Basic and clinical studies on flucytosine in patients with fungi in their urine

Satoshi Uno, Yoshio Nishitani, Daisuke Yamada, Masaya Tsugawa, Hiromi Kumon, Hiroyuki Ohmori, Katsuichi Nanba, Katsuyoshi Kondoh, Mikio Kishi

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)


We studied the pharmacokinetics and clinical efficacy of flucytosine (5-FC), an antimycotic agent, in the urological field. 1) Pharmacokinetics: A single dose of 5-FC [0.5g or 1.0g (potency)] was administered to three normal adults by the cross-over method, and drug concentrations in blood and urine were measured. Three subjects also received nine consecutive 1.0 g doses of 5-FC at 12 hour intervals for administrations, and serum concentrations were measured. In the single-dose study, maximum blood levels (7.4 µg/ml at 0.5 g, 13.9 µg/ml at 1.0 g) were observed two hours after administration and the half-lives were 3.65 and 3.90 hrs, respectively. Cumulative urinary recovery rates were 87.2% and 79.8%, respectively. In the multiple-dose study, steady-state blood concentrations were obtained after the third dose and no tendency to accumulate was observed. 2) Clinical study: We treated 25 patients with fungi in their urine with 5-FC at dose of 1.0 g t.i. d. for 7–14 days. According to the criteria Japanese U TI Committee, with a slight modification, the overall clinical efficacy rate was 77.8% (14/18). Mycologically, 15 out of 20 strains (75.0%). were eradicated. Nausea and anorexia were noted in 1 patient each, but they improved without therapy. Concerning the laboratory findings, a transient elevation of ALP and Cr, and a mild decrease in K were noted in 1 patient each. Consequently, 5-FC appears to be a useful drug in the treatment of fungi in the urine.

Original languageEnglish
Pages (from-to)1251-1262
Number of pages12
Issue number10
Publication statusPublished - Oct 1992


  • flucytosine

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Infectious Diseases
  • Pharmacology
  • Drug Discovery
  • Oncology


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