5-Fluorouracil

Indications
 Oral
Palliative treatment of carcinoma of the colon, rectum, breast, stomach or pancreas
Adult: 15 mg/kg (max: 1 g/day), may be given once wkly for maintenance.
Max Dosage: 1 g/wk.
Renal impairment: Dose reduction may be required.
Hepatic impairment: Dose reduction may be required.
Intravenous
Palliative treatment of carcinoma of the colon, rectum, breast, stomach or pancreas
Adult: 12 mg/kg/day (max 0.8-1g/day) for 3-4 days, if no toxicity occurs, may follow after 1 day with 6 mg/kg on alternate days for another 3-4 doses. Course may be repeated after 4-6 wk or maintenance doses of 5-15 mg/kg/wk (max 1g/wk) may be given. As an infusion, 15 mg/kg/day (max: 1 g daily) in 500 ml normal saline or 5% glucose over 4 hr, repeated on successive days until toxicity occurs or a total of 12-15 g is given. May repeat course after 4-6 wk.
Renal impairment: Dose reduction may be required.
Hepatic impairment: Dose reduction may be required.
Intra-arterial
Palliative treatment of carcinoma of the colon, rectum, breast, stomach or pancreas
Adult: 5-7.5 mg/kg daily as continuous infusion (regional perfusion).
Renal impairment: Dose reduction may be required.
Hepatic impairment: Dose reduction may be required.
Topical/Cutaneous
Actinic keratoses
Adult: As 0.5-5% cream or 1-5% solution in propylene glycol: Apply once or twice daily for 2-4 wk. Hgher strengths may be used for at least 3-6 wk in superficial basal cell carcinoma.
Topical/Cutaneous
Superficial basal cell carcinoma
Adult: As 0.5-5% cream or 1-5% solution in propylene glycol: Apply once or twice daily for 2-4 wk. Hgher strengths may be used for at least 3-6 wk in superficial basal cell carcinoma.

Special Populations: Dose should be halved in patients with poor nutritional status, impaired bone marrow, hepatic or renal function and within 30 days of major surgery.
Contraindications
 Topical application on mucous membranes, exposure to sunlight, hypersensitivity. Depressed bone marrow function, poor nutritional status, potentially serious infections. Pregnancy and lactation.
Warnings / Precautions
 Regular monitoring of blood counts. History of heart disease, hepatic or renal insufficiency, weak or malnourished patients, patients who with history of high-dose pelvic radiation or use of alkylating agents. Patients with widespread metastases to the bone marrow.
Adverse Reactions
 Leucopenia, thrombocytopaenia, stomatitis, GI ulceration, bleeding and diarrhoea, haemorrhage from any site (stop treatment). Nausea, vomiting, rashes, hyperpigmentation, alopecia. Topical: Local inflammatory and photosensitivity reactions. Dermatitis and erythema multiforme (rare).
Potentially Fatal: Central neurotoxicity, myocardial ischaemia.
Drug Interactions
 May increase warfarin effects. May reduce response to vaccines; possibility of generalized infection with live vaccines. Action may be modified by allopurinol. Leucovorin calcium may enhance the toxicity of fluorouracil.
See Below for More fluorouracil Drug Interactions
Mechanism of Actions
 Fluorouracil interferes with DNA synthesis by blocking the conversion of deoxyuridylic acid to thymidylic acid. It also interferes with RNA synthesis. This results in an unbalanced growth of the cells. Fluorouracil exerts greater effect on rapidly growing cells as they take up the drug at a faster rate.
Absorption: Unpredictable (oral); small amounts (topical).
Distribution: Body tissues and fluids, including blood-brain barrier.
Metabolism: Hepatic; catabolysed via dihydropyrimidine dehydrogenase.
Excretion: Urine (as unchanged drug); lungs (large amounts as carbon dioxide).
Storage Conditions
 Intra-arterial: Store at 25°C. Intravenous: Store at 25°C. Oral: Store at 25°C.
ATC Classification
 L01BC02 - fluorouracil ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
Storage
 Intra-arterial: Store at 25°C. Intravenous: Store at 25°C. Oral: Store at 25°C.
Available As
  • 5-Fluorouracil 250 mg
  • 5-Fluorouracil 50 mg

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