Fluorouracil

Generic Details

Generic Name

Fluorouracil

Other Names

  • 5-FU
  • Efudex
  • Adrucil

Drug Class

  • Antimetabolite
  • Antineoplastic

Chemical Formula

C4H3FN2O2

Molecular Weight

130.08 g/mol

Mechanism of Action

  • Inhibits thymidylate synthase
  • Incorporated into RNA and DNA leading to cell death

Indications

  • Colorectal cancer
  • Breast cancer
  • Basal cell carcinoma
  • Actinic keratosis
  • Topical use for skin conditions

Common Dosage Forms

  • Topical cream
  • Intravenous solution

Typical Dosage

  • 400-1000 mg/m2/day intravenously in divided doses
  • Topical cream applied once or twice daily as directed

Pediatric Dosage

  • Dosage must be carefully calculated based on weight and body surface area

Geriatric Dosage

  • Dosage adjustment may be needed based on renal function

Side Effects

  • Nausea and vomiting
  • Myelosuppression
  • Hand-foot syndrome
  • Diarrhea
  • Mucositis

Contraindications

  • Hypersensitivity to fluorouracil
  • Severe bone marrow suppression

Pregnancy Category

  • Category D - Positive evidence of risk

Lactation Safety

  • Should not be used while breastfeeding

Drug Interactions

  • Leucovorin - may increase toxicity of fluorouracil

Overdose Symptoms

  • Severe GI toxicity
  • Bone marrow suppression

Antidote for Overdose

  • No specific antidote, symptomatic and supportive care

Storage Conditions

  • Store at room temperature (20-25°C)
  • Protect from light and moisture

Pharmacokinetics

  • Absorption: Well absorbed after oral or topical administration
  • Distribution: Widely distributed in body tissues
  • Metabolism: Primarily hepatic
  • Excretion: Mainly through urine

Precautions

  • Monitor blood counts regularly during therapy
  • Avoid sun exposure when using topically

Warnings

  • Can cause severe and life-threatening adverse effects
  • Should only be administered under the supervision of a healthcare provider

Others

  • May cause local skin reactions when used topically