Fungal pyrimidine antimetabolite
Fungal pyrimidine antimetabolite (cytosine deaminase → 5-FU)
- Fungal cytosine permease takes it up and cytosine deaminase makes 5-fluorouracil inside the fungus — human cells lack the deaminase
- 5-FU blocks thymidylate synthase and miscodes RNA → fungal DNA and protein synthesis fail
- Resistance emerges fast alone; paired with amphotericin for cryptococcal meningitis
- Gut flora deaminate some drug → marrow suppression and hepatotoxicity; level monitoring
- Fungal cytosine permease takes it up and cytosine deaminase makes 5-fluorouracil inside the fungus — human cells lack the deaminase
- 5-FU blocks thymidylate synthase and miscodes RNA → fungal DNA and protein synthesis fail
- Resistance emerges fast alone; paired with amphotericin for cryptococcal meningitis
- Gut flora deaminate some drug → marrow suppression and hepatotoxicity; level monitoring
Drugs with this mechanism (1)
- Flucytosine — Antifungal prodrug activated to 5-FU by an enzyme fungi have and humans do not.
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