II. 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

III. 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

IV. Medications

  1. Fluorouracil IV Solution: 500 mg, 2.5 g or 5 g vials

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Alopecia
  2. Angina
  3. Diarrhea
  4. Mucositis
  5. Myelosuppression
  6. Impaired future fertility
  7. Palmar-plantar erythrodysesthesia (hand-foot syndrome)

VII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception
  3. Monitoring
    1. Complete Blood Count (CBC)

VIII. Drug Interactions

  1. Warfarin
    1. Increased INR

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Related Studies

Cost: Medications

fluorouracil (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
FLUOROURACIL 2% TOPICAL SOLN Generic $3.61 per ml
FLUOROURACIL 5% CREAM Generic $0.87 per gram
FLUOROURACIL 5% TOPICAL SOLN Generic $5.94 per ml

Ontology: Fluorouracil (C0016360)

Definition (NCI_NCI-GLOSS) A drug used to treat symptoms of cancer of the colon, breast, stomach, and pancreas. It is also used in a cream to treat certain skin conditions. Fluorouracil stops cells from making DNA and it may kill cancer cells. It is a type of antimetabolite.
Definition (NCI) An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions.
Definition (MSH) A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.
Definition (CSP) pyrimidine analog that is an antineoplastic antimetabolite.
Definition (PDQ) An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), a necessary constituent of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43130&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43130&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C505" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D005472
SnomedCT 3127006, 387172005
LNC LP16149-4, MTHU016749, LA14338-0
English 5 Fluorouracil, 5-Fluorouracil, Fluoruracil, 2,4(1H,3H)-Pyrimidinedione, 5-fluoro-, 5-FU, 5FU, 2,4-Dioxo-5-fluoropyrimidine, 5-Fluoro-2,4(1H,3H)-pyrimidinedione, fluorouracil, 5fluorouracil, Fluoro Uracil, Fluouracil, 5Fluracil, 5-fluorouracil (medication), 5-fluorouracil, FLUOROURACIL, Fluorouracil [Chemical/Ingredient], 5 fu, 5-fu, 5 fluorouracil, 5-Fluoro-2,4(1H, 3H)-pyrimidinedione, 5-Fu, Fluorouracil®, 5FU - Fluorouracil, Fluorouracil (product), Fluorouracil (substance), 5-Fluracil, FU, Fluorouracil
Swedish Fluorouracil
Czech fluorouracil
Finnish Fluorourasiili
Russian FTORURATSIL, ФТОРУРАЦИЛ
Japanese フルオロウラシル, 5-フルオロウラシル
Italian 5-FU, 5FU, 5-Fluorouracile, Fluorouracile
Polish Fluorouracyl
Portuguese Fluorouracil, Fluoruracila
Spanish 5-fluorouracilo, fluorouracilo (producto), fluorouracilo (sustancia), fluorouracilo, Fluorouracilo
French Fluorouracile
German Fluoruracil