FDA-Approved Indications

• Fluorouracil is approved by the US Food and Drug Administration (FDA) and is indicated for the
  treatment of gastric adenocarcinoma, pancreatic adenocarcinoma, breast adenocarcinoma, and colorectal adenocarcinoma.

Mechanism of Action

• Fluorouracil enters cells via a facilitated transport mechanism and undergoes conversion into
  fluorodeoxyuridine monophosphate (FdUMP).
• Fluorodeoxyuridine monophosphate is a chemotherapy metabolite, which acts as a potent
  inhibitor of enzyme thymidylate synthase which plays an important role in the DNA synthesis,
  which eventually stops the cancer cell growth.
• FdUMP forms complexes with the enzyme thymidylate synthase, which inhibits the production of
  deoxythymidine monophosphate (dTMP).
  dTMP is crucial for DNA replication and repair, depletion in dTMP causes an imbalance in
  intracellular nucleotides, which results in the generation of double-stranded DNA breaks
  facilitated by the enzyme endonuclease.
• Fluorouracil acts as a pyrimidine analog by misincorporating into RNA and DNA instead of uracil
  or thymine.
• The damage of DNA repair caused by these mechanisms results in cell death of rapidly
  proliferating cells.
  Strength:
• Fluorouracil injection is supplied as a bulk package as a vial containing 50 mg/mL of
  flourouracil.

Recommended Dosage:

• Fluorouracil dosage varies based on the type of cancer being treated, the specific regimen, and
  the patient’s condition.
• For colorectal adenocarcinoma, the recommended dose is 400 mg/m² intravenously
  as a bolus on Day 1, followed by a 46-hour infusion of 2,400 to 3,000 mg/m² every two
  weeks, or 500 mg/m² as a bolus on Days 1, 8, 15, 22, 29, and 36 in 8-week cycles.
  For breast adenocarcinoma, it’s 500–600 mg/m² intravenously on Days 1 and 8 every
  28 days for six cycles.
  In gastric adenocarcinoma, the dose ranges from 200 mg/m² to 1,000 mg/m² as a
  continuous 24-hour infusion, with frequency and cycle length depending on the specific
  regimen.For pancreatic adenocarcinoma, the dose is similar to colon cancer, with a bolus of
  400 mg/m² on Day 1, followed by 2,400 mg/m² as a continuous infusion every two
  weeks.

Warnings and Precautions:

• People who are allergic to fluorouracil should consult a doctor before starting the treatment of
  5F-Uracil.
  DPD deficiency (Dihydropyrimidine dehydrogenase) patients should inform the doctor as it may
  be dangerous for them.

Side effects:

• Fluorouracil may cause side effects such as:
• loss of appetite
• nausea
• unusual tiredness or weakness
• dizziness
• headache
• hair loss
• dry and cracked skin
• vision changes
• eye that are teary or sensitive to light
• redness, pain, swelling, or burning at the site where the injection was given
  confusion

Storage and Handling:

• Store at 20° to 25°C (68° to 77°F). Protect from light. DO NOT FREEZE.