Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 50mg/mL (500mg/10mL single-dose vial)
Colon and Rectum Cancer
Indicated for adenocarcinoma of the colon and rectum
400 mg/m² IVP on Day 1, followed by 2400-3000 mg/m² IV as a continuous infusion over 46 hr q2Weeks in combination with leucovorin with or without oxaliplatin/irinotecan
Breast Cancer
Indicated for adenocarcinoma of the breast
500 or 600 mg/m² IV on Days 1 and 8 q28Days for 6 cycles as a component of a cyclophosphamide-based multidrug regimen
Gastric Cancer
Indicated for gastric adenocarcinoma
200-1000 mg/m²/day as a continuous IV infusion over 24 hr (as part of a platinum-containing regimen)
Duration and frequency of each cycle varies based on dose and regimen
Pancreatic Cancer
Indicated for pancreatic adenocarcinoma
400 mg/m² IVP on Day 1, followed by 2400 mg/m² IV as a continuous infusion over 46 hr q2Weeks
Combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin, is 400 mg/m² IVP on Day 1, followed by 2400 mg/m² IV as a continuous infusion over 46 hr q2Weeks
Dosage Modifications
Withhold dosing for any of the following
- Development of angina, myocardial infarction/ischemia, arrhythmia, or heart failure in patients with no history of coronary artery disease or myocardial dysfunction
- Hyperammonemic encephalopathy
- Acute cerebellar syndrome, confusion, disorientation, ataxia, or visual disturbances
- Grade 3 or 4 diarrhea
- Grade 2 or 3 palmar-plantar erythrodysesthesia (hand-foot syndrome)
- Grade 3 or 4 mucositis
- Grade 4 myelosuppression
Resume at reduced dose upon resolution or improvement to Grade 1 for
- Diarrhea
- Mucositis
- Myelosuppression
- Palmar-plantar erythrodysesthesia
No recommended dose for resumption following
- Cardiotoxicity
- Hyperammonemic encephalopathy
- Acute cerebellar syndrome, confusion, disorientation, ataxia, or visual disturbances
Safety & efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (18)
- adenovirus types 4 and 7 live, oral
fluorouracil decreases effects of adenovirus types 4 and 7 live, oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressives may diminish therapeutic effects of vaccines and increase risk of adverse effects (increased risk of infection). Live-attenuated vaccines should be avoided for at least 3mo after cessation of immunosuppressive therapy.
- axicabtagene ciloleucel
fluorouracil, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- brexucabtagene autoleucel
fluorouracil, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- ciltacabtagene autoleucel
fluorouracil, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- deferiprone
deferiprone, fluorouracil. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- erdafitinib
fluorouracil will increase the level or effect of erdafitinib by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP2C9 inhibitors, monitor closely for adverse reactions and consider decreasing dose accordingly. If strong CYP2C9 inhibitor is discontinued, consider increasing erdafitinib dose in the absence of any drug-related toxicities.
- etrasimod
etrasimod, fluorouracil. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Risk of additive immune system effects with etrasimod has not been studied in combination with antineoplastic, immune-modulating, or noncorticosteroid immunosuppressive therapies. Avoid coadministration during and in the weeks following administration of etrasimod. .
- germanium
germanium increases toxicity of fluorouracil by unspecified interaction mechanism. Contraindicated. Risk of toxicity, death with combination.
- idecabtagene vicleucel
fluorouracil, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- influenza virus vaccine quadrivalent, adjuvanted
fluorouracil decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- influenza virus vaccine trivalent, adjuvanted
fluorouracil decreases effects of influenza virus vaccine trivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- lisocabtagene maraleucel
fluorouracil, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- palifermin
palifermin increases toxicity of fluorouracil by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, fluorouracil. Either increases levels of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
- siponimod
fluorouracil will increase the level or effect of siponimod by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Coadministration of siponimod with drugs that cause moderate CYP2C9 AND a moderate or strong CYP3A4 inhibition is not recommended. Caution if siponimod coadministered with moderate CYP2C9 inhibitors alone.
- tinidazole
tinidazole will increase the level or effect of fluorouracil by decreasing hepatic clearance. Avoid or Use Alternate Drug. If the concomitant use of tinidazole and fluorouracil cannot be avoided, monitor for fluorouracil-associated toxicities.
- tisagenlecleucel
fluorouracil, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tofacitinib
fluorouracil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
Monitor Closely (41)
- acalabrutinib
acalabrutinib, fluorouracil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.
