Dosing & Uses
Dosage Forms & Strengths
cream
- 0.5% (Carac)
- 1% (Fluoroplex)
- 4% (Tolak)
- 5% (Efudex)
topical solution
- 2% (Efudex)
- 5% (Efudex)
Actinic (Solar) Keratoses
Carac: Apply thin film to affected area qDay for 2-4 wk; healing may not be evident for 1-2 months
Efudex (2% solution): Apply sufficient amount to cover lesions q12hr for 2-4 wk; healing may not be evident for 1-2 months
Fluoroplex: Apply sufficient amount to cover lesions q12hr for 2-6 wk
Tolak (face, ears, or scalp): Apply sufficient amount to cover lesions of affected area(s) qDay for 4 weeks
Superficial Basal Cell Carcinoma
Efudex 5%: Apply sufficient amount of cream or solution to cover lesions q12hr for 3-6 wk; may continue application for up to 10-12 weeks
Not recommended
Adverse Effects
Frequency Not Defined
Pain
Pruritus
Headache
Insomnia
Irritability
Rash
Photosensitivity
Leukocytosis
Thrombocytopenia
Birth defects
Burning
Inflammation
Miscarriage
Herpes simplex
Allergic contact dermatits
Telangectasia
Hyperpigmentation (rare)
Scarring (rare)
Warnings
Contraindications
Hypersensitivity to any component
Women who are or may become pregnant
Dihydropyrimidine Dehydrogenase (DPD) deficiency
Cautions
Potential for delayed hypersensitivity reaction to fluorouracil
Occlusive dressings may increase inflammatory reaction in adjacent normal skin
Possibility for increased absorption through inflamed or ulcerated skin
Warn patients that the reaction in the treated areas may be unsightly during therapy and, usually, for several weeks following cessation of therapy; instruct patients to avoid exposure to ultraviolet rays during and immediately following treatment as intensity of reaction may increase
The drug may be fatal if ingested by pets; avoid allowing pets to contact the drug container or the skin where drug was applied; store drug out of reach of pets; safely discard or clean any cloth or applicator that may retain the drug and avoid leaving any residues on your hands, clothing, carpeting or furniture
Superficial BCC treatment only when conventional methods are impractical, since conventional methods have better response rate
Application site adverse reactions (erythema, scaling/dryness, edema, crusting, erosions, stinging/burning, and pruritus) are likely to occur during and for 4 weeks after treatment of actinic keratosis on the face, ears, and/or scalp
Do not apply directly into eyes, nose, mouth, or other mucous membranes because irritation, local inflammation and ulceration can occur
Avoid treatment in periocular area; eye disorders, including corneal reactions have occurred with topical fluorouracil use; avoid accidental transfer of drug into eyes and to periocular area; patients should wash hands well after applying the product; if accidental exposure occurs, seek medical care
Cases of miscarriage and birth defects occurred when pregnant women applied the topical form to mucous membranes; furthermore, fluorouracil interferes with synthesis of deoxyribonucleic acid (DNA), inhibits the formation of ribonucleic acid (RNA), and provokes unbalanced growth and death of cells
Dihydropyrimidine Dehydrogenase Deficiency
- A large percentage of fluorouracil is catabolized by the DPD enzyme; DPD enzyme deficiency may result in increased availability of fluorouracil to the anabolic pathway, which may lead to increased interference with DNA and RNA synthesis and increased cytotoxic activity and potential toxicities
- Life-threatening systemic toxicity reported with topical use of fluorouracil in a patient with DPD deficiency; patients should discontinue therapy if symptoms of fluorouracil’s systemic toxicity develop
Pregnancy & Lactation
Pregnancy
Cases of miscarriage and birth defects (including cleft lip and cleft palate) have been reported when pregnant women were exposed to a topical or parenteral form of the drug; in addition, ventricular septal defect and cases of miscarriage occurred when pregnant women applied a topical fluorouracil product to mucous membranes
Animal data
- Animal reproduction studies have shown fluorouracil to be teratogenic in mice, rats, and hamsters when given at doses equivalent to the usual human intravenous dose
Lactation
Because many drugs are excreted in human milk and there is some systemic absorption of fluorouracil after topical administration, and because of potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue drug use, taking into account the importance of the 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
Interferes with synthesis of DNA & to a lesser extent, RNA
Pharmacokinetics
Absorption: Insignificant (~6%)
Time to peak: 1 hr
Administration
Topical Administration
Apply q12hr with nonmetallic applicator, gloved hands or fingertips
If fingertips used, wash hands immediately afterwards
Solution considered more effective than cream for equivalent strength
Complete healing of lesions typically not evident for 1-2 months
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| fluorouracil intravenous - | 500 mg/10 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 - | 1 gram/20 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 |  | |
| 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 |  | |
| Carac topical - | 0.5 % cream |  | |
| Efudex topical - | 5 % cream |  | |
| Fluoroplex topical - | 1 % cream |  | |
| Tolak topical - | 4 % cream |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
fluorouracil intravenous
FLUOROURACIL - INJECTION
(flewr-oh-YOUR-uh-sill)
COMMON BRAND NAME(S): Adrucil
USES: Fluorouracil is used to treat various types of cancer. It is a chemotherapy drug that is used to slow or stop cancer cell growth.
