in both groups. The mean LDL cholesterol values increased by 10.6% vs. baseline in the DSG group and remained nearly stable in the DRSP group (+1.8%). All measured values remained within the reference ranges. No statistically significant differences were found between the two treatment groups for those primary endpoints. A slight rise in mean total cholesterol was found for all cycles after the initiation of treatment. The mean increase after 1 year of treatment was approximately 8% in both treatment groups. Mean triglyceride levels increased for both treatment groups without leaving the reference range. The increase for total triglycerides was +73.6 % in the DRSP group and +61.3% in DSG group. For total phospholipids, an increase of +13.6% (DRSP) and +18.5% (DSG) over 13 cycles was measured. The apolipoproteins Apo A-I, Apo A-II and Apo B increased slightly more during DRSP treatment than during DSG treatment. The reduction of Apo E was similar in both groups. Lipoprotein (a) remained stable in the DRSP group, whereas it increased by +10.8% in the DSG group. In conclusion, the combined low-dose oral contraceptive Yasmin, with 30 microg ethinylestradiol and 3 mg of the novel progestogen drospirenone, as well as the reference preparation, had little impact on the lipid profile. While both preparations displayed a favorable lipid profile with increased total HDL cholesterol, the antiandrogenic or missing androgenic activity of Yasmin may be regarded as responsible for the stable LDL cholesterol levels. As a result, the ratio of total HDL:LDL was increased, a pattern that is usually considered clinically beneficial with respect to cardiovascular disease risk.
    背景与目标: :在这项开放标签的随机研究中,我们比较了一种新的口服避孕药(其含量为30微克乙炔雌二醇和3 mg屈螺酮(EE DRSP = Yasmin))与一种参比制剂(其所含参比制剂为30微克乙炔雌二醇和150 microg去氧孕烯酮(EE DSG = Marvelon)的影响) )的脂质分布。主要目标变量是总高密度脂蛋白(HDL)胆固醇,HDL2胆固醇和低密度脂蛋白(LDL)胆固醇。在基线和第50,第3,第6和第13治疗周期中测量了这些以及其他脂质和脂蛋白组分,并在密度梯度超速离心后进行了评估。在13个治疗周期后,DRSP组和DSG组的平均总HDL胆固醇相对于基线略有增加(分别为12.8%)和11.8%。两组的HDL2胆固醇均无明显变化。与DSG组的基线相比,平均LDL胆固醇值增加了10.6%,而在DRSP组中则保持近乎稳定(1.8%)。所有测量值均保持在参考范围内。在这两个主要终点的两个治疗组之间未发现统计学上的显着差异。开始治疗后所有周期的平均总胆固醇均略有上升。在两个治疗组中,治疗1年后的平均增长率约为8%。两个治疗组的平均甘油三酯水平均增加,但未超出参考范围。 DRSP组的总甘油三酯增加量为73.6%,DSG组的总甘油三酯增加量为61.3%。对于总磷脂,在13个循环中测得分别增加了13.6%(DRSP)和18.5%(DSG)。与DSG处理相比,DRSP治疗期间载脂蛋白Apo A-I,Apo A-II和Apo B的增加略多。两组中Apo E的减少相似。脂蛋白(a)在DRSP组中保持稳定,而在DSG组中增加了10.8%。总之,低剂量口服避孕药Yasmin与30微克乙炔雌二醇和3 mg新型孕激素drospirenoneone以及参考制剂的结合对血脂几乎没有影响。尽管两种制剂均显示出良好的脂质分布,总HDL胆固醇增加,但Yasmin的抗雄激素或雄激素缺乏活性可能被认为是稳定的LDL胆固醇水平的原因。结果,总HDL:LDL的比例增加了,这种模式通常被认为相对于心血管疾病的风险在临床上是有益的。
  • 【多相研究含阶段性地索非孕酮的口服避孕药的功效,周期控制和耐受性。】 复制标题 收藏 收藏
    DOI:10.1080/13625180008500378 复制DOI
    作者列表:Ferguson H,Vree ML,Wilpshaar J,Eskes TK
    BACKGROUND & AIMS: OBJECTIVE:To investigate the efficacy, cycle control and tolerability of a phasic oral contraceptive containing ethinylestradiol 35/30/30 microg and desogestrel 50/100/150 microg. METHODS:A multicenter study was conducted involving 2070 healthy, fertile women, who received study treatment for six treatment cycles. RESULTS:Most of the participants (79%) had previously been using an alternative oral contraceptive. In 10,408 treatment cycles, two women became pregnant while on treatment (Pearl index, 0.25). The incidence of irregular bleeding was 10% before treatment, rising to 27% at cycle 1, and decreasing to 11% by cycle 6. Irregular bleeding was mainly due to spotting rather than breakthrough bleeding and the incidence of breakthrough bleeding remained below 2.2% for most of the study period. Only 1.8% of women withdrew due to bleeding irregularities. First-time oral contraceptive users initially experienced more irregular bleeding than switchers but these differences lessened over time. The most common adverse events during treatment were headache, breast tenderness and nausea. The incidence of these adverse events fell to below pretreatment levels with continued use. CONCLUSION:The phasic preparation was effective and well tolerated.
    背景与目标: 目的:研究一种含有炔雌醇35/30/30微克和地索孕酮50/100/150微克的阶段性口服避孕药的疗效,周期控制和耐受性。
    方法:进行了一项多中心研究,涉及2070名健康,受孕的妇女,这些妇女接受了六个治疗周期的研究治疗。
    结果:大多数参与者(79%)以前一直在使用其他口服避孕药。在10,408个治疗周期中,两名妇女在接受治疗时怀孕(Pearl index,0.25)。治疗前不规则出血的发生率是10%,在第1周期上升到27%,到第6周期下降到11%。大部分学习期间。只有1.8%的妇女因不规则出血而退出。初次口服避孕药的使用者最初比不使用切换器的人发生更多的不规则出血,但是随着时间的流逝,这些差异逐渐减少。治疗期间最常见的不良事件是头痛,乳房胀痛和恶心。通过持续使用,这些不良事件的发生率降至治疗前水平以下。
    结论:分期制剂有效,耐受性好。

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