- antithrombin III
fluorouracil increases effects of antithrombin III by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- argatroban
fluorouracil increases effects of argatroban by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- belatacept
belatacept and fluorouracil both increase immunosuppressive effects; risk of infection. Use Caution/Monitor.
- bivalirudin
fluorouracil increases effects of bivalirudin by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- cholera vaccine
fluorouracil decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- dabigatran
fluorouracil increases effects of dabigatran by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- dalteparin
fluorouracil increases effects of dalteparin by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- dengue vaccine
fluorouracil decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- denosumab
fluorouracil, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- diclofenac
fluorouracil will increase the level or effect of diclofenac by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Do not exceed diclofenac dose of 50 mg BID
- dronabinol
fluorouracil will increase the level or effect of dronabinol by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Dronabinol is a CYP2C9 substrate.
- eluxadoline
fluorouracil increases levels of eluxadoline by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C9/10 inhibitors.
- enoxaparin
fluorouracil increases effects of enoxaparin by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- ethotoin
fluorouracil increases levels of ethotoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- eucalyptus
eucalyptus increases levels of fluorouracil by Other (see comment). Use Caution/Monitor. Comment: Applies to topical preparations only. Mechanism: enhanced transdermal absorption.
- fingolimod
fluorouracil increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .
- fondaparinux
fluorouracil increases effects of fondaparinux by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- fosphenytoin
fluorouracil increases levels of fosphenytoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- glyburide
fluorouracil increases levels of glyburide by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Strong CYP2C9 inhibitors may decrease glyburide metabolism.
- heparin
fluorouracil increases effects of heparin by unspecified interaction mechanism. Use Caution/Monitor. Due to the thrombocytopenic effects of fluorouracil, an additive risk of bleeding may be seen in patients receiving concomitant anticoagulants.
- hydroxyurea
fluorouracil, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.
- influenza A (H5N1) vaccine
fluorouracil decreases effects of influenza A (H5N1) vaccine by Mechanism: pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- influenza virus vaccine (H5N1), adjuvanted
fluorouracil decreases effects of influenza virus vaccine (H5N1), adjuvanted by Mechanism: pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- lacosamide
fluorouracil increases levels of lacosamide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely. Consider decreasing lacosamide dose when coadministered with strong CYP2C9 inhibitors.
- lesinurad
fluorouracil will increase the level or effect of lesinurad by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.
- leucovorin
leucovorin increases toxicity of fluorouracil by pharmacodynamic synergism. Use Caution/Monitor.
- meningococcal group B vaccine
fluorouracil decreases effects of meningococcal group B vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Individuals with altered immunocompetence may have reduced immune responses to the vaccine.
- metronidazole
metronidazole increases toxicity of fluorouracil by decreasing elimination. Use Caution/Monitor.
- ofatumumab SC
ofatumumab SC, fluorouracil. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olaparib
fluorouracil and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.
- ospemifene
fluorouracil increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- oxaliplatin
oxaliplatin will increase the level or effect of fluorouracil by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.
- phenytoin
fluorouracil increases levels of phenytoin by unknown mechanism. Use Caution/Monitor. Based on case reports.
- siponimod
siponimod and fluorouracil both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sipuleucel-T
fluorouracil decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- terbinafine
fluorouracil will increase the level or effect of terbinafine by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.
- trastuzumab
trastuzumab, fluorouracil. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, fluorouracil. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- ublituximab
ublituximab and fluorouracil both increase immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Owing to potential additive immunosuppressive effects, consider duration of effect and mechanism of action of these therapies if coadministered
- warfarin
fluorouracil will increase the level or effect of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.
Minor (4)
- maitake
maitake increases effects of fluorouracil by pharmacodynamic synergism. Minor/Significance Unknown. Maitake mushroom has anti-tumor effects (animal/in vitro research).
- taurine
fluorouracil decreases levels of taurine by unspecified interaction mechanism. Minor/Significance Unknown.
