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Generic Efudex ( Fluorouracil )
Efudex (fluorouracil) is a topical cytotoxic agent indicated for the treatment of multiple actinic keratoses and superficial basal cell carcinoma. Fluorouracil is an antimetabolite that interferes with DNA and RNA synthesis through its conversion to 5-fluoro-2'-deoxyuridine monophosphate, which inhibits thymidylate synthetase. This leads to selective destruction of rapidly proliferating, actinically damaged skin cells while having minimal effect on healthy, normal skin. The inflammatory response that develops during treatment (erythema, erosion, and crusting) is a visible sign of the eradication of precancerous and malignant lesions.
Usual adult dose: For actinic keratoses, apply Efudex 5% cream once or twice daily to the affected area; the 1% cream is applied once daily to facial lesions for a 4‑week treatment course. For superficial basal cell carcinoma, Efudex 5% cream is applied twice daily in an amount sufficient to cover the lesion and a small margin of surrounding skin for 3 to 6 weeks. Only the 5% concentration is indicated for superficial basal cell carcinoma. All applications should be made with a non‑metal applicator, cotton swab, or a gloved fingertip, and the hands must be washed immediately afterward. Occlusive dressings should not be used. Treatment continues until the inflammatory response reaches the erosion and crusting stage; the usual duration is 2 to 4 weeks for actinic keratoses and up to 6 weeks for superficial basal cell carcinoma. Therapy is then stopped and healing occurs over 1 to 2 months.
Dosage form: Topical cream: 1% (10 mg per gram) and 5% (50 mg per gram). Available in tubes of 20 g and 40 g.
Onset of action: A visible inflammatory reaction (erythema, scaling, and mild edema) typically begins within the first week of application. The therapeutic effect relies on the controlled destruction of abnormal cells, which becomes fully evident during the healing phase following cessation of treatment.
Duration of action: Applied once or twice daily for a finite treatment course. The clinical benefit—clearance of actinic keratoses or superficial basal cell carcinoma—is assessed after the post‑treatment healing period, which usually completes 4 to 8 weeks after stopping the cream.
Alcohol recommendation: There is no known systemic interaction between topical fluorouracil and the consumption of alcoholic beverages. However, patients should avoid applying alcohol‑based lotions, astringents, or other irritants to the treatment area, as these can exacerbate skin reactions and cause excessive discomfort.
Most common side effects: Local skin reactions are expected and indicate drug activity: erythema, pain, pruritus, burning, erosion, crusting, scaling, and swelling. The severity varies by treatment site and duration; facial and scalp areas often react more intensely. Secondary complications can include bacterial infection, scarring, and temporary post‑inflammatory hyperpigmentation or hypopigmentation. Fluorouracil may cause photosensitivity, so patients must avoid prolonged sun exposure and use broad‑spectrum sunscreens. Systemic absorption is minimal, but fluorouracil is contraindicated during pregnancy (FDA Category X) and in patients with known dihydropyrimidine dehydrogenase (DPD) enzyme deficiency, as this can lead to severe systemic toxicity even from topical use. Patients should be carefully counselled about the expected treatment‑related skin reaction so that the course is not prematurely discontinued.
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