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Fluorouracil information from DrugsUpdate  

See Available Brands of Fluorouracil in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Fluorouracil (5-FU or f5U) (Adrucil, Efudex, Fluoroplex) is a pyrimidine analog, which is used as a drug in the treatment of cancer. It belongs to the family of drugs called antimetabolites. It is typically administered with leucovorin.

Pharmacodynamics

Pharmacokinetics

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).

Fluorouracil Indications / Fluorouracil Uses

Information Not Available

Fluorouracil Adverse Reactions / Fluorouracil Side Effects

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.

Precautions

Warnings
Hospitalize for first course of injection therapy because of the possibility of severe toxic reactions.

Monitor
Before each injection dose, obtain WBC with differential. Biopsy solar keratosis, which do not respond, to confirm the diagnosis. Perform follow-up biopsies as indicated in the management of superficial basal cell carcinoma.

Special 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.

Other 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.

Other Interactions

Information Not Available

Dosage

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/week.
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 weeks or maintenance doses of 5-15 mg/kg/weeks (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 weeks.
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 weeks. Hgher strengths may be used for at least 3-6 weeks 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 weeks. Hgher strengths may be used for at least 3-6 wk in superficial basal cell carcinoma.

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.

Special Populations


Dose should be halved in patients with poor nutritional status, impaired bone marrow, and within 30 days of major surgery.

Food(before/after)

Information Not Available

List of Contraindications

Fluorouracil and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Fluorouracil and Lactation

Contraindicated in lactation

Fluorouracil and Children

Safety and efficacy not established

Fluorouracil and Geriatic

Information Not Available

Fluorouracil and Other Contraindications

Topical application on mucous membranes, exposure to sunlight, hypersensitivity. Depressed bone marrow function, poor nutritional status, potentially serious infections. Pregnancy and lactation.

Storage

Intra-arterial
Store at 25°C.

Intravenous
Store at 25°C.

Oral
Store at 25°C.

Lab interference

Intra-arterial
Store at 25°C.

Intravenous
Store at 25°C.

Oral
Store at 25°C.

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