- vitamin A
vitamin A, fluorouracil. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin A enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
- vitamin E
vitamin E, fluorouracil. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin E enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
Adverse Effects
Frequency Not Defined
See Warnings section for details
Increased risk of serious or fatal adverse reactions in patients with low or absent dipyrimidine dehydrogenase activity
Cardiotoxicity
Hyperammonemic encephalopathy
Neurologic toxicity
Diarrhea
Palmar-plantar erythrodysesthesia (hand-foot syndrome)
Myelosuppression
Mucositis
Increased risk of elevated INR when administered with warfarin
Postmarketing Reports
Hematologic: Pancytopenia
Gastrointestinal (GI): GI ulceration, nausea, vomiting
Allergic reactions: Anaphylaxis and generalized allergic reactions
Neurologic: Nystagmus, headache
Dermatologic: Dry skin; fissuring; photosensitivity, as manifested by erythema or increased pigmentation of the skin; vein pigmentation
Ophthalmic: Lacrimal duct stenosis, visual changes, lacrimation, photophobia
Psychiatric: Euphoria
Miscellaneous: Thrombophlebitis, epistaxis, nail changes (including loss of nails)
Warnings
Black Box Warnings
The drug should be administered under the supervision of an experienced cancer chemotherapy physician because of the possibility of severe toxic reactions
Patient should be hospitalized for initiation of the therapy because of the risk for severe toxic reactions
Contraindications
None
Cautions
Discontinue in case of stomatitis, esophagopharyngitis, leukopenia, thrombocytopenia, intractable vomiting, GI bleeding, hemorrhage
Severe diarrhea may occur; withhold drug for Grade 3 or 4 diarrhea until resolved or decreased in intensity to Grade 1, then resume at a reduced dose; administer fluids, electrolyte replacement, or antidiarrheal treatments as necessary
Clinically significant elevations in coagulation parameters have been reported during concomitant use of warfarin and fluorouracil; closely monitor patients receiving concomitant coumarin-derivative anticoagulants such as warfarin for INR or prothrombin time to adjust anticoagulant dose accordingly
Myelosuppression
- Treatment can cause severe and fatal myelosuppression which may include neutropenia, thrombocytopenia, and anemia
- The nadir in neutrophil counts commonly occurs between 9 and 14 days after drug administration; obtain complete blood counts prior to each treatment cycle, weekly if administered on a weekly or similar schedule, and as needed
- Withhold drug until Grade 4 myelosuppression resolves; resume at a reduced dose when myelosuppression has resolved or improved to Grade 1 in severity
Palmoplantar erythrodysesthesia
- Therapy can cause palmoplantar erythrodysesthesia, also known as hand-foot syndrome (HFS)
- Symptoms of HFS include a tingling sensation, pain, swelling, and erythema with tenderness, and desquamation; HFS occurs more commonly when fluorouracil is administered as a continuous infusion than when administered as a bolus injection, and has been reported to occur more frequently in patients with previous exposure to chemotherapy
- HFS is generally observed after 8 to 9 weeks of drug administration but may occur earlier; institute supportive measures for symptomatic relief of HFS; withhold administration for Grade 2 or 3 HFS; resume fluorouracil at a reduced dose when HFS is completely resolved or decreased in severity to Grade 1
Low or absent dipyrimidine dehydrogenase (DPD) activity
- Certain homozygous or certain compound heterozygous mutations in the DPD gene can result in complete or near complete absence of DPD activity
- Patients with absent DPD activity are at increased risk for acute early-onset of toxicity and severe, life-threatening, or fatal adverse reactions caused by fluorouracil (e.g., mucositis, diarrhea, neutropenia, and neurotoxicity)
- Patients with partial DPD activity may also have increased risk of severe, life-threatening, or fatal adverse reactions
- Withhold or permanently discontinue fluorouracil based on clinical assessment of onset, duration and severity of observed toxicities in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of DPD activity
- No fluorouracil dose has been proven safe for patients with complete absence of DPD activity; data are insufficient to recommend a specific dose in patients with partial DPD activity as measured by any specific test
Cardiotoxicity
- 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 IV bolus and presence of coronary artery disease
- Withhold fluorouracil for cardiotoxicity
- Risks of resuming in patients with cardiotoxicity that has resolved is not established
Hyperammonemic encephalopathy
- Can cause hyperammonemic encephalopathy in absence of liver disease or other identifiable cause, based on postmarketing reports
- Signs or symptoms of hyperammonemic encephalopathy reported to start within 72 hr after initiating fluorouracil infusion; these included altered mental status, confusion, disorientation, coma, or ataxia, in the presence of concomitant elevated serum ammonia level
- Withhold fluorouracil for hyperammonemic encephalopathy and initiate ammonia-lowering therapy; risks of resuming in patients with hyperammonemic encephalopathy that has resolved have not been established
