Oral Administration of 5-Fluorouracil: Renal Clearance and Urinary Concentration in Man

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Abstract
The pharmacokinetics of 5-fluorouracil 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 .apprx. 40 ml/min. The maximum serum (1100 ng/ml serum) and urinary concentrations (49,000 ng/ml urine) of 5-fluorouracil occurred 20 and 40 min 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.