fluorouracil topical (Rx)

Brand and Other Names:Efudex, Carac, more...Fluoroplex, Tolak
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Dosing & Uses

AdultPediatric

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

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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)

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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
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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.

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Pharmacology

Mechanism of Action

Interferes with synthesis of DNA & to a lesser extent, RNA

Pharmacokinetics

Absorption: Insignificant (~6%)

Time to peak: 1 hr

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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

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Images

BRAND FORM. UNIT PRICE PILL IMAGE
Adrucil intravenous
-
5 gram/100 mL vial
Adrucil intravenous
-
500 mg/10 mL vial
Adrucil intravenous
-
2.5 gram/50 mL vial
fluorouracil topical
-
0.5 % cream
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % solution
fluorouracil topical
-
2 % solution
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % cream
Carac topical
-
0.5 % cream
Fluoroplex topical
-
1 % cream
Efudex 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
-
5 gram/100 mL vial
fluorouracil intravenous
-
500 mg/10 mL vial
fluorouracil intravenous
-
500 mg/10 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
-
2.5 gram/50 mL vial

Copyright © 2010 First DataBank, Inc.

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Patient Handout

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Patient Education
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.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 (e.g., stinging, watering), trouble sleeping, irritability, temporary hair loss, or abnormal taste in the mouth may also occur.If any of these effects persist or worsen, contact 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 any of these rare but very serious side effects occur: stomach/abdominal pain, bloody diarrhea, vomiting, signs of infection (e.g., fever, chills, persistent sore throat), easy bruising/bleeding, mouth sores.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms: 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.This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: a certain enzyme deficiency (dihydropyrimidine dehydrogenase - DPD).Before using this medication, tell your doctor or pharmacist your medical history, especially of: 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.This medication must not be used during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, inform your doctor right away. Consult your doctor for more details and to discuss reliable forms of birth control.It is not known if this medication passes into breast milk. Due to the potential risk to a nursing infant, breast-feeding is not recommended while using this drug. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

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 between 68-77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. 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 for more details about how to safely discard your product.

Information last revised August 2021. Copyright(c) 2021 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.

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.