Flucytosine

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Definition
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Flucytosine, a pyrimidine derivative that can only be administered intravenously, is an antimycotic (cytostatic) whose fungistatic and fungicidal effects are due to disorders in protein and DNA synthesis. In contrast to mammalian cells, flucytosine is selectively taken up by fungi via cytosine permease, deaminated and incorporated as 5-fluorouracil (5-FU) into the cell RNA, where it acts as a "false base" and induces a misprogrammed protein biosynthesis (cytostatic effect). In addition, DNA synthesis is inhibited because 5-fluorouracil blocks thymidilate synthesis (Liu Y et al. 2018).

Half-life
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3–5,3 h

Indication
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Severe syst. Infections from Candida or Cryptococcus neoformans.

Limited indication
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Dose adjustment for renal insufficiency, pregnancy, lactation.

Dosage and method of use
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150-200 mg/kg bw/day i.v. in 4 ED.

Undesirable effects
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Fever, fatigue, anemia, leukopenia, thrombopenia, nausea, diarrhea, allergic skin reactions, photosensitization, liver necrosis (also with fatal outcome).

Interactions
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Ganciclovir and zidovudine lead to a mutual increase in toxicity, cytostatic drugs increase the blood formation disorders.

Contraindication
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Flucytosine intolerance, blood formation disorders, liver damage.

Preparations
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Ancotil®

Literature
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  1. Gerson B (1987)Flucytosines (5-fluorocytosines). Clin Lab Med 7:541-544.
  2. Liu Y et al (2018) Simultaneous detection of 5-fluorocytosine and 5-fluorouracil in human cells carrying CD/5-FC suicide gene system by using capillary zone electrophoresis. J Chromatogr B Analyt Technol Biomed Life Sci 1076:1-7.

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Last updated on: 29.10.2020