HOW TO USE: This medication is usually given by injection into a vein by a health care professional. It may also be given by other methods of injection depending upon your medical condition. The dosage is based on your medical condition, body size, and response to therapy.
SIDE EFFECTS: Nausea, vomiting, loss of appetite, dry/itchy skin, or skin darkening may occur. Nausea and vomiting can be severe. In some cases, drug therapy may be necessary to prevent or relieve nausea and vomiting. Not eating before your treatment may help relieve vomiting. Changes in diet such as eating several small meals or limiting activity may help lessen some of these effects. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Mild diarrhea is also a common side effect. However, diarrhea can rarely become severe, causing very serious problems due to dehydration. Tell your doctor right away if you develop: diarrhea that is severe or doesn't stop, abdominal or stomach pain/cramping, or blood/mucus in your stool.Temporary hair loss may occur. Normal hair growth should return after treatment has ended.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.Hand and foot problems sometimes occur with fluorouracil use. You can prevent or reduce these problems by protecting your hands and feet from a great deal of heat or pressure. For example, avoid taking hot baths/showers, handwashing dishes with hot water, taking long walks, and rubbing your hands/feet. Tell your doctor right away if you develop the following symptoms on your hands/feet: redness, peeling skin, blisters, pain, numbness, tingling, or swelling. If you develop these symptoms, consult your doctor for treatment options (such as reducing your dose or stopping fluorouracil therapy, applying ice packs to the hands/feet).Tell your doctor right away if you have any serious side effects, including: headache, mental/mood changes (such as confusion), vision changes, unusual eye movements, loss of coordination, unusual tiredness.Get medical help right away if you have any very serious side effects, including: easy bruising/bleeding, blood in the urine, black/bloody stools, vomit that looks like coffee grounds, stomach/abdominal pain, chest pain, jaw/left arm pain, fast/slow/irregular heartbeat, mouth sores, sore throat, painful swallowing, heartburn, pain/redness/swelling of the arms/legs.This medication can lower the body's ability to fight an infection. Tell your doctor promptly if you develop any signs of an infection such as sore throat that doesn't go away, fever, or chills.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.Fluorouracil can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Get medical help right away if you develop a rash.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, 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: poor nutrition, decreased bone marrow function/blood cell disorders (such as anemia, leukopenia, thrombocytopenia), a certain enzyme deficiency (dihydropyrimidine dehydrogenase - DPD), a serious infection, liver problems, kidney problems.Tell your health care professional that you are using fluorouracil before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.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. Tell your doctor right away if you get sunburned or have skin blisters/redness.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using fluorouracil. Fluorouracil may harm an unborn baby. Men and women using this medication should ask about reliable forms of birth control during treatment and for some time after the last dose. If you or your partner becomes pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
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.A product that may interact with this drug is: warfarin.Fluorouracil is very similar to flucytosine and capecitabine. Do not use medications containing flucytosine or capecitabine while using fluorouracil.
OVERDOSE: 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: Lab and/or medical tests (such as complete blood counts) should be done while you are using this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.
STORAGE: Consult the product instructions and your pharmacist for storage details. 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.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised June 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.
