5-氟尿嘧啶的口服给药：人体中的肾脏清除率和尿药浓度
Oral administration of 5-fluorouracil: renal clearance and urinary concentration in man.
作者信息
Leissner K H, Gustavsson B
出版信息
J Urol. 1982 Oct;128(4):697-9. doi: 10.1016/s0022-5347(17)53140-7.
The pharmacokinetics of 5-fluouracil were studied in 9 patients with a history of bladder malignancies. A single dose of 250 mg. 5-fluorouracil was given orally and the renal clearance of active 5-fluorouracil was approximately 40 ml. per minute. The maximum serum (1,100 ng./ml. serum) and urinary concentrations (49,000 ng./ml. urine) of 5-fluorouracil occurred 20 and 40 minutes after administration, respectively. The urinary concentration per se is highly cytotoxic, whereas the short-lasting serum concentration previously has been proved to be without general cytotoxic effects even after continuous use of the drug for years. Although high concentrations of 5-fluorouracil are noted in the urine the antitumor effects of this treatment must be investigated further.
对9例有膀胱恶性肿瘤病史的患者进行了5-氟尿嘧啶的药代动力学研究。口服单剂量250mg 5-氟尿嘧啶，活性5-氟尿嘧啶的肾清除率约为每分钟40ml。5-氟尿嘧啶的血清最高浓度（血清1100ng/ml）和尿液最高浓度（尿液49000ng/ml）分别在给药后20分钟和40分钟出现。尿液中的浓度本身具有高度细胞毒性，而先前已证明即使连续使用该药物数年，短暂的血清浓度也无一般细胞毒性作用。尽管尿液中5-氟尿嘧啶浓度较高，但这种治疗的抗肿瘤效果仍需进一步研究。
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