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 topical - | 0.5 % cream |  | |
| fluorouracil topical - | 2 % solution |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % solution |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| fluorouracil topical - | 5 % cream |  | |
| Adrucil intravenous - | 5 gram/100 mL vial |  | |
| Adrucil intravenous - | 500 mg/10 mL vial |  | |
| Adrucil intravenous - | 2.5 gram/50 mL vial |  | |
| Carac topical - | 0.5 % cream |  | |
| fluorouracil intravenous - | 500 mg/10 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 mL vial |  | |
| fluorouracil intravenous - | 5 gram/100 mL vial |  | |
| fluorouracil intravenous - | 1 gram/20 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 |  | |
| Efudex topical - | 5 % cream |  | |
| Fluoroplex topical - | 1 % 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 provided by your pharmacist before you start using this medication and each time you get a refill. If you have any questions, consult 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, 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.
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 2022. 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.
