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Fluorouracil

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Fluorouracil, Adrucil, 5-FU, 5-Fluorouracil

  • See Also
  1. Topical Fluorouracil
  2. Antimetabolite Chemotherapy
  3. Chemotherapy
  • Indications
  1. See Topical Fluorouracil
  2. FDA Approved
    1. Colon Cancer
    2. Rectal Cancer
    3. Breast Cancer
    4. Gastric Cancer
    5. Pancreatic Cancer
  3. Off-Label Uses
    1. Anal Cancer
    2. Bladder Cancer
    3. Cervical Cancer
    4. Esophageal Cancer
    5. Head and Neck Cancer
    6. Hepatobiliary Cancer
    7. Nasopharyngeal Cancer (children)
    8. Neuroendocrine Tumors
    9. Penile Cancer
    10. Vulvar Cancer
  4. References
    1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  • Mechanism
  1. Pyrimidine Antimetabolite Chemotherapy with antineoplastic activity
  2. Pyrimidine Analog of the Nucleoside uracil
  3. Fluoruracil is a prodrug converted to multiple active metabolites in vivo
    1. F-UMP (5-fluoroxyuridine monophosphate)
    2. F-dUMP (5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate)
  4. F-UMP incorporates into RNA, replacing uracil
    1. Inhibits RNA processing, Protein synthesis and cell growth
  5. F-dUMP inhibits thymidylate synthase
    1. Depletes thymidine triphosphate (TTP), a Nucleotide precursor
    2. With less TTP available, DNA synthesis is inhibited
  • Medications
  1. Fluorouracil IV Solution: 500 mg, 2.5 g or 5 g vials
  • Dosing
  1. See other references for disease specific dosing protocols
  • Adverse Effects
  1. Alopecia
  2. Angina
  3. Diarrhea
  4. Mucositis
  5. Myelosuppression
  6. Impaired future fertility
  7. Palmar-plantar erythrodysesthesia (hand-foot syndrome)
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception
  3. Monitoring
    1. Complete Blood Count (CBC)
  • Drug Interactions
  1. Warfarin
    1. Increased INR
  • Resources
  1. Fluorouracil (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=ea3497db-23b9-4ace-9a6f-b54853d04a82
  2. Fluorouracil (StatPearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK549808/