el Etreby M F, Habenicht U F, Louton T, Nishino Y, Schröder H G
Research Laboratories of Schering AG, Berlin (West)/Bergkamen, Federal Republic of Germany.
Prostate. 1987;11(4):361-75. doi: 10.1002/pros.2990110408.
Cyproterone acetate (CPA) has a stronger inhibitory effect than megestrol acetate (MGA) and flutamide (FL) on the prostate and seminal vesicle of intact adult rats. Only in the clinically irrelevant regimen of castration and simultaneous androgen substitution is FL as a competitive androgen antagonist more potent than CPA and MGA. The latter inhibit complete involution of the ventral prostate but not of the seminal vesicle of castrated adult rats. This effect is very small in magnitude, cannot be increased by the use of higher doses, and is only reduced but not blocked by simultaneous treatment with high doses of FL. Further, CPA is unable to stimulate proliferation or restore the function of the involuted rat prostate. CPA and MGA inhibit adrenal weight in rats, thus indicating a glucocorticoidlike activity in this species. A critical review of all available data on the antiandrogenic, glucocorticoidlike, and possible paradoxical androgenlike activities of CPA in different animal experiments has no important bearing on the clinical effectiveness of CPA in the treatment of prostatic cancer.
醋酸环丙孕酮（CPA）对成年未阉割大鼠的前列腺和精囊的抑制作用比醋酸甲地孕酮（MGA）和氟他胺（FL）更强。仅在临床上不相关的去势并同时进行雄激素替代的方案中，作为竞争性雄激素拮抗剂的FL才比CPA和MGA更有效。后两者抑制成年去势大鼠腹侧前列腺的完全退化，但不抑制精囊的退化。这种作用程度非常小，不能通过使用更高剂量来增强，并且仅通过同时给予高剂量的FL治疗而降低但未被阻断。此外，CPA无法刺激大鼠退化前列腺的增殖或恢复其功能。CPA和MGA抑制大鼠肾上腺重量，因此表明该物种具有类糖皮质激素活性。对不同动物实验中关于CPA的抗雄激素、类糖皮质激素以及可能的矛盾性类雄激素活性所有现有数据的批判性综述，对CPA治疗前列腺癌的临床有效性并无重要影响。