Neurologic toxicity
- Neurotoxicity reported, including acute cerebellar syndrome and other neurologic events
- Neurologic symptoms included confusion, disorientation, ataxia, or visual disturbances
- Withhold fluorouracil for neurologic toxicity
- Data are insufficient on risks of resuming in patients with neurologic toxicity that has resolved
Mucositis
- Mucositis, stomatitis or esophagopharyngitis, which may lead to mucosal sloughing or ulceration, can occur with fluorouracil
- Incidence is reported to be higher with administration by IV bolus compared with administration by continuous infusion
- Withhold administration for Grade 3 or 4 mucositis; resume at a reduced dose once mucositis has resolved or decreased in severity to Grade 1
Pregnancy & Lactation
Pregnancy
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
If this drug is used during pregnancy, or patient becomes pregnant while taking this drug, apprise the patient of the potential hazard to a fetus
Contraception
- Females: Based on mechanism of action, drug can cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during treatment with fluorouracil and for up to 3 months following cessation of therapy
- Males: Fluorouracil may damage spermatozoa; advise males with female partners of reproductive potential to use effective contraception during and for 3 months following cessation of therapy
Infertility
- Females: Advise females of reproductive potential that, based on animal data, fertility may be impaired while receiving fluorouracil
- Males: Advise males of reproductive potential that, based on animal data, fertility may be impaired while receiving fluorouracil
Animal data
- Administration to rats and mice during selected periods of organogenesis, at doses lower than a human dose of 12 mg/kg, caused embryolethality and teratogenicity; malformations included cleft palate and skeletal defects
- In monkeys, maternal doses of fluorouracil higher than an approximate human dose of 12 mg/kg resulted in abortion
Lactation
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
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits DNA synthesis during S phase by inhibition of thymidylate synthetase
Pharmacokinetics
Half-Life: 16 min
Onset: 2-7 d, but may take up to 12 wk
Duration: 24 hr
Metabolism: liver
Metabolites: urea, fluorouracil, dihydrofluorouracil, expired CO2 metabolite
Excretion: urine
Pharmacogenomics
Dihydropyrimidine dehydrogenase (DPD), an enzyme encoded by the DPYD gene, is the rate-limiting step in pyrimidine catabolism and deactivates >80% of 5FU standard doses and the 5FU prodrug capecitabine
Contraindicated in patients with DPD deficiency; causes severe toxicity with conventional doses (ie, grade III/IV toxicity and potentially fatal neutropenia, mucositis, and diarrhea)
Because true DPD deficiency is rare and because the clinical implications of partial deficiency are still unclear, screening for mutations prior to initiating therapy is not warranted
Genetic testing laboratories
- The following companies currently offer testing for DPYD*2A mutations
- EntroGen (http://www.entrogen.com)
- Myriad (http://www.myriadtests.com)
- LabCorp (http://www.labcorp.com)
- Molecular Diagnostics Laboratories (http://www.mdl-labs.com)
Administration
IV Incompatibilities
Additive: carboplatin, cisplatin, cytarabine, diazepam, doxorubicin, epirubicin, fentanyl, leucovorin, metoclopramide, morphine sulfate
Syringe: doxorubicin (at high conc of doxo & 5FU, compatible at lower conc), droperidol, epirubicin
Y-site: aldesleukin, amphotericin B cholesteryl SO4, droperidol, filgrastim, ondansetron(?), topotecan, vinorelbine
IV Compatibilities
Solution: compatible w/ most common solvents
Additive: bleomycin, cyclophosphamide, cyclophosphamide/methotrexate, etoposide, floxuridine, hydromorphone, ifosfamide, methotrexate, mitoxantrone, vincristine
Syringe: bleomycin, cisplatin, cyclophosphamide, furosemide, heparin, leucovorin, methotrexate, metoclopramide, mitomycin, vinblastine, vincristine
Y-site: (partial list) allopurinol, furosemide, granisetron, heparin, hydrocortisone-Na-succinate, leucovorin, linezolid, metoclopramide, piperacillin/tazobactam, KCl, propofol, vit B/C
IV Preparation
IV Push: dose/syringe (concentration: 50 mg/mL); max syringe size for IVP is 30 mL syringe and syringe should be <75% full
Continuous IV Infusion/IVPB: dose/50-1000 mL D5W or NS; syringe and solution are stable for 72 hr at 4 to 25°C
IV Administration
Direct IV push injection (50 mg/mL solution needs no further dilution) or by IV infusion
Toxicity may be reduced by giving the drug as a constant infusion
Bolus doses may be administered by slow IVP or IVPB
Warm to body temperature before using
Continuous IV infusion may be administered in D5W or NS
Solution should be protected from direct sunlight
5-FU may also be administered intra-arterially or intra-hepatically
Use plastic IV containers for continuous infusions (stable in plastic IV bags than in glass bottles)
Storage
Store intact vials at room temp & protect from light
Slight discoloration does not usually denote decomposition
Don't use cloudy solutions
- If crystals form, redissolve by warming
Don't refrigerate
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Fluoroplex topical - | 1 % cream |  | |
| Efudex topical - | 5 % cream |  | |
