Edgren R A, Sturtevant F M
Am J Obstet Gynecol. 1976 Aug 15;125(8):1029-38. doi: 10.1016/0002-9378(76)90804-8.
Oral contraceptives are combinations of estrogens and progestogens or, in the case of the mini-pills, progestogens alone. With specific test procedures in laboratory animals or human subjects, it is possible to assign potency evaluations to the components relative to the progestational, estrogenic, or antiestrogenic activities of the progestogen or to the estrogenic potencies of the estrogenic component. It might even be possible to quantify the synergistic effects of the estrogen on the progestational agent. Unfortunately, however, it is impossible now to amalgamate such assay results into single estimates of the potencies of the combinations (either the combination products per se or the combination tablets of sequential products). For example, an over-all estrogenic potency of a combination preparation would involve the integration of contributions form the estrogen itself plus the estrogenic products of metabolism of the progestogen minus the antagonistic effect of the progestational agent, if any. These factors cannot now be quantified independently, much less merged into a single figure of clinical significance. Further, even if it were possible to produce such an estimate, it is unlikely that the evaluation would be meaningful in relation to any putative side effect or adverse reaction, i.e., the alleged thrombogenic effects of oral contraceptives cannot currently be related directly to any measure of potency that will allow prediction of these clinical conditions from laboratory models. Any evaluation of the potential of a given contraceptive to produce a specific side effect will depend upon data generated with specific regard to that adverse reaction and the individual product in question.
口服避孕药是雌激素和孕激素的组合,或者在短效口服避孕药的情况下,仅含孕激素。通过在实验动物或人体受试者中采用特定的测试程序,有可能根据孕激素的孕激素活性、雌激素活性或抗雌激素活性,或雌激素成分的雌激素效力,对各成分进行效力评估。甚至有可能量化雌激素对孕激素的协同作用。然而,不幸的是,目前无法将这些测定结果合并为对组合制剂效力(无论是组合产品本身还是序贯产品的组合片剂)的单一估计值。例如,一种组合制剂的总体雌激素效力将涉及雌激素本身的贡献、孕激素代谢产生的雌激素产物以及孕激素的拮抗作用(如果有的话)的整合。目前这些因素无法独立量化,更不用说合并为一个具有临床意义的单一数值了。此外,即使有可能得出这样的估计值,该评估对于任何假定的副作用或不良反应而言也不太可能有意义,即目前口服避孕药所谓的血栓形成作用无法直接与任何效力指标相关联,从而无法从实验室模型预测这些临床情况。对特定避孕药产生特定副作用可能性的任何评估将取决于针对该不良反应和相关个别产品所产生的数据。