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Fluorouracil

    Brands

    DEA Class; Rx

    Common Brand Names; Adrucil, Efudex, Carac, Fluoroplex, Tolak

    • Antineoplastics, Antimetabolite
    • Dermatologics, Other; 
    • Antineoplastics, Topical

    Antimetabolite antineoplastic agent; fluorinated pyrimidine antineoplastic agent; toxicities and efficacy of 5-FU differ depending upon the route of administration; used for breast, colorectal, gastrointestinal, and head and neck cancers; used topically for malignant keratoses.

    Indicated for the treatment of

    • Breast Cancer
    • Gastric Cancer
    • Pancreatic Cancer
    • Glioblastoma Multiforme (Orphan)
    • Actinic (Solar) Keratoses
    • Superficial Basal Cell Carcinoma

    Other Indications & Uses

    Off-label use for cervical, bladder, hepatic, prostate, endometrial, and head and neck carcinoma

    Hypersensitivity to any component

    Women who are or may become pregnant

    Dihydropyrimidine Dehydrogenase (DPD) deficiency

    • Loss of appetite
    • Headache
    • Nausea
    • Vomiting
    • Diarrhea
    • Mucositis
    • Myelosuppression
    • Alopecia
    • Photosensitivity
    • Hand-foot syndrome
    • Maculopapular eruption (pruritic)

    Discontinue in case of stomatitis, esophagopharyngitis, leukopenia, thrombocytopenia, intractable vomiting, GI bleeding, hemorrhage

    Severe diarrhea may occur; withhold fluorouracil for Grade 3 or 4 diarrhea until resolved or decreased in intensity to Grade 1, then resume fluorouracil at a reduced dose; administer fluids, electrolyte replacement, or antidiarrheal treatments as necessary

    Therapy can cause neurologic toxicity, including acute cerebellar syndrome and other neurologic events, based on postmarketing reports; neurologic symptoms included confusion, disorientation, ataxia, or visual disturbances; withhold fluorouracil for neurologic toxicity; there are insufficient data on risks of resumption of fluorouracil in patients with neurologic toxicity that has resolved

    Treatment can cause cardiotoxicity, including angina, myocardial infarction/ischemia, arrhythmia, and heart failure; reported risk factors for cardiotoxicity are administration by continuous infusion rather than intravenous bolus and presence of coronary artery disease; withhold fluorouracil for cardiotoxicity; risks of resumption of fluorouracil in patients with cardiotoxicity that has resolved not established

    There are no adequate and well-controlled studies with fluorouracil in pregnant women; based on its mechanism of action, the drug can cause fetal harm when administered to a pregnant woman

    Not known whether fluorouracil or its metabolites are present in human milk; because many drugs are present in human milk and because of potential for serious adverse reactions in nursing infants from fluorouracil, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account importance of drug to the mother

    NOTE: The suggested maximum tolerated dose (MTD) for systemic fluorouracil is dependent on performance status, other chemotherapy agents or radiation given in combination, and disease state. The optimal dose or infusion duration of fluorouracil alone or in combination has not been determined. Therefore, dosing may vary from protocol to protocol. If questions arise, clinicians should consult the appropriate references to verify the dose.

    Adults

    The manufacturer recommends a maximum 5-FU dose of 800 mg/day IV; however, higher doses as are routinely given. Intravenous bolus doses of 20—25 mg/kg generally result in severe toxicity or fatalities due to hemorrhagic colitis or bone marrow suppression. By continuous infusion, higher daily doses (i.e., 1—2 g/day) have been given successfully with less hematologic toxicity. Maximum doses are not available for topical products.

    Geriatric

    The manufacturer recommends a maximum 5-FU dose of 800 mg/day IV; however, higher doses as are routinely given. Intravenous bolus doses of 20—25 mg/kg generally result in severe toxicity or fatalities due to hemorrhagic colitis or bone marrow suppression. By continuous infusion, higher daily doses (i.e., 1—2 g/day) have been given successfully with less hematologic toxicity. Maximum doses are not available for topical products.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Fluorouracil

    injectable solution

    • 50mg/mL

    cream

    • 0.5% (Carac)
    • 1% (Fluoroplex)
    • 4% (Tolak)
    • 5% (Efudex)

    topical solution

    • 2% (Efudex)
    • 5% (Efudex)