Fluorouracil

Registered South African indications:

• Solar and senile keratoses
• Bowen’s disease
• Single or multiple superficial basal-cell carcinomas
• Premalignant conditions and superficial basal-cell carcinomas in radiation damaged skin

Nodular basal-cell and squamous-cell carcinoma do not respond to fluorouracil treatment

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy, nor where pregnancy cannot be excluded

Cautions

• Contact with eyes and mucous membranes
• Large surface areas
• Exposure to ultraviolet radiation
• Occlusive dressings
• Encephalopathy
• Patients who have had high-dose pelvic radiation
• Patients on a controlled sodium diet
• Coadministration with folinic acid
• Live vaccines

Forms avail. in SA and covered in this monograph: oin

Fluorouracil should only be used under strict medical supervision

Solar and senile keratoses

• Topical (oin): Apply a thin layer to affected area(s), 1-2 times dly, generally without a dressing

Bowen’s disease
Single or multiple superficial basal-cell carcinomas
Premalignant conditions and superficial basal-cell carcinomas in radiation-damaged skin

• Topical (oin): For all other conditions (including keratosis palmaris), apply a fresh occlusive dressing daily; Continue treatment up to the ulceration stage in the case of basal-cell carcinoma and up to the erosion stage in the case of other types of lesions; Treatment duration: Usually 3-4 weeks, but it may prove necessary to exceed this on occasion

The total area of skin being treated with fluorouracil at any one time should not exceed 500cm² (approx. 23 x 23 cm). Larger areas should be treated a section at a time

The ointment should not be allowed to come into contact with mucous membranes or the eyes. The hands should be carefully washed after applying

No information available

Pregnancy

• Contraindicated
• There are no adequate and well-controlled studies in pregnant women, however, foetal defects and miscarriages have been reported
• Women of childbearing potential should be advised to avoid becoming pregnant and use an effective method of contraception during treatment with fluorouracil and up to 6 months afterward
• If the drug is used during pregnancy, or if the patient becomes pregnant while taking the drug, the patient should be fully informed of the potential hazard to the foetus and genetic counseling is recommended
• Fluorouracil should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus

Breastfeeding

• Contraindicated
• Since it is not known whether fluorouracil passes into breast milk, breast-feeding must be discontinued if the mother is treated with fluorouracil

Fertility

• Men treated with fluorouracil are advised not to father a child during and for up to 6 months following cessation of treatment. Advice on conservation of sperm should be sought prior to treatment because of the possibility of irreversible infertility due to therapy with fluorouracil

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• No dose adjustment recommended

Elderly            

• No dose adjustment recommended

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dysgeusia
• Headache
• Dizziness

Gastrointestinal Disorders

• Haemorrhagic diarrhoea 
• Diarrhoea
• Nausea and vomiting
• Abdominal pain
• Stomatitis

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Urticaria
• Rash 
• Erythemas 
• Erythema multiforme
• Dermal and epidermal conditions
• Skin and subcutaneous skin ulcerations
• Dermatitis 
• Eczema 
• Blisters
• Alopecia 
• Skin pain
• Increased sensitivity to sunlight
• Mucosal inflammation

Immune, Blood and Lymphatic System Disorders

• Haematological disorders
• Pancytopenia
• Neutropenia
• Thrombocytopenia
• Leucocytosis
• Allergic conditions 
• Pyrexia

Sensory Disorders

• Conjunctival irritation
• Keratitis
• Increased lacrimation

• Folinic acid
• Leucovorin
• Nucleoside analogues
• Sorivudine 
• Brivudine
• Antimetabolites (e.g. methotrexate)
• Metronidazole
• Cimetidine
• Warfarin 
• Levamisole 
• Phenytoin 
• Clozapine
• Interferon alfa
• Allopurinol
• Thiazide diuretics
• Myelosuppressive agents
• Live vaccines
• Poliomyelitis virus
• Cisplatin
• Cytostatic agents and irradiation therapy
• Vinorelbine

None routine

• This drug should be administered only under the supervision of a qualified physician with extensive experience in cytotoxic treatment

Fluorouracil is a pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the thymidylate synthetase conversion of deoxyuridylic acid to thymidylic acid. Fluorouracil may also interfere with RNA synthesis.

Ointment (per g) 50mg

• Efudix (Mylan) originator

Also available in the following form: Injection.