アリルエストレノールの抗前立腺作用に関する基礎的,臨床的研究

Abstract

ラット前立腺腹葉を対象としアリルエストレノールの抗前立腺作用を検討し, 直接的, 間接的抗前立腺作用で, 酢酸クロルマジノンに匹敵する作用効果を認めた.前立腺肥大症19例に45mg経口投与し, 排尿障害の改善と肥大結節萎縮につき満足すべき臨床効果を得た.4例の病期D前立腺癌に90mg経口投与し, ある程度の制癌効果を得た

The anti-androgen activity of allylestrenol was studied in the rat, and it was found to have an activity which was equivalent to that of chlormadinone acetate. The direct anti-prostatic activity is the result of the following mechanism: inhibition of serum testosterone uptake into the prostate, inhibition of testosterone-5 alpha-reductase activity and inhibition of 5 alpha-DHT . receptor complex formation. Large doses of allylestrenol administered to normal mature rats, inhibit the hypothalamus-pituitary-gonadal axis, and atrophy of the prostate will be more marked due to an indirect effect as a result of the reduction in the serum testosterone level. Based on this finding, we performed a clinical trial with allylestrenol in patients with hypertrophy of the prostate and cancer of the prostate. We administered 45 mg a day allylestrenol to 19 patients with prostatic hypertrophy and obtained satisfactory clinical results in so far as improvement of micturition and reduction in prostate mass was concerned. We also administered 90 mg a day of allylestrenol to 4 patients with cancer of the prostate and obtained a cytostatic effect.