Hammerstein J
Abteilung für Gynäkologische Endokrinologie, Klinikum Steglitz Freien Universität Berlin.
Wien Med Wochenschr. 1987 Oct 15;137(18-19):441-9.
Following introductory terminological clarifications, the pharmacological peculiarities of the synthetic estrogens and progestogens used in oral contraception are outlined. With the low-dose formulations containing less than 50 micrograms estrogen per pill ("micropill") coming in preferential use, the definite differences between the profiles of effects of the three major progestational categories--estranes, gonanes and pregnanes--lost much of their impact on clinical tolerance. Within the three classes of progestogens, the profiles of effects of the various compounds are, anyhow, very similar with major deviations occurring only exceptionally. As to the contraceptive estrogens, ethinyl estradiol differs from mestranol, if any, in quantitative but not in qualitative respect, the latter substance not being commonly used in Europe any longer. Besides potencies and profiles of effects of the individual contraceptive steroids, the quantitative estrogen/progestogen relationship of a "pill" is another variable of great importance for the development of unwanted side effects in the field of lipid and carbohydrate metabolism as well as of blood coagulation. Due to the lack of influence on lipid metabolism, progestogens of the pregnane series, being driven into an outsider position since long, deserve increasing attention again. As a general principle, women of all age groups should at least try to use the "micropill"--either combination-type or tristep formulations--in order to minimize risks. Only a few indications are left for the primary prescription of high-dose combination-type, sequential and step-up preparations as well as for the progestogen-only "minipill". With "micropill" becoming the oral contraceptives of the first choice, also rational reasons for changing formulations have become rare.(ABSTRACT TRUNCATED AT 250 WORDS)
在进行术语介绍性说明后,概述了口服避孕药中使用的合成雌激素和孕激素的药理学特性。随着每片含雌激素低于50微克的低剂量制剂(“微型药丸”)的优先使用,三种主要孕激素类别——雌甾烷类、孕甾烷类和孕烷类——的作用谱之间的明确差异对临床耐受性的影响大大降低。在这三类孕激素中,各种化合物的作用谱非常相似,只有在极少数情况下才会出现重大偏差。至于避孕雌激素,炔雌醇与炔雌醚在数量上而非质量上有所不同,后者在欧洲已不再常用。除了各个避孕类固醇的效力和作用谱外,“药丸”中雌激素/孕激素的定量关系是脂质和碳水化合物代谢以及血液凝固领域出现不良副作用的另一个重要变量。由于对脂质代谢没有影响,长期处于边缘地位的孕烷系列孕激素再次值得更多关注。一般原则是,所有年龄段的女性都应至少尝试使用“微型药丸”——组合型或三步制剂——以将风险降至最低。高剂量组合型、序贯和逐步增加制剂以及仅含孕激素的“迷你药丸”的主要处方适应证已所剩无几。随着“微型药丸”成为首选口服避孕药,更换制剂的合理理由也变得很少见。(摘要截选至250字)