Bioavailability, Distribution and Pharmacokinetics of Diethylstilbestrol Converted from Diethylstilbestrol Diphosphate in Patients with Prostatic Cancer

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タイトル ( eng )
Bioavailability, Distribution and Pharmacokinetics of Diethylstilbestrol Converted from Diethylstilbestrol Diphosphate in Patients with Prostatic Cancer
作成者
NAKAMURA Koji
収録物名
Hiroshima Journal of Medical Sciences
35
4
開始ページ 325
終了ページ 338
収録物識別子
[PISSN] 0018-2052
[EISSN] 2433-7668
[NCID] AA00664312
抄録
A method for the radioimmunoassay of diethylstilbestrol (DES) was established to evaluate the distribution of DES in patients with prostatic carcinoma receiving intravenous infusion of 500 mg of diethylstilbestrol diphosphate (DES-DP). The plasma DES concentration was markedly elevated to 4.9 μg/ml immediately after DES-DP infusion and rapidly decreased to 0.8 μg/ml at 3 hr after the DES-DP infusion. The DES concentration in the prostatic tissue was 1.6 μgig w.w. at 1 hr after infusion, and thereafter was predominantly similar to that in the plasma. The DES excretion in the urine was 23.7 mg at 0 to 3 hr after DES-DP infusion, and decreased gradually thereafter. In addition, the DES distribution in the subcellular fractions of benign hypertrophic prostates was studied following DES-DP infusion. The DES concentration in the nuclear fraction decreased with time. Furthermore, the protein specifically bound to DES was not detected in the cytosolic fraction. Therefore, the DES converted from DES-DP did not accumulate in the prostate. Subsequently, the bioavailabilities of DES were examined. The dihydrotestosterone (DHT) content of the prostatic tissue was significantly decreased at 24 hr after DES-DP infusion. However, the cytosolic androgen receptor content was insignificantly changed within 24 hr of infusion. Since the plasma luteinizing hormone (LH) level in the castrated patient with prostatic cancer was significantly lowered 3 hr after infusion, and further decreased with time, the main effect of DES was considered to be suppression of hypophyseal function.
著者キーワード
Diethylstilbestrol
Prostatic cancer
Dihydrotestosterone
Androgen receptor
NDC分類
医学 [ 490 ]
言語
英語
資源タイプ 紀要論文
出版者
Hiroshima University School of Medicine
発行日 1986-12
出版タイプ Version of Record(出版社版。早期公開を含む)
アクセス権 オープンアクセス
収録物識別子
[ISSN] 0018-2052
[NCID] AA00664312
[PMID] 3570844