fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak)
Classes: Dermatologics, Other; Antineoplastics, Topical
Dosing and uses of Fluorouracil topical (Efudex, Carac, Fluoroplex, Tolak)
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
