Fluorouracil topical

Fluorouracil topical is a prescription medication used to treat the symptoms of Actinic (Solar) Keratosis and Superficial Basal Cell Carcinoma. 

• Fluorouracil topical is available under the following different brand names: Efudex, Carac, Fluoroplex, Tolak

Common side effects of Fluorouracil topical include:

• skin redness, followed by dryness, tenderness, and crusting,
• skin peeling or flaking,
• skin darkening or scarring,
• small blood vessels under the skin,
• mild rash, and
• mild irritation at the injection site

Serious side effects of Fluorouracil topical include:

• severe pain or swelling of treated skin,
• severe itching, burning or irritation,
• open skin sores, and
• shedding of dead skin

Rare side effects of Fluorouracil topical include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

 Adult dosage

Cream

• 0.5% (Carac)
• 1% (Fluoroplex)
• 4% (Tolak)
• 5% (Efudex)
• Topical solution
• 2% (Efudex)
• 5% (Efudex)
• Actinic (Solar) Keratoses
• Adult dosage
• Carac: Apply a thin film to the affected area once a day for 2-4 weeks; healing may not be evident for 1-2 months
• Efudex (2% solution): Apply a sufficient amount to cover lesions every 12 hours for 2-4 weeks; healing may not be evident for 1-2 months
• Fluoroplex: Apply a sufficient amount to cover lesions every 12 hours for 2-6 weeks
• Tolak (face, ears, or scalp): Apply a sufficient amount to cover lesions of the affected area(s) once a day for 4 weeks
• Superficial Basal Cell Carcinoma
• Adult dosage
• Efudex 5%: Apply a sufficient amount of cream or solution to cover lesions every 12 hours for 3-6 weeks; may continue the application for up to 10-12 weeks

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, 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, health care provider, or pharmacist first

• Fluorouracil topical has no noted severe interactions with any other drugs.
• Fluorouracil topical has no noted serious interactions with any other drugs.
• Fluorouracil topical has no noted moderate interactions with any other drugs.
• Fluorouracil topical has no noted minor interactions with any other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity to any component
• Women who are or may become pregnant
• Dihydropyrimidine Dehydrogenase (DPD) deficiency

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Fluorouracil topical?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Fluorouracil topical?”

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 the intensity of the reaction may increase
• The drug may be fatal if ingested by pets; avoid allowing pets to contact the drug container or the skin where the drug was applied; store the 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 a 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 the eyes, nose, mouth, or other mucous membranes because irritation, local inflammation, and ulceration can occur
• Avoid treatment in the periocular area; eye disorders, including corneal reactions, have occurred with topical fluorouracil use; avoid accidental transfer of drug into eyes and to the 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 the 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 was 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

• 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

Lactation

• Because many drugs are excreted in human milk and there is some systemic absorption of fluorouracil after topical administration, and because of the 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