fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak)

Dosing and uses of Fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak)

• Adult
• Pediatric

 

Adult dosage forms and 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

 

Pediatric dosage forms and strengths

Not recommended

 

Fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak) adverse (side) 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

Avoid prolonged exposure to sunlight or other UV irradiation

Superficial BCC treatment only when conventional methods are impractical, since conventional methods have better response rate

 

Pregnancy and lactation

Pregnancy category: X

Lactation: Unknown; not recommended

 

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 of Fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak)

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