| fluorouracil topical - | 2 % solution |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 0.5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % solution |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil intravenous - | 500 mg/10 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 5 gram/100 mL vial |  | |
| fluorouracil intravenous - | 5 gram/100 mL vial |  | |
| fluorouracil intravenous - | 2.5 gram/50 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 500 mg/10 mL vial |  | |
| fluorouracil intravenous - | 2.5 gram/50 mL vial |  | |
| fluorouracil intravenous - | 5 gram/100 mL vial |  | |
| fluorouracil intravenous - | 2.5 gram/50 mL vial |  | |
| fluorouracil intravenous - | 5 gram/100 mL vial |  | |
| fluorouracil intravenous - | 2.5 gram/50 mL vial |  | |
| fluorouracil intravenous - | 500 mg/10 mL vial |  | |
| fluorouracil intravenous - | 500 mg/10 mL vial |  | |
| Tolak topical - | 4 % cream |  | |
| Carac topical - | 0.5 % cream |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
fluorouracil topical
FLUOROURACIL - TOPICAL
(flewr-oh-YOUR-uh-sill)
COMMON BRAND NAME(S): Efudex, Fluoroplex
USES: This medication is used on the skin to treat pre-cancerous and cancerous skin growths. Fluorouracil belongs to a class of medications known as anti-metabolites. It works by blocking the growth of abnormal cells that cause the skin condition.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using this medication and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Use this medication as directed by your doctor. Before you apply this medication to the skin, clean the affected area and dry well. Wait 10 minutes, then apply a small amount of medication to the affected skin, using just enough to cover the area with a thin film. Wash your hands immediately after applying this medication, even if you have used gloves.The treated area may become unsightly during treatment and in some cases for several weeks after treatment. Do not cover the area with tight dressings or plastic bandages. Check with your doctor whether you may cover the treated area loosely with gauze.Avoid applying this medication in or around the eyes or eyelids. Also, do not apply this medication inside the nose or mouth. If you do get the medication in these areas, rinse with plenty of water.This medication may cause serious harm (even death) in pets. Keep this medication securely away from pets, and do not allow pets to lick the area where the medication was applied. Contact your vet right away if your pet comes into contact with this medication.Use this medication exactly as prescribed. Do not stop using this medication without consulting your doctor. Do not increase your dose or use it more often than directed. Your condition will not clear faster, but side effects will be increased.If your condition worsens or does not improve, consult your doctor or pharmacist promptly.
SIDE EFFECTS: Skin irritation, burning, redness, dryness, pain, swelling, tenderness, or changes in skin color may occur at the site of application. Eye irritation (such as stinging, watering), trouble sleeping, irritability, temporary hair loss, or abnormal taste in the mouth may also occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: stomach/abdominal pain, bloody diarrhea, vomiting, signs of infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding, mouth sores.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using fluorouracil, tell your doctor or pharmacist if you are allergic to it; or to flucytosine; or to capecitabine; or if you have any other allergies. This product may contain inactive ingredients (such as peanut oil found in some brands), which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain enzyme deficiency (dihydropyrimidine dehydrogenase - DPD), red/irritated/infected/open sores on skin.This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. After using fluorouracil cream, wait 2 hours before applying sunscreen or moisturizer to the treated area. Do not use other skin products including creams, lotions, medications, or cosmetics unless instructed by your doctor to do so. Tell your doctor right away if you get sunburned or have skin blisters/redness.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication must not be used during pregnancy. It may harm an unborn baby. Discuss the use of reliable forms of birth control with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breastfeeding is not recommended while using this medication. Consult your doctor before breastfeeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: This medicine may be harmful if swallowed. If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.This medication must be used under close medical supervision. Be sure to keep all your medical appointments so your doctor can monitor your progress or any side effects.Discard any unused medication when the treatment is finished. Do not use it for any other skin conditions unless directed to do so by your doctor.There are different brands and forms of this medication available. Not all have identical effects. Do not change brands or forms without consulting your doctor or pharmacist.
MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature. Do not freeze. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised October 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
